Synthesis of 1,3,5-trisubstituted-1,2,4-triazoles by microwave-assisted N-acylation of amide derivatives and the consecutive reaction with hydrazine hydrochlorides
作者:Jongbok Lee、Myengchan Hong、Yoonchul Jung、Eun Jin Cho、Hakjune Rhee
DOI:10.1016/j.tet.2012.01.003
日期:2012.2
Facile and efficient procedures for the N-acylation reaction of amide derivatives with various acid anhydrides and the cyclization reaction of N-acylated amide derivatives with various hydrazinehydrochlorides were described. The reactions were carried out under microwave irradiation to give products in good yields in a few minutes. The synthesis of 1,3,5-trisubstituted-1,2,4-triazoles from benzamides
Malonicacid derivatives have been successfully applied in a Ag-catalyzed decarboxylative fluorination reaction, providing an unprecedented route to either gem-difluoroalkanes or α-fluorocarboxylic acids by the judicious selection of base and solvent. This reaction features the use of readily available starting materials, tunable chemoselectivity and good functional group compatibility as well as gram-scale
A process for preparing 4-haloazetidinones of the formu-
which comprises reacting in an inert solvent at a temperature between about -20°C. and about 45°C. a 4-sulfino- azetidinone of the formula
with at least one molar equivalent of a positive halogen reagent, where in the above formulas M is hydrogen, sodium or potassium, X is chloro, bromo, or iodo; R is a carboxy-protecting group; and R, is an acylamido or diacylamido group useful as intermediates for the preparation of β-lactam antibiotics.
一种制备式-4-卤代氮杂环丁酮的工艺
式的 4-氨基磺氮杂环丁酮与至少一种摩尔当量的正卤素试剂反应。
式中 M 为氢、钠或钾,X 为氯、溴或碘;R 为羧基保护基团;R 为酰氨基或二酰基氨基,可用作制备 β-内酰胺类抗生素的中间体。
Heterocyclic compounds having anti-diabetic activity, their preparation and their use
申请人:SANKYO COMPANY LIMITED
公开号:EP0676398A2
公开(公告)日:1995-10-11
Compounds of formula (I) :
[wherein: X represents an unsubstituted or substituted indolyl, indolinyl, azaindolyl, azaindolinyl, imidazopyridyl or imidazopyrimidinyl group ; Y represents an oxygen or sulphur atom ; Z represents a 2,4-dioxothiazolidin-5-ylidenylmethyl, 2,4-dioxothiazolidin-5-ylmethyl, 2,4-dioxooxazolidin-5-ylmethyl, 3,5-dioxooxadiazolidin-2-ylmethyl or N-hydroxyureidomethyl group ; R represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, a hydroxy group, a nitro group, an aralkyl group or a unsubstituted or substituted amino group ; and m is an integer of from 1 to 5] have hypoglycemic and anti-diabetic activities.
式(I)化合物:
其中X 代表未取代或取代的吲哚基、吲哚啉基、氮杂吲哚啉基、咪唑吡啶基或咪唑嘧啶基; Y 代表氧原子或硫原子;Z 代表 2,4-二氧代噻唑啉-5-亚甲基、2,4-二氧代噻唑啉-5-基甲基、2,4-二氧代恶唑啉-5-基甲基、3,5-二氧代恶唑啉-2-基甲基或 N-羟基脲基甲基;R 代表氢原子、烷基、烷氧基、卤素原子、羟基、硝基、芳烷基或未取代或取代的氨基;以及 m 是 1 至 5 的整数]具有降血糖和抗糖尿病活性。
n-Butylammonium carboxylates/Tf2O: ionic liquid based systems for the synthesis of unsymmetrical imides via a Ritter-type reaction
作者:Mohammad Mehdi Khodaei、Ehsan Nazari
DOI:10.1016/j.tetlet.2012.03.121
日期:2012.6
We have developed a new method for the preparation of unsymmetrical imides using liquid carboxylate salts via a Ritter-type process. The reactions were carried out with nitriles and n-butylammonium carboxylates as ionic liquids in the presence of triflic anhydride (Tf2O) as the promoter. Mild reaction conditions, simplicity of the procedure, and proton-free conditions are the main advantages of this procedure. (C) 2012 Elsevier Ltd. All rights reserved.