通过 2,2-二氟-1-碘-1-硅基乙烯的 Suzuki-Miyaura 交叉偶联反应高效合成硅基化 2,2-二氟苯乙烯衍生物。

Efficient synthesis of silylated 2,2-difluorostyrene derivatives through Suzuki-Miyaura cross-coupling of 2,2-difluoro-1-iodo-1-silylethenes.

机构信息

Canada Research Chair in Organic and Medicinal Chemistry, Department of Chemistry, 1045 avenue de la Médecine, Université Laval, Québec, Canada.

出版信息

Org Biomol Chem. 2013 Feb 28;11(8):1367-75. doi: 10.1039/c2ob27221k.

DOI:10.1039/c2ob27221k

PMID:23321719

Abstract

We report a new synthetic sequence for the preparation of silylated 2,2-difluorostyrene derivatives. This new route has numerous advantages over the previous one including enhanced scope, higher yields, ease of purification, and significant reduction of the amount of desilylated side-products. An unexpected transformation of a silylated 2,2-difluorostyrene derivative is also presented.

摘要

我们报告了一种新的合成序列，用于制备硅基化 2,2-二氟苯乙烯衍生物。与之前的方法相比，这条新路线具有许多优势，包括扩大了反应范围、提高了产率、简化了纯化过程，并且显著减少了脱硅副产物的量。我们还提出了一种硅基化 2,2-二氟苯乙烯衍生物的意外转化。