Method for manufacturing a purine derivative

摘要

(1S,4R)-4-(2-Amino-6-chloro-9-H-purin-9-yl)-2-cyclopentene-1-methanol or its salts (I) production involves reducing (-)-2-azabicyclo[2.2.1]hept-5-en-3-one or (-)-acyl-2-azabicyclo[2.2.1]hept-5-en-3-one of the formulae (II) or (III) with a metal hydride into an amino-alcohol of the formula (IV) or in a cyclopentene derivate of formula (V). The cyclopentene derivate is transformed into the corresponding hydrohalogenated salts. The hydrohalogenated salts are converted into (1S,4R)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentene-1-methanol of formula (VII) with N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide of formula (VI), and cyclized into the compound of the formula (I) in well known manner. The compound (1S,4R)-4-(2-amino-6-chloro-9-H-purin-9-yl)-2-cyclopentene-1-methanol or its salts having the general formula (I), is new. For formulae (III,V), R : 1-4C-alkyl, 1-4C-alkoxy, aryl or aryloxy. [Image] [Image] [Image] [Image] [Image] [Image] [Image].