A Convenient Two-Step One-Pot Synthesis of Alkylthiophosphoramidates Derivatives

N-thiophosphonylamino groups have been greatly overlooked as potentially potent, transition-state analogues, or tetrahedral--intermediate inhibitors of metalloproteases. Alkylthiophosphoramidates derivatives were synthesized y reaction of O-isopropyl phosphorodichloridothioate with an amino acid este followed by hydrolysis in 2M NH 4 OH. The reaction was monitored by 31 P NMR spectroscopy.     

3-甲基犬尿喹啉酸衍生物的合成

报道了六个具有潜在生物活性 3 甲基犬尿喹啉酸衍生物的合成 .它们以取代苯胺和 3 甲基 2 酮丁二酸二乙酯为起始原料 ,经加成脱水 ,环化而得到 .其中三个新的含氟化合物的结构分别经IR ,1 HNMR ,MS ,元素分析等表征     

Facile and One-Pot Synthesis of 2 H -Chromene Derivatives Mediated by Vinyl triphenylphosphonium Salt

An efficient process that converts 2-hydroxybenzaldehyde and their derivetives to chromene derivatives via intramolecular Wittig reaction is described.     

An Efficient One-Pot Synthesis of Hippuric Acid Ethyl Ester Derivatives

A rapid, one-pot procedure is described for the preparation of the ethyl esters of a number of ring-substituted N-benzoyl glycine (hippuric acid) derivatives from readily-available starting materials.     

微波辅助酸催化水相一锅高效合成吖啶酸

本文建立一种以去离子水为溶剂,在微波辅助酸催化下一锅串联高效合成吖啶酸的新方法,该反应条件温和、操作简单、绿色高效。在优化反应条件下考察了多种取代基团对反应的影响,结果显示该方法具有良好的适应性,以83%～97%收率得到18个吖啶酸化合物。所有化合物结构均经过¹H NMR、¹³C NMR、HRMS、熔点等表征确认。     

One-Pot Synthesis of 3-Benzylflavones

The synthesis of 3-benzylflavone derivatives was efficiently performed in a one-pot method using substituted 2-hydroxy-acetophenone and appropriate benzaldehydes in the presence of pyrrolidine and ethanol. The distinct features of this methodology include simple procedure, easy purification, and good yields.     

One-Pot Preparation of 3,5-Hexadienoic Acid Compounds from Phenylacetaldehyde Derivatives

The synthesis of 6-aryl-4-methoxycarbonyl-3-methyl-3,5-hexadienoic acids by condensation of dimethyl-3-methyl glutaconate and phenylacetaldehyde derivatives in a stereoselective process is described.     

One-Pot Synthesis of 2-Alkylsulfanyldihydrofuran Derivatives from Tetracyanocyclopropyl Ketones

Russian Journal of Organic Chemistry - Successive treatment of 3-acylcyclopropane-1,1,2,2-tetracarbonitriles with sodium hydrogen carbonate and alkylmercaptan in water environment results in the...     

Synthesis of 3-Carboxycoumarins from O-Methoxybenzylidene Meldrum's Acid Derivatives

Reaction of o-methoxybenzaldehydes with Meldrum's acid followed by cyclization in sulfuric acid of the benzylidene derivatives 3a-g affords 3-carboxycoumarins in excellent yields.     

Application of Heteropolyacids as Heterogeneous and Recyclable Catalysts for One-Pot Synthesis of 3-Cyanopyridine Derivatives

A simple, clean and environmentally benign route to the synthesis of 3-cyanopyridines is described via a one-pot multi-component reaction of 3,4-dimethoxyacetophenone, malonitrile or ethylcyanoacetate, aldehyde and ammonium acetate using heteropolyacids as heterogeneous and recyclable catalysts in very good yields.     

聚乙二醇衍生物的合成研究进展

功能化聚醚尤其是功能化聚乙二醇衍生物,如聚乙二醇对甲苯磺酸酯、胺基聚乙二醇、羧基聚乙二醇、聚乙二醇－聚酯及聚乙二醇－聚氨基酸共聚物等在有机合成、多肽合成,高分子合成、药物的缓释控释、靶向施药等多方面具有广泛的应用前景,目前它已成为国内外研究的热点,本文综述了近年来聚乙二醇衍生物的合成研究进展。     

四甲基吡嗪衍生物合成及其5-HT3受体拮抗活性的筛选

恶性肿瘤常用的内科治疗方法为放射治疗和化学治疗,这两种治疗方法均会造成严重的恶心和呕吐等胃肠道副反应．早期的抗呕吐药物不仅其止吐效果差,还伴有严重的锥体外系副反应．自从20世纪70年代末发现5-HT3受体与呕吐机制有关以来引,5-HT3受体及其拮抗剂的研究极为活跃,目前上市的药物有Ondansetron,Granisetron,Tropisetron和Azasertron等,还有许多药物正处于临床研究阶段。     

Synthesis and Spectroscopic Properties of Mixed Aryloxide-Glycolate Derivatives of Arsenic(III)

The reaction in 1:1 molar ratio of {gg4}OGOAsCl , where G = CH 2 CH 2 , CHMeCHMe, CMe 2 CMe 2 , CHMeCH 2 CMe 2 , and CMe 2 CH 2 CH 2 CMe 2 , and substituted phenols ArOH (Ar = C 6 H 3 Me 2 -2,6; C 6 H 3 Pr i -5-Me-2; C 6 H 3 Pr i -2-Me-5 and C 6 H 3 Pr i 2 -2,6), in the presence of one equivalent of triethylamine in benzene afford volatile colorless liquids of the type {gg4}OGOAsOAr . All these derivatives have been characterized by elemental analyses, molecular weight measurements, and spectroscopic [IR, NMR( 1 H and 13 C)] studies.     

新型2,4-二取代四氢吡咯-3-羧酸衍生物的合成

N-三甲硅甲基苯甲醛亚胺为非稳定型亚甲胺基叶立德前体,在磷酸催化下与取代噁唑烷酮烯烃经1,3-偶极环加成反应合成了10个具有cis-trans立体结构的新型2,3,4-三取代四氢吡咯-3-羧酸衍生物（3a~3j）,收率65%~75%,其结构经¹H NMR, ¹³C NMR和HR-MS表征。3b的立体结构经X-单晶衍射确证。     

Choline Chloride/Urea Ionic Liquid Catalyzed a Convenient One-Pot Synthesis of Indole-3-propanamide Derivatives

A sequential three-component reaction of aromatic aldehydes with Meldrum's acid and N-methyl indole in the presence of choline chloride/urea ionic liquid as green catalyst has been described. In this one-pot multicomponent reaction, a series of indole-3-propanamide derivatives were synthesized with good to excellent yields. This methodology shows several advantages including fast reaction, easy isolation, operational simplicity that make it a useful and attractive option for the library generation of indole-3-propanamides (5a–l) for drug discovery.

[Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resources: Full experimental and spectral details.]     

Eco-Friendly One-Pot Synthesis of 2,4-Disubstituted Thiazoles by Grinding Under Catalyst- and Solvent-Free Conditions

Abstract

An efficient and facile synthesis of 2,4-disubstituted thiazoles is achieved by a one-pot reaction of aldehydes and α-bromoketones with thiosemicarbazide by grinding under catalyst- and solvent-free conditions. This method has notable advantages in terms of simple workup, neat conditions, high yield, reasonably rapid reaction rate, and environmental friendliness.

Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.

GRAPHICAL ABSTRACT     

(E)-6-氯-2-芳乙烯基-3-喹啉甲酸衍生物的合成

以6-氯-2-氯甲基-3-喹啉甲酸乙酯(1)与芳香醛类化合物3a-f′为起始化合物,通过简便有效的“一锅法”反应,合成了(E)-6-氯-2-芳乙烯基-3-喹啉甲酸衍生物4a-f′。所合成的32个化合物4a-f′均未见文献报道,其结构经红外光谱、核磁共振氢谱、核磁共振碳谱和高分辨质谱得以确认。     

氨基-3-氰基丙酸衍生物的合成

以廉价易得的2,5-二溴吡啶为原料,经取代、氧化、R-(+)-叔丁基亚磺酰胺手性诱导、氨基化、氨基酸缩合等反应,合成了氨基-3-氰基丙酸衍生物,其结构经¹H-NMR, ¹³C-NMR和LC-MS确证。同时对吡啶环5位取代反应机理进行探讨,并且采用ELISA法研究了氨基-3-氰基丙酸衍生物对炎症细胞（BMDM）Caspase-1活性的影响。结果表明：经11步合成的氨基-3-氰基丙酸衍生物结构新颖,并且对Caspase-1的抑制活性具有剂量依赖性。      

2-巯基苯并噻唑衍生物的合成进展

2-巯基苯并噻唑具有很好的经济价值.为了增强和完善2-巯基苯并噻唑的应用性能,通过将其作为一种中间体,与油溶性基团的活性元素结合在同一分子内,开发和研究了其一系列新型的具有良好性能的衍生物,可用作配体、染料、硫化促进剂、蛋白质酶抑制剂以及杀菌、除草和抗病毒药物.对通过包括苯环、巯基上的S、杂环上的N等3个位置上的取代或加成来合成这些衍生物的简单可行方法进行了综述.