A palladium-catalysed urea arylation route to a CRF1 receptor antagonist

被引：5
作者：
Popkin, Matthew E. [1 ]
Bellingham, Richard K. [1 ]
Hayes, Jerome F. [1 ]
机构：
[1] GlaxoSmithKline Inc, Chem Dev, Tonbridge TN11 9AN, Kent, England
来源：
SYNLETT | 2006年 / 17期
关键词：
CRF antagonist; palladium; catalysis; ligands; urea; arylations;
D O I：
10.1055/s-2006-950276
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A new synthetic approach to a potent CRF antagonist, GW808990 (NB135583), is reported. The route hinges on the palladium-catalysed intramolecular arylation of a urea with 2-chloropyridine. Spontaneous piperazine ring closure means that a high-yielding bisarmulation reaction is the final step.
引用
收藏
页码：2716 / 2718
页数：3
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