C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 271/28 (2006.01) C07C 269/06 (2006.01) C07D 277/34 (2006.01) C07D 417/12 (2006.01) A61K 31/427 (2006.01) A61P 3/10 (2006.01)
Patent
CA 2377233
This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, (see formulas III, II, IV and I) wherein R1 is C1-C6 alkyl, C1-C6 alkoxyl, etc., R2 is C1-C6 alkyl, and R3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.
L'invention concerne des intermédiaires pour la synthèse de composés de benzimidazole présentant une excellente activité antihyperglycémique ou leurs sels et un procédé de préparation de ceux-ci. Le procédé de préparation de composés de benzimidazole (I) est caractérisé par la condensation d'un dérivé d'amine (III) avec un dérivé d'acide carboxylique (II) pour former un composé (IV) et soumettre ce composé (IV) à la fermeture du cycle en présence d'un acide (dans laquelle R<1> représente alkyle C1-C6, alcoxy C1-C6 ou similaires; R<2> représente alkyle C1-C6; et R<3> représente hydrogène ou un groupe protecteur).
Abe Narumi
Kishi Naoyuki
Nakamura Yoshitaka
Takebayashi Toyonori
Daiichi Sankyo Company Limited
Marks & Clerk
Sankyo Company Limited
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