A General One-Pot Protocol for Hindered N-Alkyl Azaheterocycles from Tertiary Carboxylic Acids

被引:12
作者
Merchant, Rohan R. [1 ]
Lang, Simon B. [1 ]
Yu, Tingting [2 ]
Zhao, Shuilian [2 ]
Qi, Zhiqi [2 ]
Suzuki, Takao [2 ]
Bao, Jianming [1 ]
机构
[1] Merck & Co Inc, Dept Discovery Chem, San Francisco, CA 94080 USA
[2] WuXi AppTec Co Ltd, IDSU, Shanghai 200131, Peoples R China
关键词
DISCOVERY; PYRAZOLE; INHIBITORS;
D O I
10.1021/acs.orglett.0c01254
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
In this letter, we report a general one-pot strategy that utilizes three elementary steps (decarboxylative hydrazination, Boc deprotection, and heterocycle condensation) to regioselectively prepare hindered C(sp(3)) substituted pyrazoles and triazoles. The operational simplicity of this sequence and ubiquity of tertiary carboxylic acids allow rapid access to hindered N-alkyl azaheterocycles that will be useful to practitioners of medicinal chemistry and agro-chemistry.
引用
收藏
页码:4180 / 4184
页数:5
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