Tetrahedron

An efficient and convergent synthesis of the potent and selective H 3 antagonist ABT-239

…, YM Pu, T Grieme, P Sharma, AV Bhatia, M Cowart

文献索引：Ku, Yi-Yin; Pu, Yu-Ming; Grieme, Tim; Sharma, Padam; Bhatia, Ashok V.; Cowart, Marlon Tetrahedron, 2006 , vol. 62, # 18 p. 4584 - 4589

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被引用次数: 17

摘要

An efficient and convergent process for the preparation of a potent and selective H3 receptor antagonist, ABT-239, was accomplished with an overall yield of 64%. The key step in the synthesis is a Sonogashira coupling/cyclization reaction of 1-but-3-ynyl-2-(R)- methylpyrrolidine () with 4′-hydroxy-3′-iodo-biphenyl-4-carbonitrile (). Additionally, the key amine component 2-(R)-methylpyrrolidine () was effectively synthesized from the ...