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麝香吡啶及其类似物的合成
引用本文:王存英,张德勇,黄龙珍. 麝香吡啶及其类似物的合成[J]. 药学学报, 1991, 26(5): 379-382
作者姓名:王存英  张德勇  黄龙珍
作者单位:中国医学科学院药物研究所,中国医学科学院药物研究所,中国医学科学院药物研究所 北京 100050,北京 100050,北京 100050
摘    要:麝香吡啶(muscopyridine Ⅰ)是从天然麝香中分离出的一种香味成分,因其含量极低,合成方法又较复杂,有关药理作用的研究还未见报道。为观察其药理作用,我们合成了消旋麝香吡啶及其类似物Ⅱ,Ⅲ和Ⅳ。

关 键 词:麝香吡啶  交叉偶合  双格氏试剂  环合
收稿时间:1990-01-19

SYNTHESIS OF MUSCOPYRIDINE AND ITS ANALOGS
CY Wang,DY Zhang and LZ Huang. SYNTHESIS OF MUSCOPYRIDINE AND ITS ANALOGS[J]. Acta pharmaceutica Sinica, 1991, 26(5): 379-382
Authors:CY Wang  DY Zhang  LZ Huang
Affiliation:Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing.
Abstract:Muscopyridine (1) is one of the odoriferous constituents of natural musk. 1 was prepared previously in very low yield in multisteps. We report here one-step preparation of muscopyridine and its analogs by the cross-coupling method. The cyclocoupling is effected by slow dropwise addition of a THF solution of di-Grignard reagent under nitrogen to a well stirred mixture of an equimolar quantity of a dichloropyridine in THF containing a catalytic amount of Ni (dppp)Cl2. The reaction mixture is stirred at 35-40 degrees C for up to 20 h. Analogs 2, 3 and 4 have also been prepared by this method. The structure of these products and intermediates are determined by UV, IR, MS, and 1HNMR spectral data.
Keywords:Cross—coupling  di-Grignard reagent  Cyclization  Muscopyridine
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