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Unprecedented one-pot synthesis of 3,4-dihydropyrimidine-2-(1h)-ones catalyzed by hydrazine sulfate through Biginelli reaction, ADMET property, molecular docking studies and their antibacterial activity on Bacillus brevis and E. coli 在硫酸肼催化下通过 Biginelli 反应前所未有地一步合成 3,4-二氢嘧啶-2-(1h)-酮、ADMET 特性、分子对接研究及其对布氏杆菌和大肠杆菌的抗菌活性
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-27 DOI: 10.1080/00397911.2024.2405931
{"title":"Unprecedented one-pot synthesis of 3,4-dihydropyrimidine-2-(1h)-ones catalyzed by hydrazine sulfate through Biginelli reaction, ADMET property, molecular docking studies and their antibacterial activity on Bacillus brevis and E. coli","authors":"","doi":"10.1080/00397911.2024.2405931","DOIUrl":"10.1080/00397911.2024.2405931","url":null,"abstract":"<div><div>The syntheses of 3,4-dihydropyrimidin-2(1<em>H</em>)-ones by one-pot, three-component condensation of aldehydes, β-ketoesters and urea or thiourea have been made more simple and efficient by using 20 mol% hydrazine sulfate as catalyst. Aldehydes, β-ketoesters and urea are cyclocondensed in the presence of hydrazine sulfate to produce dihydropyrimidines in ethanol under reflux conditions. The advantages of using hydrazine sulfate as a catalyst over the traditional Biginelli reaction conditions include outstanding yields (80–91%) and a shorter (10–15 hours) reaction time. In order to evaluate the antibacterial efficiencies of the synthesized compounds, we have studied the inhibitions of microbial proliferation of both Gram-positive (<em>Bacillus brevis</em>) and Gram-negative (<em>E. coli</em>) bacterial strains in comparison to a control group. The microbial inhibitions occur in the range of 40–98% by different derivatives of dihydropyrimidinones. Molecular docking studies of the synthesized compounds have also been done using software tools such as SwissADME.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142427565","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design, synthesis, characterization and biological evaluation of coumarin bound 1,2,3-triazoles using click chemistry 利用点击化学设计、合成与香豆素结合的 1,2,3-三唑，并对其进行表征和生物学评价
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-26 DOI: 10.1080/00397911.2024.2407435
{"title":"Design, synthesis, characterization and biological evaluation of coumarin bound 1,2,3-triazoles using click chemistry","authors":"","doi":"10.1080/00397911.2024.2407435","DOIUrl":"10.1080/00397911.2024.2407435","url":null,"abstract":"<div><div>In an endeavor to invent new antimalarial and antimicrobial agents, a series of coumarin bound 1,4-disubstituted 1,2,3-triazoles was synthesized through Cu(I)-promoted click reaction between coumarin bound terminal alkynes, that is, 4/7-(prop-2-yn-1-yloxy)-2<em>H-</em>chromen-2-one and 2-azido-<em>N</em>-arylpropanamides. The synthesized 1,2,3-triazoles were characterized by FTIR,<sup>1</sup>H NMR,<sup>13</sup>C NMR, and HRMS techniques and were assessed for <em>in vitro</em> antimalarial activity against <em>Plasmodium falciparum</em> as well as <em>in vitro</em> antimicrobial activity against four bacterial strains (<em>Staphylococcus aureus</em>, <em>Bacillus subtilis</em>, <em>Escherichia coli</em>, and <em>Klebsiella pneumoniae</em>) and two fungal strains (<em>Candida albicans</em>, <em>Aspergillus niger</em>). Compound <strong>7o</strong> [(<em>N</em>-(4-fluorophenyl)-2-(4-(((2-oxo-2<em>H</em>-chromen-7-yl)oxy)methyl)-1<em>H</em>-1,2,3-triazol-1-yl)propanamide)] displayed better activity against <em>P. falciparum</em> while compound <strong>7y</strong> [(<em>N</em>-(3-nitrophenyl)-2-(4-(((2-oxo-<em>2H</em>-chromen-7-yl)oxy)methyl)-<em>1H</em>-1,2,3-triazol-1-yl)propanamide)] displayed excellent activity against all the tested bacterial and fungal strains, amongst the synthesized triazoles. Also, the molecular docking studies of the most potent compounds against DNA gyrase (<em>S. aureus</em>) were also performed to have an insight on binding interactions.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142528227","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
L-proline catalyzed one-pot synthesis of benzoxanthenes in aqueous medium 水介质中 L-脯氨酸催化苯并氧杂蒽的一步法合成
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-19 DOI: 10.1080/00397911.2024.2403141
{"title":"L-proline catalyzed one-pot synthesis of benzoxanthenes in aqueous medium","authors":"","doi":"10.1080/00397911.2024.2403141","DOIUrl":"10.1080/00397911.2024.2403141","url":null,"abstract":"<div><div>An operationally simple, cost-effective, and environmentally benign method has been described for the synthesis of various polysubstituted benzoxanthenes via L-proline-catalyzed three-component condensation of β-naphthol, aromatic aldehydes, dimedone, or 2-hydroxy-1,4-naphthoquinone in aqueous medium. This process has additional benefits such as simple product isolation and purification techniques, good to higher yields, and above all, efficient catalyst reusability. The addition of sodium dodecyl sulfate is an extra benefit to speed up this reaction.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142426878","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Scalable synthesis of tranexamic acid under modest reaction conditions using early stage isomerization of dimethyl 1,4-cyclohexanedicarboxylate as a key step 以 1,4-环己烷二羧酸二甲酯的早期异构化为关键步骤，在适度反应条件下规模化合成氨甲环酸
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-14 DOI: 10.1080/00397911.2024.2399795
{"title":"Scalable synthesis of tranexamic acid under modest reaction conditions using early stage isomerization of dimethyl 1,4-cyclohexanedicarboxylate as a key step","authors":"","doi":"10.1080/00397911.2024.2399795","DOIUrl":"10.1080/00397911.2024.2399795","url":null,"abstract":"<div><p>A commercially scalable five-step synthetic process starting from cis/trans (7:3) mixture of dimethyl 1,4-cyclohexanedicarboxylate is devised for preparation of tranexamic acid with more than 99.5% purity. All impurities are controlled as per monograph. 47% overall yield over five steps has been achieved based on recovery. Epimerization of a cis-predominant isomeric mixture to trans predominant isomeric mixture under mild conditions followed by exploiting the difference in solubility to obtain trans isomer in very high purity is the key feature of the synthesis. In addition to this, use of readily available and cost efficient raw materials/reagents, recycling of cis isomer, explicit design of downstream processing enabling the retention of the trans-stereochemistry until final API are some of the highlights of this synthesis. This process also circumvents the use of hazardous chemicals and harsh reaction conditions making it greener and safer compared to the previous reports.”</p></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142229238","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Deoxygenation of benzylphenyl sulfones using 1,2-bis(diphenylphosphino)ethane (dppe)/NBS under metal-free conditions 在无金属条件下使用 1,2-双（二苯基膦）乙烷 (dppe)/NBS 对苄基苯砜进行脱氧反应
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-14 DOI: 10.1080/00397911.2024.2401135
{"title":"Deoxygenation of benzylphenyl sulfones using 1,2-bis(diphenylphosphino)ethane (dppe)/NBS under metal-free conditions","authors":"","doi":"10.1080/00397911.2024.2401135","DOIUrl":"10.1080/00397911.2024.2401135","url":null,"abstract":"<div><p>An efficient route for the chemoselective deoxygenation of benzylphenyl sulfones to the corresponding sulfides has been developed using a mixture of 1,2-bis(diphenylphosphino)ethane(dppe) and NBS as an effective promoter. This is the first development on the deoxygenation of diverse benzylphenyl sulfones under metal-free conditions. The mild reaction conditions, formation of the water soluble by-product and tolerance of a wide range of functional groups promote its broad applications in organic synthesis.</p></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142228868","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
An efficient one-step synthesis of a new series of mutifunctional olefins and direct hydroxymethylation of α-substituted β-keto esters 一步法高效合成一系列新的突变官能团烯烃和直接羟甲基化α-取代的β-酮酯
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-13 DOI: 10.1080/00397911.2024.2403775
{"title":"An efficient one-step synthesis of a new series of mutifunctional olefins and direct hydroxymethylation of α-substituted β-keto esters","authors":"","doi":"10.1080/00397911.2024.2403775","DOIUrl":"10.1080/00397911.2024.2403775","url":null,"abstract":"<div><div>An efficient one-step procedure for the synthesis of a new series of multifunctional olefins by condensation of α-substituted β-diketones as well as β-phosphonoesters and benzoylated β-ketoesters with formaldehyde, using potassium carbonate in refluxing THF, followed by a deacylation reaction, is herein described. In contrast, the α-substituted β-keto esters, bearing an acyl moiety, only undergo a hydroxymethylation reaction, with no metal catalysts/activating agents, as is usually required for the process, affording the corresponding α-hydroxymethyl β-keto esters in high yields.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142251672","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
An efficient, green and solvent-free three-component synthesis of 2,4,6-triarylpyridines utilizing ZSM-5 as a heterogeneous catalyst 利用 ZSM-5 作为异相催化剂高效、绿色、无溶剂地合成 2,4,6-三芳基吡啶的三组分方法
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-12 DOI: 10.1080/00397911.2024.2403779
{"title":"An efficient, green and solvent-free three-component synthesis of 2,4,6-triarylpyridines utilizing ZSM-5 as a heterogeneous catalyst","authors":"","doi":"10.1080/00397911.2024.2403779","DOIUrl":"10.1080/00397911.2024.2403779","url":null,"abstract":"<div><div>ZSM-5, an efficient and reusable heterogeneous catalyst, is employed for the one-pot, three-component synthesis of 2,4,6-triarylpyridines from substituted benzaldehydes, acetophenones and ammonium acetate using a simple, efficient, and green method. Both electron-releasing and withdrawing aldehydes and ketones went smoothly into substituted 2,4,6-triarylpyridines. Notably, the present reaction was carried out in the solvent-fee condition. The key merits of the present protocol are the milder reaction condition, easy workup protocol, high yield of desired pyridines and recyclability and reusability of the catalyst. The developed protocol offers a broad scope of substrate applicability and good sustainability.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142427825","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
An environment-friendly phosphotungstic acid catalyzed cross-dehydrogenative coupling reaction to synthesize 9-substituted-9H-xanthenes with photoelectrochemical performance 以环境友好型磷钨酸催化交叉脱氢偶联反应合成具有光电化学性能的 9-取代-9H-氧杂蒽
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-12 DOI: 10.1080/00397911.2024.2402833
{"title":"An environment-friendly phosphotungstic acid catalyzed cross-dehydrogenative coupling reaction to synthesize 9-substituted-9H-xanthenes with photoelectrochemical performance","authors":"","doi":"10.1080/00397911.2024.2402833","DOIUrl":"10.1080/00397911.2024.2402833","url":null,"abstract":"<div><div>An environment-friendly phosphotungstic acid catalyzed cross-dehydrogenative coupling reaction for the synthesis of 9-substituted-9H-xanthenes under oxygen and solvent-free conditions have been developed. The economic and practical reaction exhibited good substrate applicability tolerance, various 9-substituted-9H-xanthenes were synthesized in moderate to excellent yields by tuning the ratio of xanthenes and ketones (22 examples, up to 99% yield). By testing the photoelectrochemical performance, some of the xanthene derivatives (<strong>10c</strong>, <strong>12c</strong>, <strong>13c</strong> and <strong>2d</strong>) showed stable photocurrent value, especially <strong>2d</strong> had better cathode photocurrent value and application potential.</div></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142426889","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of furo[2,3-c]carbazoles as potent α-glucosidase and α-amylase inhibitors 合成呋喃并[2,3-c]咔唑类强效 α-葡萄糖苷酶和 α-淀粉酶抑制剂
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-10 DOI: 10.1080/00397911.2024.2401628
{"title":"Synthesis of furo[2,3-c]carbazoles as potent α-glucosidase and α-amylase inhibitors","authors":"","doi":"10.1080/00397911.2024.2401628","DOIUrl":"10.1080/00397911.2024.2401628","url":null,"abstract":"<div><p>The carbazole-3-carbaldehyde <strong>2</strong>, produced by <em>N</em>-ethyl carbazole <em>via</em> Vilsmeier-Haack reaction, was subjected to Dakin type oxidation with H<sub>2</sub>O<sub>2</sub> and H<sub>2</sub>SO<sub>4</sub> in methanol to produce the carbazole-3-ol <strong>3</strong>. The reaction of <strong>3</strong> with a range of commercially available α-haloketones <strong>4a–f</strong> in the presence of Al<sub>2</sub>O<sub>3</sub> as catalyst in xylene led to their regio-selective cyclization to afford the furo[2,3-c]carbazoles <strong>5a–f</strong>. Identification of the furo[2,3-c]carbazoles <strong>5a–f</strong> were performed through <sup>1</sup>H NMR,<sup>13</sup>C NMR, FT-IR and high resolution mass spectrometry. Single crystal X-ray diffraction analysis was employed to further confirm the structures of the some of the targeted compounds. <em>In vitro</em> antidiabetic activities of the newly synthesized furocarbazoles <strong>5a–e</strong> were investigated utilizing α-glucosidase and α-amylase enzymes. The biological evaluation revealed the obvious efficiencies of the targeted molecules toward the α-glucosidase enzyme inhibition with the potent IC<sub>50</sub> values compared to the standard acarbose. In the case of α-glucosidase inhibition, the furo[2,3-c]carbazoles chloro substituted <strong>5c</strong> and nitro substituted <strong>5f</strong> were found to be more potent than acarbose with the values of 215.0 and 162.70 μM, respectively. On the other hand, the compound <strong>5f</strong> was found to be only promising candidate for α-amylase enzyme but not as effective as the standard acarbose.</p></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142229239","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
An efficient piperazine-based tertiary poly(amic acid) heterogeneous catalyst to prepare pyrrolidinone scaffolds 制备吡咯烷酮支架的高效哌嗪基三级聚（胺酸）异相催化剂
IF 1.8 3区 化学
Synthetic Communications Pub Date : 2024-09-05 DOI: 10.1080/00397911.2024.2400561
{"title":"An efficient piperazine-based tertiary poly(amic acid) heterogeneous catalyst to prepare pyrrolidinone scaffolds","authors":"","doi":"10.1080/00397911.2024.2400561","DOIUrl":"10.1080/00397911.2024.2400561","url":null,"abstract":"<div><p>Given the abundance of functional groups, meso- and macro-pores, and a high surface area, the piperazine-based poly(amic acid) was employed as a heterogeneous catalyst in the multicomponent reaction to prepare pyrrolidinone scaffolds in a green solvent, acting as a medium for mass transfer and crystallization solvent. The important parameters of the reaction were investigated to find the optimal reaction conditions. A conversion of 100% was obtained at reflux conditions within 30–100 min using a catalytic amount of 200 mg of piperazine-based poly(amic acid) per 2 mmol of reactants (100 mg of cat./1 mmol of reactant). The piperazine-based poly(amic acid) exhibited high recyclability and the recovered catalyst could be used in successive runs without worthy loss in its activity. This work revealed the catalytic activity of the piperazine-based poly(amic acid) as a promising functional polymeric heterogeneous catalyst for organic synthesis.</p></div>","PeriodicalId":22119,"journal":{"name":"Synthetic Communications","volume":null,"pages":null},"PeriodicalIF":1.8,"publicationDate":"2024-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142216109","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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