A reliable and efficient synthesis of SR 142801

GAM Giardina, M Grugni, R Rigolio, M Vassallo…

文献索引：Giardina; Grugni, Mario; Rigolio, Roberto; Vassallo, Marco; Erhard, Karl; Farina, Carlo Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 19 p. 2307 - 2310

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被引用次数: 12

摘要

A convenient synthesis of the potent human NK-3 receptor antagonist SR 142801,(S)-(+)-N- {{3-[1-benzoyl-3-(3, 4-dichlorophenyl) piperidin-3-yl] prop-1-yl}-4-phenylpiperidin-4-yl}-N- methylacetamide [(S)-(+)-(15)], is described. Improvements over the previously reported procedure are the preparation of the intermediate 5via the novel imide 3 and subsequent reaction with the nucleophile 14, which reacts, regioselectively, at the endocyclic nitrogen.

63843-83-4

1-苄基-4-苯基哌啶-4-醇

~79%

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~70%

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~79%

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~63%

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~55%

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Structure-guided design and synthesis of position 1-phenylcy...

[Tagad, Harichandra D.; Hamada, Yoshio; Nguyen, Jeffrey-Tri; Hidaka, Koushi; Hamada, Takashi; Sohma, Youhei; Kimura, Tooru; Kiso, Yoshiaki Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 17 p. 5238 - 5246]