“一锅串联法”合成2-[(E)-2-2-氯-1-甲基-3-吲哚基)乙烯基]喹啉-3-羧酸(英文)

设计了以2-(溴甲基)喹啉-3-甲酸乙酯(4)与2-氯-1-甲基-3-吲哚醛(5)为起始化合物,通过简便有效的"一锅法"反应,首次将吲哚环引入2-苯乙烯基喹啉骨架模型,从而得到一新颖结构的双杂环化合物,即(E)-2-(2-(2-氯-1-甲基-1H-3-吲哚基)乙烯基)喹啉-3-羧酸(3),其结构通过波谱数据和元素分析得以证实。     

"一锅法"合成N-链烯基-(2R,3R)-O,O-二乙酰酒石酰亚胺

本文报导一种由(2R,3R)-二乙酰酒石酸酐合成N-ω-链烯基二乙酰酒石酰亚胺的简单有效的"一锅合成法", 并使总产率有大幅度的提高。     

One-pot Synthesis of 3-Aryl-1,5-bis（2-hydroxyaryl）pentane-1,5-diones

A simple method for the synthesis of 3-aryl-1,5-bis(2-hydroxyaryl)pentane-1,5-diones is developed by one-potreaction involving 2-hydroxyacetophenone and arylaldehyde in aqueous potassium hydroxide.     

温和条件下丁二酰亚胺-N-磺酸催化合成双吲哚甲烷和香豆素衍生物(英文)

A mild and simple procedure is described for the synthesis of bis(indolyl)methane and coumarin derivatives using succinimide-N-sulfonic acid as an efficient,cheap,and reusable catalyst under mild conditions.     

邻甲基苯磺酸铜催化"一锅法"合成3,4-二氢嘧啶-2(1H)-酮

二氢嘧啶酮(DHPMs)及其衍生物具有广泛的生物活性,如抗病毒、抗肿瘤、抗癌、抗高血压及消炎等作用[1].此外,DHPMs及其衍生物作为钙通道阻滞剂、α1a-对抗剂和神经肽Y的对抗剂,显示出良好的药理活性[2].更重要的是,最近几种含二氢嘧啶酮-5-羧酸盐的海洋生物碱被成功分离出来,并表现出重要的生物学性质[3],某些可以阻止HIVgp-120-CD4键的形成,是一种潜在的HIV抑制剂[4].因此,对DHPMs及其衍生物的研究成为生物活性有机杂环化合物的研究热点之一.     

对甲基苯磺酸亚铈催化一锅法合成取代2,3-二氢-4(1H)-喹唑啉酮

以对甲基苯磺酸亚铈为催化剂,靛红酸酐、醛和铵盐或伯胺为原料,在乙醇水溶液中三组分一锅法合成了一系列单取代和双取代2,3-二氢-4(1H)-喹唑啉酮衍生物。考察了溶剂条件及催化剂用量对产率的影响。经催化剂循环研究,催化活性无明显变化。产物的结构通过熔点、IR、1H NMR、13C NMR、质谱和元素分析进行测定和结构表征。     

One-pot,four-component synthesis of benzylpyrazolyl naphthoquinone derivatives and molecular docking studies

A highly efficient, green, one-pot, four-component approach for the synthesis of benzylpyrazolyl naphthoquinone derivatives (5a–p) have been developed by the domino reaction of 2-hydroxy naphthoquinone, aromatic aldehyde, ethyl acetoacetate, and phenyl hydrazine derivatives in water and employed p-toluene sulfonic acid (p-TSA) as the right choice of catalyst at reflux. Docking simulation was performed to position compounds 5a, 5b, and 5g into the anaplastic lymphoma kinase (ALK) structure active site to determine the probable binding model.     

One-pot synthesis of novel ether-linked diisoxazole derivatives via sequential O-propargylation and 1,3-dipolar cycloaddition from 2-bromohomoallylic alcohols

Abstract

A simple and efficient, one-pot approach for the synthesis of ether-linked diisoxazole derivatives has been developed through sequential reactions, which includes O-propargylation of 2-bromohomoallylic alcohols with propargyl bromide in the presence of sodium hydride in THF, and 1,3-dipolar cycloaddition by the addition of hydroximinoyl chlorides and triethylamine. This protocol provides some advantages such as high regioselectivity, easy operation and good product yields with a wide scope of substrates under mild conditions.     

One-pot three-component synthesis of the spiroacenaphthylene derivatives

A facile and efficient one-pot three-component synthesis of the spiroacenaphthylene derivatives was achieved, via the reaction of acenaphthequinone, malononitrile/ethylcyanoacetate and various reagents including α-methylencarbonyl compounds/enols.     

3-乙基-2-丙基喹啉衍生物的合成工艺研究

以芳胺和正丁醛为原料,对甲基苯磺酸(TsOH)为促进剂,采用"一锅法"合成了3-乙基-2-丙基喹啉衍生物,系统地考察了原料比例、溶剂以及芳胺上取代基对反应的影响,比较了不同的质子酸促进剂对喹啉衍生物产率以及选择性的影响,并对产物进行了核磁共振表征.实验结果表明当用对甲基苯磺酸(TsOH)为促进剂时,3乙基-2-丙基喹啉收率可达到59%,同时生成40%N-丁基苯胺;磷钼酸、浓硫酸也可以选择性地得到喹啉衍生物,但收率较低,分别只有28%和24%.同时,考察了苯胺环上取代基对喹啉收率的影响,当苯环上有供电子基时,有利于喹啉的生成,而吸电子基则不利于喹啉的生成.并推测了反应机理.     

Biginelli reaction for synthesis of novel trifluoromethyl derivatives of bis(tetrahydropyrimidinone)benzenes

A facile one-pot three-component condensation of terephthalic aldehyde with urea and fluorinated 1,3-dicarbonyl derivatives is developed using catalytic quantities of chlorotrimethylsilane at ambient temperature. As a consequence, efficient synthesis of novel trifluoromethyl derivatives of bis(tetrahydropyrimidinone)benzenes is observed within short time periods. The procedure is shown to be equally efficient when urea is replaced with thiourea or guanidine.     

硅胶固载硫酸镧催化一锅法合成3,4-二氢嘧啶-2(1H)-酮

以硅胶固载硫酸镧作为催化剂,由芳香醛、β-酮酸酯和脲(硫脲)合成了相应的3,4-二氢嘧啶-2(1H)-酮化合物,考察了苯甲醛、乙酰乙酸乙酯、脲三组分发生Biginelli反应时的催化剂用量、反应物物质的量比、反应时间及催化剂重复使用对反应收率的影响;并利用核磁共振谱(1H NMR)和红外光谱(IR)表征了合成产物的结构...     

“一锅法”合成2-[(2,4-二叔丁基苯氧基)甲基]-6,7-二氧戊环并[1,3-g]喹啉-3-羧酸(英文)

采用一锅法的合成方式有效地合成了2-(2,4-二叔丁基苯氧基)甲基-6,7-二氧戊环并[1,3-g]喹啉-3-羧酸,其特点是将威廉姆逊反应和碱水解这两步反应在"一锅里"进行.所得化合物的结构经IR、1 HNMR、MS和元素分析得以证实.     

One-pot synthesis of asymmetric annulated bis(pyrrole)s

Condensation of activated functionalized pyrroles with acetone results in asymmetric bis(pyrrole)s, formed via ring annulation. The methodology is somewhat general and can be applied to a variety of ketones, as well as to a range of pyrrolic substrates that do not bear electron-withdrawing groups directly adjacent to the pyrrole ring.     

One-pot synthesis of 2-(dicyanomethylene)-1,2-dihydropyridine derivatives

The synthesis of 2-(dicyanomethylene)-1,2-dihydropyridine derivatives from the reactions of arylmethylidene derivatives of malononitrile dimers with 1,3-dicarbonyl compounds is described.     

Improved synthesis of bis[p-(phenylethynyl)phenyl]hetarylenes

Bis[p-(phenylethynyl)phenyl]hetarylenes were synthesized in high yields by an improved method using cross-coupling between phenylacetylene and 4,4′-dibromobenzil followed by condensation of the 4,4′-di(phenylethynyl)benzil obtained with eithero-phenylenediamine and 3,4-diaminobenzoic acid or with benzaldehyde andp-nitrobenzaldehyde in the presence of ammonium acetate. Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 10, pp. 1889–1890, October, 1997.     

以CO_2和环氧氯丙烷为底物一锅合成碳酸甘油酯

以环氧氯丙烷和CO2为底物,三乙胺作为溶剂和CO2活化试剂,一锅合成碳酸甘油酯.该方法反应条件温和,反应收率较高,所使用的底物环氧氯丙烷工业上可由甘油制得,因此该方法直接和间接地利用了CO2和甘油两个工业副产物,并为碳酸甘油酯的合成提供了一种高效实用的方法.     

K2CO3-catalyzed synthesis of 2-amino-3-cyano-4H-chromene derivatives with different substituents in water

The direct three-component condensation of resorcinol, 1-(2,4-dihydroxyphenyl)ethanone or 2,4-dihydroxybenzophenone with benzaldehydes and malononitrile to generate some novel 2-amino-3-cyano-4H-chromene derivatives has been carried out over K₂CO₃ (25 mol%) with high efficiency in water as a green solvent at 70 °C.     

One-pot catalytic asymmetric cascade synthesis of cycloheptane derivatives

A regiospecific, highly chemo-, diastereo-, and enantioselective one-pot catalytic cascade synthesis of cycloheptane derivatives is presented. In this chiral-amine-catalyzed asymmetric process, six new bonds and five new stereocenters were formed with excellent stereocontrol (>25:1 d.r. and 98- >99 ee).     

One-pot synthesis of 2-amino-3-cyanopyridine derivatives under solvent-free conditions

A series of 2-amino-3-cyanopyridines were obtained from aryl aldehydes, substituted acetophenones, malononitrile and ammonium acetate in good to excellent yields by proceeding through a simple, mild and efficient procedure utilizing N,N,N′,N′-tetrabromobenzene-1,3-disulfonamide [TBBDA] and poly(N-bromo-N-ethylbenzene-1,3-disulfonamide) [PBBS] as catalysts.