Synthetic Communications

General Route for the Preparation of Diverse 17-Membered Macrocycles Based on RCM and Examination of the E/Z Selectivity

TJ Heckrodt, R Singh

文献索引：Heckrodt, Thilo J.; Singh, Rajinder Synthetic Communications, 2012 , vol. 42, # 19 p. 2854 - 2865

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被引用次数: 5

摘要

A convergent, general synthetic route to 17-membered macrocycles was developed to support biological evaluation and structure–activity relationship (SAR) studies during phenotypic screening for immunology targets. A series of amide coupling reactions led to a ring-closing metathesis (RCM) precursor that was cyclized using Grubbs' catalysts. It was found that the reaction formed the macrocyclic products in a 3:1 ratio of E/Z isomers. Moreover, it was shown that a ...