PHENETHYLAMINES VIA HECK ARYLATION OF A NEW VINYLAMINE EQUIVALENT

被引：25

作者：

BUSACCA, CA

JOHNSON, RE

SWESTOCK, J

机构：

[1] Department of Medicinal Chemistry, Sterling Winthrop Pharmaceuticals Research Division, Rensselaer

来源：

JOURNAL OF ORGANIC CHEMISTRY | 1993年 / 58卷 / 12期

关键词：

D O I：

10.1021/jo00064a015

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new vinylamine equivalent, N-vinyloxazolone 3, has been prepared in three steps and shown to undergo Heck arylation with a variety of substrates. The Heck adducts thus obtained are then converted in one step and high yield to phenethylamine hydrochlorides. As a general synthetic method for preparation of substituted phenethylamines, use of this new reagent is shown to be superior to N-vinylphthalimide in number of steps, regiospecificity, and chemical yield.

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页码：3299 / 3303

页数：5

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