A concise synthesis of a novel insulin-like growth factor I receptor (IGF-IR) inhibitor

被引：30

作者：

Slade, Joel ^{[1
]}

Bajwa, Joginder ^{[1
]}

Liu, Hui ^{[1
]}

Parker, David ^{[1
]}

Vivelo, James ^{[1
]}

Chen, Guang-Pei ^{[1
]}

Calienni, John ^{[1
]}

Villhauer, Edwin ^{[1
]}

Prasad, Kapa ^{[1
]}

Repic, Oljan ^{[1
]}

Blacklock, Thomas J. ^{[1
]}

机构：

[1] Novartis Pharmaceut, Proc Res & Dev, E Hanover, NJ 07936 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2007年 / 11卷 / 05期

关键词：

D O I：

10.1021/op700052u

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

An efficient synthesis of a potent insulin-like growth factor I receptor (IGF-IR) hihibitor AEW541 (1) is described. The key step in the synthesis is the cis-selective reductive amination of cyclobutanone, which sets up the desired 1,3-stereochemistry of the cyclobutane ring. The amino group thus generated is used as a handle to build the pyrrolopyrimidine ring. The final step resulting in 1 is accomplished by alkylation of in situ generated mesylate with azetidine.

引用

页码：825 / 835

页数：11

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