Dang Thi Tuyet Anh

• Doctor of Philosophy
• Senior Researcher at Vietnam Academy of Science and Technology

Simple and efficient strategies have been developed for the synthesis of three structurally diverse dipyrrolo[1,2‐a : 2′,1′‐c][1,4]benzodiazepine (DPBD) derivatives. Firstly, two‐component reaction between 4‐aroylpyrrolo[1,2‐a][1,4]benzodiazepines and electron‐deficient internal alkynes in different conditions was applied to obtain isomeric geminal...

Podophyllotoxin, along with its numerous derivatives and related compounds, is well known for its broad-spectrum pharmacological activity, especially for anticancer potential. In this study, several isatin–podophyllotoxin hybrid compounds were successfully synthesized with good yields through microwave-prompted three-component reactions of 2-amino-...

Hydroxamate and lupane triterpenoid derivatives have a wide range of applications due to their interesting biological and pharmacological activities. Our previous study reported the synthesis of new compounds based on the combination of hydroxamate and lupane triterpenoid moieties. Evaluating their in vitro cytotoxicity on Hep-G2 cancer cell line s...

A series of new fluorinated dihydrofurano-napthoquinone compounds were sucessfully synthesized in good yields using microwave-assisted multi-component reactions of 2-hydroxy-1,4-naphthoquinone, fluorinated aromatic aldehydes, and pyridinium bromide. The products were fully characterized using spectroscopic techniques and evaluated for their anti-in...

Epoxy resin has been extensively used in many industrial and daily applications due to its unique properties. However, the high flammability of epoxy has limited its further development. DOPO derivatives, which are organophosphorus compounds, are highly effective components of flame retardant epoxy composites due to their good compatibility with th...

Two different synthetic approaches to novel heterocyclic hybrid compounds of 4-azapodophyllotoxin were investigated. The obtained products were characterized by infrared spectroscopy, nuclear magnetic resonance spectroscopy, and high-resolution mass spectrometry. MTT protocol was then performed to examine the cytotoxic activity of these products ag...

Objective: The study was conducted to evaluate the in vitro acetylcholinesterase (AchE) inhibition activity of novel pyrano[2,3- d]pyrimidine derivatives. Methods: A series of new pyrano[2,3- d]pyrimidine derivatives were synthesized in moderate to good yields (63%-81%) by using microwave-prompted “one-pot” two-step multicomponent reactions of cycl...

A flame‐retardant composite material (designated as GFPA) was prepared by incorporating a blend of polycarbonate‐acrylonitrile butadiene styrene (PC/ABS, 80/20 wt%) and two additives of potassium perfluorobutane sulfonate (PFBS) at 0.5 wt% and graphene nanoplatelets (GNP) at 1 wt%. The structural characterization results indicated that incorporatin...

Betulinic acid derivatives exhibit different biological activity against diversified targets, such as anticarcinogenic activity in experimental animals, anti-HIV, antihyperglycemia, and anti-inflammatory in humans. In this work, we investigated the synthetic procedure of 24-nor-3-oxo-20(29)-lupen-28-oic acid (1) derivatives. Starting from compound...

In this research, microwave‐assisted “one‐pot” multicomponent reactions have been employed for the synthesis of new chromeno[2,3‐d]pyrimidines containing fluorine atoms. The biological significance of the obtained compounds was highlighted by evaluating in vitro for cytotoxic activity against four human cancer cell lines (HepG2, hepatoma carcinoma;...

Objective: The study was conducted to evaluate the in vitro and in silico anticancer activity of fluorinated podophyllotoxin derivatives. Methods: Microwave-assisted multicomponent reactions were carried out in an Anton Paar Microwave Synthetic Reactor Monowave 400 in order to synthesize fluorinated podophyllotoxin derivatives. These products were...

The efficient synthesis of 12‐substituted‐3,4,4a,5,12,12a‐hexahydrobenzo[ b ]acridine‐1,6,11(2 H )‐triones starting from 2‐amino‐1,4‐naphthoquinone, 1,3‐cyclohexanedione, and different (hetero)aromatic aldehydes was developed. These reactions were carried out in acetic acid under microwave irradiation in the presence of p ‐toluenesulfonic acid as c...

749 γ-Butyrolactone, an ester functionality containing five-membered heterocycle, is one of the privileged structures of diverse natural products, such as sesquiterpene lactones and lignan lactones. 1,2 They have attracted considerable attention because of their in vitro cytotoxic, 3-5 anti-malarial, 6 antiH1N1, 7 antimicrobial, 7-9 anti-inflammato...

A convenient two step “one‐pot” four‐component synthetic approach was developed for the synthesis of new 6‐arylated 5‐hydroxy‐benzo[a]phenazine derivatives using 2‐hydroxy‐1,4‐naphthoquinone, a variety of aromatic aldehydes, benzene‐1,2‐diamine, and tetronic acid. In all cases, the synthesis proceeded via three key steps including condensation, Mic...

A series of novel naphthoquinone-fused podophyllotoxins containing fluoro and trifluoromethyl substituents were synthesized in a medium with good yields using two different synthetic approaches: microwave-assisted four-component reactions of 2-hydroxy-1,4-naphthoquinone, tetronic acid, fluorinated arylaldehydes, and ammonium acetate, and microwave-...

A new approach for the synthesis of podophyllotoxin-naphthoquinone compounds using microwave-assisted three-component reactions is reported in this study. Novel podophyllotoxin-naphthoquinone derivatives with modification on ring E were synthesized. All the synthetic compounds were assessed in terms of their cytotoxicity profile against four cancer...

A convenient three‐component synthetic approach was developed en route to new and significative N‐arylated‐dihydrobenzo[g]quinoline‐5,10‐diones using 2‐hydroxy‐1,4‐naphthoquinone, a variety of aromatic aldehydes, and 4‐(arylamino)furan‐2(5H)‐ones. A sequence of steps including Knoevenagel condensation, Michael addition, [1,3]‐hydrogen shift, intram...

Twelve new compounds including 2-aminobenzamide derivatives bearing benzothiazole and phenylamine moiety were designed and synthesized. The synthesized compounds were tested their cytotoxic activity against A549 and SW480 tumor cell lines. Compounds 3a and 3c exhibited cytotoxicity toward A549 cell line with IC 50 values of 24.59 and 29.59 µM, resp...

The green and efficient approach for synthesis of 2-hydroxy-3-(arylmethyl)(4-hydroxy-2-oxo-2,5-dihydrofuran-3-yl)-1,4-naphthoquinones starting from 2-hydroxy-1,4-naphthoquinone, tetronic acid, and aromatic aldehydes was developed. These reactions were carried out in ethanol under microwave irradiation in the presence of ammonium acetate as catalyst...

Tóm tắt: Các dẫn xuất azide của isatin là các chất đầu cần thiết cho phản ứng click để tạo ra dị vòng 1,2,3-triazole. Các dẫn xuất N-(ω-bromoalkyl)isatin cần cho chuyển hoá được tổng hợp từ phản ứng thế nucleophile của các isatin tương ứng với các dibromoalkane thích hợp. Một số N-(ω-azidoalkyl)isatin có chứa nhóm thế hoặc không thế ở vòng benzene...

New approach for the introduction of a perfluoroalkynyl fragment into 1-R2–2-methyl-1,2,3,4-tetrahy- droisoquinolines has been developed. Synthesized 1,1-disubstituted isoquinoline compounds under the action of methyl propiolate (24 ◦C) and acetylacetylene (-17 ◦C) in trifluoroethanol are converted into 6-perfluoroalkyl substituted allene benzaze...

Novel 1,4-pyranonaphthoquinone derivatives were successfully synthesized via the microwave-assisted three-component reaction of 1,4-naphthoquinone, malononitrile, and various arylaldehydes in ethanol in the presence of 4-(dimethylamino)pyridine (DMAP) as a catalyst, and subsequently evaluated in terms of their antimicrobial and antifungal activitie...

For the first time the 4-dimethylaminopyridine (DMAP) catalyzed straightforward and efficient procedure has been developed for the synthesis of 3,3′-(arylmethylene) bis(2-hydroxynaphthalene-1,4-dione) derivatives starting from lawsone (2-hydroxy-1,4-naphthoquinone) and a variety of (hetero)aromatic aldehydes in ethanol under microwave irradiation....

A facile and efficient synthesis of novel naphthoquinone-based chalcone hybrids (7 and 24) via the microwave-assisted one-pot three-component reactions of 2-substituted-1,4-naphthoquinones, N,N-dimethylformamide dimethyl acetal (DMF-DMA), and acetophenone derivatives has been reported. Whereas the synthesis of hybrids 7 proceeded via a condensation...

Substituted N-propargyl isatins were synthesized by SN2 reaction of corresponding substituted isatins with propargyl bromide in the presence of anhydrous K2CO3 as base. We reported about study on systematically synthesis of these compounds using heating procedures under different reaction conditions, including microwave-assisted heating conditions...

Lycopene and resveratrol are well-known for their high bioactivity, anti-inflammatory effects, and strong antioxidant properties. The combination of lycopene and resveratrol was synergistic in the potentializing immunity of the mammal body. In this study, the scalable co-encapsulation of lycopene and resveratrol into polymeric nanoparticles was per...

An efficient method was developed to prepare a series of novel 3-benzoyl-4H-benzo[g]chromene-5,10-dione derivatives from 2-hydroxy-1,4-naphthoquinone, aromatic aldehydes and arylenaminones in glacial acetic acid under microwave irradiation. This transformation presumably occurs via a Knoevenagel condensation – dehydration – Michael addition – O-cyc...

A convenient microwave-assisted one-pot four-component synthetic approach was developed en route to novel functionalized benzo[a]pyridazino[3,4-c]phenazine derivatives starting from 2-hydroxy-1,4-naphthoquinone, aromatic aldehydes, methyl hydrazine and o-phenylenediamine. Nine new derivatives were successfully synthesized and subsequently evaluated...

Genus Styrax belongs to the family Styracaceae, which is widely distributed in tropical and subtropical regions and has been applied in pharmacological uses and food chemical products. Original research articles related to Styrax plants are now abundant, but there has not been an overview account to demonstrate the highlights in phytochemical and p...

Synthesis of novel 3-arylated 2-hydroxy-1,4-naphthoquinone derivatives via microwave-assisted three-component reaction starting from 2-hydroxy-1,4-naphthoquinone, tetronic acid, and various aromatic aldehydes has been described. This multicomponent domino reaction proceeded through the Knoevenagel condensation, Michael addition, deprotonation, and...

A series of novel podophyllotoxin-naphthoquinone compounds 5a-p were synthesized in good yields using microwave-assisted four-component reactions of 2-hydroxy-1,4-naphthoquinone, aromatic benzaldehydes, tetronic acid and ammonium acetate. All the synthezied compounds were fully characterized by spectral data and evaluated for their cytotoxicity act...

Zinc oxide nanoflakes were synthesized using the wet precipitation method from aqueous solutions of zinc nitrate and sodium hydroxide. The obtained materials were characterized by means of X-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy, and nitrogen adsorption–desorption methods. The presence of sodium laur...

The title compound, C21H23NO4S, obtained by alkaline treatment of 1,5-bis­(1-phen­oxy)-3-aza­pentane at moderate heating, is a N-tosyl­ated secondary vinyl­amine. An intra­molecular S=O⋯H—C hydrogen bond generates a 13-membered ring. The benzalacetone moiety adopts a trans conformation with respect to the C=C double bond, which is slightly longer t...

Synthesis of novel indeno[1,2-c]isoquinoline derivatives, functionalized at the D ring and bearing 1,2,3-triazole unit, has been reported. These hybrid compounds display cytotoxic activity against two human cancer cell lines – KB and HepG2 with half maximal inhibitory concentration (IC50) values in a range of 20–40 μM.

Five 2-aroyl-5-bromo­benzo[b]furan-3-ol compounds (two of which are new) and four new 2-aroyl-5-iodo­benzo[b]furan-3-ol compounds were synthesized starting from salicylic acid. The compounds were characterized by mass spectrometry and ¹H NMR and ¹³C NMR spectroscopy. Single-crystal X-ray diffraction studies of four com­pounds, namely, (5-bromo-3-hy...

A series of new hydroxamate derivatives of lupane triterpenoids has been designed and successfully synthesized. The synthesized compounds were evaluated for their in vitro antitumor activity using the 3-[4,5-dimethylthiazol-2-yl]−2,5-diphenyltetrazolium bromide-based assay against the human cancer cell lines KB and HepG2. Most of these derivatives...

The occurrence and fate of antibiotic compounds in water can adversely affect human and animal health; hence, the removal of such substrates from soil and water is indispensable. Herein, we described the synthesis method of mesoporous carbon (MPC) via the pyrolysis route from a coordination polymer Fe-based MIL-53 (or MIL-53, shortly). The MPC stru...

Two γ-piperidone compounds from domino reaction of aldehyde, ketone, ammonium acetate and two piperidone oximes from reaction of γ-piperidone and hydroxylamine were prepared using ultrasonic sound. Compared with conventional method, ultrasonic sound accelerated the formation of target compounds in shorter time with better yield. The chemical struct...

The unexpected domino transformation of perhydrotriazinothioazacrown ether with dimethyl acetylenedicarboxylate (DMAD) was studied. Triazoline derivatives were separated from reaction mixture and their structures were determined by IR, 1 H NMR and MS spectra. According to the HPLC-MS data, an (azirino)azacrown ether and its dimer, trimer were forme...

Carboxyl‐terminated poly(acrylonitrile‐co‐butadiene) (CTBN)‐grafted epoxidized linseed oil (ELO) (CTBN‐g‐ELO) was synthesized and used as an effective toughener to simultaneously enhance the mechanical properties and fracture toughness of epoxy resin (EP). The ELO was fabricated from linseed oil via epoxidation processing. The characteristics of th...

A new benzofurane 7-methoxy-2-(3-hydroxy-4-methoxyphenyl)-benzofuran-5-carboxylate (1) and 5 known compounds, such as propacin (2), hisbiscolatone A (3), heliclactone (4), rosmarinic acid (5), and syringaldehyde (6), were isolated from methanol extract of the Helicteres hirsuta stems. Their structures were elucidated by spectroscopic analysis as Nu...

In this study, Fe 3 O 4 nanoparticles used as an adsorbent for the removal of toxic gases were successfully synthesized via the facile coprecipitation method. The Fe 3 O 4 nanoparticles displayed a well-defined morphology with the size of ∼10 nm and a porous structure with a specific area of 115.90 m ² /g and a wide range of pore sizes. These nanop...

In this research, nanostructured magnesium oxide was synthesized through the sol-gel calcination or hydrothermal calcination method using various surfactants. The X-ray diffraction pattern of the materials confirmed that all the prepared magnesium oxide samples were single phase without any impurity. The scanning electron microscopy images and spec...

In order to find out the influence of carboxylic acid functionalities in the N-lactam side chains of indenoisoquinolines on cytotoxic activities, several new compounds have been synthesized and structurally characterized by analytical and spectral methods. The incorporation of a carboxylic acid group into the lactam side chain of indenoisoquinoline...

A series of 4-anilinoquinazoline-triazole-AZT hybrids were designed and synthesized as anticancer agents. Their cytotoxic potential has been evaluated by means of a micro-dilution assay against three human cancer cell lines (KB, epidermoid carcinoma; HepG2, hepatoma carcinoma; SK-Lu-1, non-small lung cancer). The biological results revealed that co...

Hemiasterlin is a potent antimitotic agent acting through inhibition of microtubule depolymerization. For this reason, the synthesis of new hemiasterlin derivatives has attracted a lot of interest in the organic chemistry community recently. In this paper, the synthesis and evaluation of the cytotoxicity of new simplified and racemic hemiasterlin d...

1-(p-Methoxyphenyl)tetrazolyl-substituted 6,7-dimethoxy(6,7-methylenedioxy)-1,2,3,4-tetrahydroisoquinolines formed tetrazolyl-substituted azocines in high yields by using activated alkynes. Unsubstituted at 6,7,8-aromatic fragment 1-tetrazolylisoquinoline interacted in several pathways forming tetrazolyl-substituted azocines, 1-tetrazolyl-1-R-vinyl...

In this research several series of novel dioxygenated ring fused 4-anilinoquinazolines (10a-d) and 4-anilinoquinazoline-substituted triazole hybrid compounds (11-14) have been designed and synthesized. Their biological significance was highlighted by evaluating in vitro for anticancer activities, wherein several compounds displayed excellent activi...

Series of novel artemisinin derivatives were designed and synthesized in which the amino propanol group was bonded to the artemisinin nucleus through C-C linkage. Ten new compounds were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.

Series of novel triterpenoid hybrids were designed and synthesized by introducing 2-aminobenzamide moiety at C28 position of triterpenoid derivatives. Thirteen new conjugates were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.

The syntheses of nine new 5-iodo­salicylic acid-based 1,3,4-oxa­diazo­line derivatives starting from methyl salicylate are described. These compounds are 2-[4-acetyl-5-methyl-5-(3-nitro­phen­yl)-4,5-di­hydro-1,3,4-oxa­diazol-2-yl]-4-iodo­phenyl acetate (6a), 2-[4-acetyl-5-methyl-5-(4-nitro­phen­yl)-4,5-di­hydro-1,3,4-oxa­diazol-2-yl]-4-iodo­phenyl...

Several substituted triazole–artemisinin hybrids were synthesized based on ‘click’ chemistry between propargyl‐substituted derivatives and artemisinin containing a 2‐hydroxypropane unit. The structures of all obtained compounds were confirmed by means of IR, NMR, and MS spectroscopy. Four new hybrids were evaluated as cytotoxic agents, revealing an...

Betulin was converted to the corresponding alkyne-functionalized esters and amides and subsequently deployed as substrates for a 'click' chemistry-mediated coupling with 3'-azido-3'-deoxythydimine (AZT) to furnish a novel betulin-triazole-AZT hybrid compounds. Eleven new hybrids were thus successfully prepared and evaluated as cytotoxic agents, rev...

A novel ordered mesoporous catalyst was prepared from rice husk (MRH catalyst) through condensation–evaporation method in alkaline media. The process used cetyltrimethylammonium bromide (CTAB) as a structure-directing agent (template) and sulfonated biochar obtained from partial rice husk carbonization (SBRH) as precursor. Various parameters such a...

[Figure not available: see fulltext.] 1-Tetrazolyl-substituted tetrahydro-β-carbolines undergo a reaction with activated alkynes (acetylacetylene, methyl propiolate, and dimethyl acetylenedicarboxylate) over 4–8 days in MeOH or 1 day in CF3CH2OH with the formation of multicomponent mixtures, from which spiro[indole-3,4'-pyridines] were isolated chr...

Novel ester derivatives of betulin with AZT, d4T, and 3TC were synthesized and assessed for antitumor activities against the KB and HepG2 human cancer cell lines in vitro by MTT assay. Some derivatives displayed high anticancer properties, with IC50 values between 1 and 21 μM on the two cancer cell lines.

Condensations of 1,5-bis(2-formylphenoxy)-3-oxapentane (1a) or 1,8-bis(2-formylphenoxy)-3,6-dioxanoctane (1b) podands and 1,8-bis(2-acetylphenoxy)-3,6-dioxanoctane (2) gave two novel crown ethers: tetrakis-(benzo)-31-crown-7 ether (5) and tetrakis(benzo)-34-crown-8 ether (6). Their molecular structures were established by IR, NMR and MS methods.

The title compound, C24H29NO4, is the product of a Petrenko–Kritchenko condensation of 1,5-bis­(2-formyl­phen­oxy)-3-oxa­pentane, pentan-3-one and methyl­ammonium acetate in ethanol. The mol­ecule has mirror symmetry. The aza-14-crown-3 ether ring adopts a bowl conformation stabilized by a weak intra­molecular C—H⋯O hydrogen bond. The conformation...

Six novel biological active podands based on N-arylthiosemicarbazide were synthesized from 1,5-bis(2-formylphenoxy)-3-oxapentane or 1,8-bis-(2-formylphenoxy)-3,6-dioxaoctane. All podands have tested cytotoxicity on human cancer cell lines RL, MCF7, RD, and HepG2 and antimicrobial activity.

Dihydroartemisinin was converted to its corresponding alkyne-functionalized esters, which were subsequently deployed as substrates for a ‘click’ chemistry-mediated coupling with 3’-azido-3’-deoxythydimine (AZT) to furnish novel triazole–artesunate–AZT hybrid compounds. Moreover, various substituted triazole–artemisinin hybrids were synthesized base...

A convenient one-pot multicomponent synthetic approach was developed for the synthesis of novel 2-aryl-3-benzoyl-1H-benzo[f]indole-4,9-diones using 2-amino-1,4-naphthoquinone, N-acylmethylpyridinium bromides, and a variety of aromatic aldehydes.

The synthesis of various substituted triazole-indenoisoquinoline hybrids was performed based on a CuI-catalyzed 1,3-cycloaddition between propargyl-substituted derivatives and the azide-containing indenoisoquinoline. Besides, a variety of N-(alkyl)propargylindenoisoquinolines was used as substrates for the construction of triazole-indenoisoquinolin...

Tuberculosis has remained a challenge for medicinal chemists worldwide. In the framework of a collaborative program to identify and evaluate novel antitubercular candidate compounds, the biological properties of benzo[g]isoquinoline-5,10-diones have been found to be very promising. In this paper we have further expanded the library by incorporation...

Six novel 9-(arylidene)amino-11-(2-hydroxyphenyl)-8-oxa-12-azatricyclo[7.3.1.02,7]-tridecatrienes incorporating formally 1,5-oxazocine moiety were synthesized by one step protocol from 2,6-di(2-hydroxyphenyl)-4-oxopiperidines with aromatic aldehydes and ammonium acetate.

2-hydroxy-1-naphthaldehyde was synthesized from β-naphthol and chloroform in ethanol and sodium hydroxide solution. Then, salen ligand was synthesized from the condensation reaction of (R,R)-1,2-cyclohexanediamine and 2-hydroxy-1-naphthaldehyde. Complexes were synthesized from the ligand and transition metals including Cu(II), Co(II), Ni(II) Fe(III...

2-Aza-anthraquinones can be found in nature. Many of these azaanthraquinones derivatives have indeed been discovered to possess diverse and pronounced biological activities, including antimicrobial, antiparasitic, antiviral and anticancer properties. These compounds have been shown to be an intercalating agent to DNA. In continuation of our synthet...

The synthesis of N-substituted indenoisoquinolines was performed by applying a two-step condensation between 2-carboxybenzaldehyde and phthalide, followed by treatment with various primary amines. N-allylindenoisoquinoline was subsequently selected as a substrate for hydroxybromination, providing 6-(3-bromo-2-hydroxy)indenoisoquinoline as a key int...

A convenient one-pot multicomponent synthetic approach was developed en route to novel functionalized dihydrobenzo[h]cinnoline-5,6-diones using 2-hydroxy-1,4-naphthoquinone, methylhydrazine, and a variety of aromatic aldehydes. Fifteen new derivatives were thus prepared and subsequently evaluated in terms of their cytotoxicity profile, revealing a...

Three-component reactions of tetrahydropyrrolo[1,2-a][1,4]benzodiazepines with methyl propiolate or acetylacetylene and СН, NH, SH, and ОН acids were studied in various solvents. The reaction direction is assumed to depend on the nucleophilicity of anion, formed through deprotonation of acid by the anionic center of initial Michael-type zwitterion.

1,4-Dihydroxy-2-naphthoic acid was used as a substrate for a straightforward five-step synthesis of 3-substituted 1H-benzo[g]isochromene-5,10-diones, with a Michael addition of N-acylmethylpyridinium ylides across 2-hydroxymethyl-1,4-naphthoquinone and a subsequent acid-mediated dehydratation of intermediate hemiacetals as the key steps. The obtain...

One-pot synthesis of ester-linked conjugates of betulinic, ursolic or oleanolic acids with anti-HIV drugs AZT, derivatives of AZT and 3TC was performed, the resulting conjugates having shown high anti-HIV activities.

Betulinic acid and analogous naturally occurring triterpenoid acids were transformed into the corresponding propargyl esters and subsequently deployed as substrates for a click chemistry-mediated coupling with azidothymidine (AZT) en route to novel 1,2,3-triazole-tethered triterpenoid-AZT conjugates. Twelve new hybrids were thus prepared and assess...

Aziridine (IV) is obtained in three steps including reduction of the ester moiety, hydrogenation and tosylation.

A five-step procedure for the synthesis of cis-1-tosyl-2-tosyloxymethyl-3-(trifluoromethyl)aziridine was developed, starting from 1-ethoxy-2,2,2-trifluoroethanol, involving imination, aziridination, ester reduction, hydrogenation, and N-,O-ditosylation steps. Further synthetic elaborations revealed a remarkable difference in the reactivity of cis-1...

A convenient approach toward nonactivated 1-alkyl-2-(trifluoromethyl)azetidines as a new class of constrained azaheterocycles was developed starting from ethyl 4,4,4-trifluoroacetoacetate via imination, hydride reduction, chlorination, and base-induced ring closure. Furthermore, the reactivity profile of these 2-CF(3)-azetidines was assessed by mea...

An efficient and straightforward approach towards the synthesis of 1-alkyl-2-(trifluoromethyl)aziridines starting from 1,1,1-trifluoroacetone via imination, α-chlorination, hydride reduction and ring closure was developed. In addition, novel primary β-iodo amines were obtained by regioselective ring opening of these 2-(trifluoromethyl)aziridines us...