54596-01-9Relevant articles and documents
Efficient synthesis of a highly selective NPY-5 receptor antagonist: A drug candidate for the treatment of obesity
Itoh, Takahiro,Kato, Shinji,Nonoyama, Nobuaki,Wada, Toshihiro,Maeda, Kenji,Mase, Toshiaki,Zhao, Matthew M.,Song, Jake Z.,Tschaen, David M.,McNamara, James M.
, p. 822 - 828 (2012/12/22)
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-BuMgCl and n-BuLi. This protocol also dramatically increased the thermal stability of the aryllithium intermediate and eliminated the requirement for costly cryogenic conditions. The union of the spirolactone piperidine 2 and aminopyrazine 3 via a carbonyl group was accomplished using phenyl chloroformate delivering the target molecule in high yield.
Process for making spiro isobenzofuranone compounds
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, (2008/06/13)
This invention relates to a process for making spiro isobenzofuranone compounds by coupling of an aminopyrazine fragment with a spirolactone piece.
