Hitendra M PatelSardar Patel University · Department of Chemistry
Hitendra M Patel
Doctor of Philosophy
Professor, Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar388120. Gujarat, India
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60
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Introduction
Dr Hitendra M. Patel is a Professor of Chemistry at the Department of Chemistry of the Sardar Patel University, V. V. Nagar 388 120, Gujarat, India. He was an Elected Member of the Organic Division Council and was admitted as a Fellow of the Royal Society of Chemistry, London in 2020-23. He acts as Editor and Board member in many international high reputed journals. He has 55 and 27 years of experience in Teaching and Research respectively. He worked as an Expert reviewer in many Journals.
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February 2015 - September 2022
Publications
Publications (60)
A diverse set of 4,7‐dihydro‐[1,2,3]thiadiazolo[5,4‐b]pyridine‐6‐carboxamides 4(a‐o) were synthesized via a one‐pot reaction of 5‐amino[1,2,3]thiadiazole, various aromatic aldehydes, and different acetoacetanilides, using glacial acetic acid as the solvent and without the need for any catalysts. The resulting compounds were obtained in moderate to...
In this study, we describe a one-pot three-component synthesis of bioactive tetrahydopyrimidinecarboxamide derivatives employing lanthanum triflate as a catalyst. Out of the synthesized compounds, 4f had the most potent anti-cancer activity and impeded cell cycle progression effectively. Anti-cancer bioactivity was observed in 4f against liver, bre...
Over the past few years, there has been significant interest in a developing trans-dermal delivery technology due to its ability to effectively deliver therapeutic and cosmeceutical products for various purposes. These applications include vaccines, drugs, and biomolecules aimed at addressing skin-related issues. One major advantage of transdermal...
Abrus precatorius Linn is a woody twinning plant belonging to the Fabaceae family and it is an imperative medicinal plant that is a source of a variety of phytochemicals from its distinct parts which illustrate miscellaneous biological activities such as antioxidant, antidiabetic, antimicrobial, cytotoxic, etc. This review summarizes the isolation...
Abrus precatorius Linn is a woody twinning plant belonging to the Fabaceae family and it is an imperative medicinal plant that is a source of a variety of phytochemicals from its distinct parts which illustrate miscellaneous biological activities such as antioxidant, antidiabetic, antimicrobial, cytotoxic, etc. This review summarizes the isolation...
In this communication, we explored the synthesis of novel alkoxy-functionalised dihydropyrimido[4,5-b]quinolinones using a microwave-assisted multicomponent reaction. All the synthesized molecules were screened for anti-proliferative and anti-invasive activity against glioblastoma cells. 5c shows the most potent anti-proliferative activity with a h...
There is a continuous and pressing need to establish new brain-penetrant bioactive compounds with anti-cancer
properties. To this end, a new series of 4′-((4-substituted-4,5-dihydro-1H-1,2,3-triazol-1-yl)methyl)-[1,1′-
biphenyl]-2-carbonitrile (OTBN-1,2,3-triazole) derivatives were synthesized by click chemistry. The series of
bioactive compound...
In this study, a highly efficient green synthetic protocol was developed for the synthesis of spiroacridines and spiroquinolines via a multicomponent reaction of 3,4 methylenedioxyaniline, isatin and cyclic 1,3-diones in glacial acetic acid. This metal-free multicomponent approach offers mild reaction conditions, shorter reaction time and easy prod...
Owing to the massive importance of dihydropyrimidine (DHPMs) scaffolds in the pharmaceutical industry and other areas, we developed an effective and sustainable one-pot reaction protocol for the synthesis of (R/S)-2-thioxo-DHPM-5-carboxanilides via the Biginelli-type cyclo-condensation reaction of aryl aldehydes, thiourea and various acetoacetanili...
Regardless of the benefits, pharmaceutical companies are reticent to engage further in covalent organic framework‐based drug development and drug delivery systems, preferring rather to explore preexisting chemical compound libraries for drug delivery. As such, this study aims to account for the efficacy of covalent organic frameworks (COFs) in the...
A diverse set of tetrahydrobenzofuran-4(2H)-one derivative 4(a-o) were synthesized using a one-pot treatment of
dimedone, 3-(1H-imidazol-1-yl)benzaldehyde, and different phenacyl bromide by utilizing cesium carbonate as a
cost-effective catalyst in acetonitrile under mild reaction condition. During the synthesis of compounds, two
carbon–carbon (C–C...
In this study, we effectively developed a catalyst-free multicomponent synthesis of 5-((2-aminothiazol-5-yl)(phenyl)methyl)-6-hydroxypyrimidine-2,4(1H,3H)-dione derivatives employing 2-aminothiazole, N',N'-dimethyl barbituric acid/barbituric acid and different aldehydes at 80 °C in an aqueous ethanol medium (1 : 1) using group-assisted purification...
The biomedical, biotech, and food industries all use polysaccharides as vital biomolecules with a variety of applications. Polysaccharides have a great deal of potential as biomaterials, and polysaccharide-based nanogels have attracted a lot of attention as carriers for different bioactive agents due to their unique versatile groups, specifically f...
In this study, imidazo[5,1-b]quinazoline derivatives 4(a–t) were synthesized via a three-component reaction of 5-aminoimidazole-4-carbonitrile, 1,3-cyclohexanedione derivatives and various aromatic aldehydes by employing glacial acetic acid as a reaction medium and without catalyst. This approach affords mild reaction conditions and has operational...
Herein, an efficient synthesis of spiro-indoline-pyrano[3,2-c]quinolines derivatives of spiroxindolines by the water-mediated three-component condensation reaction of 2-hydroxyquinoline-4-one 1(a-b), isatin derivatives 2(a-n), and malononitrile 3 in the presence of water-soluble and phase transfer Tetrabutylammonium bromide (TBAB) catalyst is descr...
The pyranopyrimidine core is a key precursor for medicinal and
pharmaceutical industries due to its broader synthetic applications as well as its bioavailability. Among its four possible isomers, we found that 5H-pyrano[2,3-d]pyrimidine scaffolds have a wide range of applicability, and in recent years, they have been intensively investigated, but t...
An efficient, regioselective, and environmentally benign approach was established using the multicomponent reaction-based synthesis of novel antioxidant spiroquinoline derivatives such as spiro[dioxolo[4,5-g]quinoline], spiro[dioxino[2,3-g]quinoline], and spiro[pyrazolo[4,3-f]quinoline] by reaction of aryl aldehyde, Meldrum's acid, and amine deriva...
Spiro derivatives are important scaffolding substances found in many natural products and pharmaceuticals. In the last decade, numerous new approaches based on multicomponent reactions have been explored for the selective and efficient development of new spiro derivatives using various organocatalytic and transition metal‐based catalytic systems. T...
In this study, we demonstrate a simple, highly efficient, rapid and convenient series of 2,4-dimethoxy-tetrahydropyrimido[4,5-b]quinolin-6(7H)-ones 4a-v. Microwave irradiation facilitates the one-pot multicomponent reaction of different aromatic aldehydes, 6-amino-2,4-dimethoxypyrimidine and dimedone using glacial acetic acid. Metal-free multicompo...
1,2,3-Triazole scaffolds are not obtained in nature, but they are still intensely investigated by synthetic chemists in various fields due to their excellent properties and green synthetic routes. This review will provide a library of all synthetic routes used in the past 21 years to synthesize 1,2,3-triazoles and their derivatives using various me...
A series of N-(4-chlorophenyl) substituted pyrano[2,3-c]pyrazoles was synthesised and screened for their potential to inhibit kinases and exhibit anticancer activity against primary patient-derived glioblastoma 2D cells and 3D neurospheres. A collection of 10 compounds was evaluated against glioma cell lines, with compound 4j exhibiting promising g...
Herein, a solvent-free synthesis of 5-bromothiophene based 3,4-dihydropyrimidin-2-(1H)-(thi)ones was explored. The main advantages of this study are that pure products are readily obtained through an easy workup and without using any separation technique and in good yields (66-80% yield), All the synthesized products were characterized by ¹H and ¹³...
We report a one-pot two-step synthesis of a bioactive 6-amino-2-pyridone-3,5-dicarbonitrile derivative using natural product catalysts betaine and guanidine carbonate. Anti-cancer bioactivity was observed in specific molecules within the library of 16 derivatives. Out of the compounds, 5o had the most potent anti-cancer activity against glioblastom...
Herein, acetic acid mediated multicomponent synthesis of novel 2,4-dimethoxy-tetrahydropyrimido[4,5-b]quinolin-6(7H)-one (2,4-dimethoxy-THPQs) was reported. Single-crystal XRD analysis of four newly developed crystals of 2,4-dimethoxy-THPQs and their DFT study were also reported. The structure of all molecules was optimized using DFT B3LYP/6-31G(d)...
Herein we report a one-pot two-step synthesis of a bioactive 6-amino-2-pyridone-3,5-dicarbonitrile derivative using natural product catalysts betaine and guanidine carbonate. Upon identification of the anticancer bioactivity of the compound, we carried out structure-activity relationship and rationally designed a library of 16 derivatives. Out of t...
Proteasome-addicted neoplastic malignancies present a considerable refractory and relapsed phenotype with patients exhibiting drug-resistance and high mortality rates. To counter this global problem, novel proteasome-based therapies are being developed. In the current study we extensively characterize TIR-199, a syrbactin-class proteasome inhibitor...
Proteasome-addicted neoplastic malignancies present a considerable refractory and relapsed phenotype with patients exhibiting drug-resistance and high mortality rates. To counter this global problem, novel proteasome-based therapies are being developed. In the current study we extensively characterize TIR-199, a syrbactin-class proteasome inhibitor...
Herein, Solvent-free synthesis of 5-bromothiophene based 3,4-dihydropyrimidin-2-(1 H )-thi(ones) was explored. The main advantages of this study are that pure product comes in hand with easy workup and without using any separation technique, a good amount of yield, and formation of product in crude form. We developed a single crystal of 4c , and we...
p>A series of novel pyrano[2,3-c]pyrazoles were synthesized and screened for their potential to inhibit kinases and exhibit anti-cancer activity against primary patient derived glioblastoma 2D cells and 3D neurospheres. A collection of 10 compounds were evaluated against glioma cell lines, with compound 4j exhibiting promising glioma growth inhibit...
In this study, we report on antiproliferative benzyloxy dihydropyrimidinones (DHPMs) produced by the Biginelli reaction of benzyloxy benzaldehyde, urea, and diverse 1,3‐diones. The reaction was catalyzed by lanthanum triflate and completed within 1–1.5 h, with 74–97% yield. The antiproliferative assay was carried out for all synthesized dihydropyri...
Green synthesis of pyrazolo[3,4-b]quinolinones was designed using bioproduct pyridine-2-carboxylic acid (P2CA) as a green and efficient catalyst. The multi-component reaction of aldehydes, 1,3-cyclodiones and 5-amino-1-phenyl-pyrazoles regioselectively produced pyrazolo[3,4-b]quinolinones in excellent yield (84–98%). Recyclization of the catalyst w...
A versatile and substrate oriented multicomponent reaction for the syntheses of novel highly diastereoselective tetrahydro-1′H-spiro[pyrazolo[4,3-f]quinoline-8,5′-pyrimidine]-2′,4′,6′(3′H)-triones (d.r. up to 20 : 1 (syn : anti)) and tetrahydro-8H-pyrazolo[4,3-f]pyrimido[4,5-b]quinoline-8,10(9H)-diones via formation of selective multiple C–C bonds...
A one-pot procedure for the preparation of functionalized 1,4-dihydropyridines by three-component reaction using substituted heterocyclic aldehydes, ammonium acetate, and substituted β-ketoesters catalyzed by L-proline was described. Present protocol offers excellent yield up to 92%, flexibility with different substitution, convenient operation, an...
Nowadays, synthesis of novel nitrogen-bearing heterocyclic scaffolds is a challenging and demanding task as well. In our present work, we demonstrated a novel one-pot pseudo four-component reaction of 3,4-methylenedioxyaniline, N,N-dimethylbarbituric acid, and aryl/heteroaryl aldehyde for the regioselective construction of functionalized 6,8-dihydr...
In this study, we successfully explored the effect of steric hindrance on the one-pot reaction of different aryl aldehydes with malononitrile and N-substituted 2-cyanoacetamide in the presence of piperidinium acetate as the catalyst. It involved the Knoevenagel condensation of the aldehyde and malononitrile to produce arylidene malononitrile as an...
Herein our team explored a promising synthetic trail to Functionalized pyrazolodihydropyridine core using hydroxyl alkyl ammonium ionic liquid via one-pot fusion of 3-methyl-1-phenyl-1H-pyrazole-5-amine, different heterocyclic aldehydes and 1, 3-Cyclic diones. The aimed compounds were obtained by Domino-Knoevenagel condensation and Michael addition...
Herein, we established a straightforward synthetic route for biological relevant [1,2,4]triazolo[5,1‐b]quinazolin‐8(4H)one scaffolds using the group‐assisted purification (GAP) chemistry via one‐pot and three component reaction of 3‐Amino‐5‐methylthio‐1H‐1,2,4‐triazole (1), Aryl aldehyde(2 a–g), and 1,3‐cyclodione (3 a–b) using L‐proline and aqueou...
In this study, we explored the catalyst‐free one‐pot multi‐component synthesis of 1,4‐dihydropyridine derivatives by following green chemistry protocol. The present approach shows the significant outcomes such as yield up to 94%, catalyst‐free reaction, easy workup procedure and shorter period of reaction time. In this work we also highlighted the...
Background
We report here an efficient synthesis of new Mannich products 4(a-m) in excellent yields via multi-component reaction for the condensation of 5-bromothiophene- 2-carboxaldehyde (5-BT-2C), 2,4-dihydroxybenzophenone (2,4-DHBP) and primary/secondary amine derivative using Ethyl Ammonium Nitrate (EAN) as ionic liquid, which is reusable and p...
A novel green and efficient one-pot multicomponent reaction of dihydropyridine derivatives was reported as having good to excellent yield. In the presence of the catalyst ceric ammonium nitrate (CAN), different 1,3-diones and same starting materials as 5-bromothiophene-2-carboxaldehyde and ammonium acetate were used at room temperature under solven...
Background: We developed Multicomponent synthesis for novel Mannich products with biologically active quinoline nucleolus under solvent free condition. This methodology provided us good amount of yield with the exception of chromatographic separation. The structure of novel compounds (4d1-d13) was characterized by elemental, mass,¹H-NMR,¹³C-NMR and...
Background: In these study we report here one-pot multi-component and solvent free Mannich reaction of U.V. absorbing material, five member heterocyclic ring system and amides/carbamates has been efficiently catalyzed by recyclable ethyl ammonium nitrate as ionic liquid at ambient temperature to produce mannich compounds in high yields. This method...
Novel acid mono azo and mordent acid mono azo dyes were synthesized by the coupling of diazonium salt solution of different aromatic amines with 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid. The resulting dyes were characterized by spectral techniques like elemental analysis, IR, 1H-NMR and UV visible spectroscopy. The dyeing performance of all...
The novel mordent and disperse heterocyclic dyes were prepared by coupling of various diazo solution of aromatic amines with 1-[(2-butyl-2,3-dihydrobenzofuran-3-yl)]-1-(4-hydroxyphenyl)methanone. The resultant mordent and disperse heterocyclic dyes were characterized by elemental analyses, IR and 1H-NMR and 13C-NMR spectral studies. The UV-visible...
Aniline derivatives were diazotized and coupled with 3-aminocrotononitrile to give the corresponding 2-arylhydrazono-3-ketiminobutyronitriles. Cyclization of these arylhydrazono derivatives with hydrazine monohydrate afforded 5-amino-4-arylazo-3-methyl-1H-pyrazoles which were subsequently diazotized and coupled with malononitrile to yield a series...
Novel heterocyclic acid and mordant acid dyes were synthesised by the coupling of a diazonium salt solution of different aromatic amines with 2-butyl-3-(4-hydroxybenzoyl)benzofuran. The resulting heterocyclic acid dyes were characterized by elemental analysis, IR, H-1-NMR and C-13-NMR spectral studies and UV-Vis spectroscopy. The dyeing performance...
In the field of dye industries, heterocyclic compounds can play the important role to synthesis the various acid and mordent dyes which can give the variety of shades to different fabrics. Here, new heterocyclic acid and mordent acid dyes were synthesized by the coupling of diazonium salt solution of different aromatic amines having acidic groups w...
Solvent dyes have been prepared by the coupling of diazo solution of different aromatic amines with 2-hydroxy-4-n-octyloxybenzophenone. The resultant dyes were characterized by elemental analysis as well as IR and 1H NMR spectral studies. The UV-Visible spectral data have also been discussed in terms of structure property relationship. The printing...
Novel acid mono azo and mordent acid mono azo dyes were synthesised by the coupling of diazonium salt solution of different aromatic amines with 2-hydroxy-4-methoxybenzophenone. The resulting dyes were characterized by spectral techniques, i.e., elemental analysis, IR, 1H-NMR and UV–visible spectroscopy. The dyeing performance of all the dyes was e...
Novels disperse and mordent azo dyes were prepared by coupling of various diazo solutions of aromatic amines with 2-hydroxy-4-methoxy-benzophenone. The resultant dyes were characterized by elemental analyses, IR and 1 H NMR spectral studies. The UV-visible spectral data have also been discussed in terms of structural property relationship. The dyei...
Novel acid azo and mordent acid azo dyes have been prepared by the coupling of diazo solution of different aminonaphthol sulphonic acids and aromatic amino acids with 2,4-dihydroxybenzophenone. The resultant dyes were characterized by elemental analysis as well as IR and 1H NMR spectral studies. The UV-visible spectral data have also been discussed...
The novel mordent and disperse heterocyclic dyes were prepared by coupling of various diazo solution of aromatic amines with 2-Butyl-3-(4-hydroxybenzoyl)benzofuran. The resultant mordent and disperse heterocyclic dyes were characterized by elemental analyses, IR and NMR spectral studies. The UV-visible spectral data have also been discussed in term...
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