EOCS-MCP 2008研讨会组织

Longbing Cao, Ruwei Dai, V. Gorodetski
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引用次数: 1

摘要

一种制备由式(I) (I)表示的2-硫代2-取代烷酸衍生物的方法,其中A、R、R3和R4如下所定义,其包括缩合式(V) A- cho (V)的醛类化合物,其中A如下所定义,与式CHX3的卤化物(其中X如下所定义)和式(IV) R3SH (IV)的硫醇化合物(其中R3如下所定义),在存在基地生产2 - (arylthio或alkylthio) 2-substituted-acetic酸的公式(3)(3)中定义以下和R3,和反应生成2 - (arylthio或alkylthio) 2-substituted-acetic酸烷化剂的公式(3)由公式(2)RZ (II)在R和Z是以下的定义,存在至少2摩尔基地每摩尔的2 - (arylthio或alkylthio) 2-substituted-acetic酸,形成式(I)的化合物,其中R4表示氢原子,并且任选地通过酯化将所得化合物转化为式(I)的化合物,其中R4表示烷基。
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EOCS-MCP 2008 Workshop Organization
A process for preparing a 2-thio-2-substituted-alkanoic acid derivative represented by the formula (I) (I) wherein A, R, R3 and R4 are as defined hereinafter, which comprises condensing an aldehyde compound of the formula (V) A-CHO (V) wherein A is as defined hereinafter, with a haloform of the formula CHX3 wherein X is as defined hereinafter and a mercaptan compound of the formula (IV) R3SH (IV) wherein R3 is as defined hereinafter, in the presence of a base to produce a 2-(arylthio or alkylthio)-2-substituted-acetic acid of the formula (III) (III) wherein A and R3 are as defined hereinafter, and reacting the resulting 2-(arylthio or alkylthio)-2-substituted-acetic acid of the formula (III) with an alkylating agent represented by the formula (II) RZ (II) wherein R and Z are as defined hereinafter, in the presence of at least 2 mols of a base per mol of the 2-(arylthio or alkylthio)-2-substituted-acetic acid, to form the compound of the formula (I) wherein R4 represents a hydrogen atom and, optionally, converting the resulting compound to the compound of the formula (I) wherein R4 represents an alkyl group by esterification.
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