Efficient synthesis of a highly selective NPY-5 receptor antagonist: A drug candidate for the treatment of obesity

…, N Nonoyama, T Wada, K Maeda, T Mase…

Index: Itoh, Takahiro; Kato, Shinji; Nonoyama, Nobuaki; Wada, Toshihiro; Maeda, Kenji; Mase, Toshiaki; Zhao, Matthew M.; Song, Jake Z.; Tschaen, David M.; McNamara, James M. Organic Process Research and Development, 2006 , vol. 10, # 4 p. 822 - 828

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Citation Number: 11

Abstract

A concise and practical synthesis of highly selective NPY-5 receptor antagonist 1 is described. The animopyrazine intermediate 3 was synthesized via either monobromination of aminopyrazine or palladium-catalyzed regioselective debromination of dibromopyrazine followed by an efficient Suzuki-Miyaura coupling. For the preparation of the spirolactone piperidine 2, significantly improved yield was achieved by using a combination of n- ...