用于合成稠合杂环的杂原子取代丙二烯的高区域选择性钯催化环化反应。

Highly regioselective palladium-catalyzed annulation reactions of heteroatom-substituted allenes for synthesis of condensed heterocycles.

作者信息

Inamoto Kiyofumi, Yamamoto Akio, Ohsawa Kazutoshi, Hiroya Kou, Sakamoto Takao

机构信息

Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.

出版信息

Chem Pharm Bull (Tokyo). 2005 Nov;53(11):1502-7. doi: 10.1248/cpb.53.1502.

DOI:10.1248/cpb.53.1502

PMID:16272743

Abstract

We have developed a highly regioselective synthesis of heterocycles via palladium-catalyzed annulation reaction of heteroatom-substituted allenes. Various aryl halides were reacted and one regioisomer was observed exclusively in all reactions. In addition, subsequent functionalizations of annulated products were carried out using alkyl metal reagents, and the introduction of alkyl moieties was accomplished.

摘要

我们通过钯催化的杂原子取代丙二烯环化反应，开发了一种高度区域选择性的杂环合成方法。使各种芳基卤化物发生反应，并且在所有反应中仅观察到一种区域异构体。此外，使用烷基金属试剂对环化产物进行后续官能化反应，实现了烷基部分的引入。