摘要 |
<p>Preparation of 1-amino-4-(hydroxymethyl)-2-cyclopentene (I), in the form of its racemate or optically active isomer, comprises hydrolysis of a cyclopentene derivative (III), in the form of its racemate or optically active isomers, with an alkali metal hydroxide. Preparation of 1-amino-4-(hydroxymethyl)-2-cyclopentene of formula (I), in the form of its racemate or optically active isomer, comprises hydrolysis of a cyclopentene derivative of formula (III), in the form of its racemate or optically active isomers, with an alkali metal hydroxide. R : 1-4C alkyl, 1-4C alkoxy, aryl or aryloxy. An independent claim is also included for the preparation of (1S,4R)-4-(2-amino-6-chloro-9H-purine-9-yl)-2-cyclopenten-1-methanol or its salt comprising reacting (-)-2-azabicyclo[2.2.1]hept-5-en-3-one or (-)-acyl-2-azabicyclo[2.2.1]hept-5-en-3-one compound of formula (IV) and a metal hydride to give (I) or (III); reducing and reacting the obtained product with hydrohalogenized salt and then with N-(2-amino-4,6-dichloropyrimidine)-5-yl)formamide to give (1S,4R)-4-[(2-amino-6-chlor-5-formamido-4-pyrimidinyl)-amino]-2-cyclopenten-1-methanol; and cyclizing (1S,4R)-4-[(2-amino-6-chlor-5-formamido-4-pyrimidinyl)-amino]-2-cyclopenten-1-methanol. [Image] [Image].</p> |
申请人 |
LONZA AG |
发明人 |
BERCHTOLD, KATJA;RODUIT, JEAN-PAUL;BERNEGGER-EGLI, CHRISTINE, DR.;URBAN, EVA MARIA;PETERSEN, MICHAEL, DR. |