Development of large-scale preparations of indole derivatives: Evaluation of potential thermal hazards and studies of reaction kinetics and mechanisms

被引：10

作者：

Akao, Atsushi

Nonoyama, Nobuaki

Mase, Toshiaki

Yasuda, Nobuyoshi

机构：

[1] Merck Res Labs, Preclin Dev, Proc Res, Tsukuba, Ibaraki 3002611, Japan

[2] Merck Res Labs, Dept Proc Res, Rahway, NJ 07065 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2006年 / 10卷 / 06期

关键词：

D O I：

10.1021/op060150f

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Hydrogenation of (E)-2-nitropyrrolidinostyrene in the presence of the doped rhodium catalyst is safe, scalable, and highly effective for the preparation of 6-benzyloxyindole. Reaction kinetics with/without additives also were examined using in situ IR for the first time. Results showed that the additives decelerate the hydrogenolysis of benzyl ethers, while simultaneously accelerating the de-oxygenation of N-oxy-intermediates.

引用

页码：1178 / 1183

页数：6

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