Process for the preparation of aminoalcohol and (1S,4Rú®or (1R,4S)-1-amino-4-(methylol)-2-cyclopentene or its salts

本发明涉及制备外消旋或旋光的化学式I的氨基醇的新方法，该方法包括用碱金属氢氧化物水解外消旋体或一种其旋光异构体形式的化学通式III的环戊烯衍生物。本发明还涉及制备化学式V或VI的(1S，4R)-或(1R，4S)-1-氨基-4-(羟甲基)-2-环戊烯或其盐的方法，该方法包括化学水解化学通式VII或VIII的(1S，4R)-或(1R，4S)-1-氨基-4-(羟甲基)-2-环戊烯衍生物。 Production of optionally (1S,4R)- or (1R,4S)-1-amino-4-(hydroxymethyl)-2-cyclopentene (VII) or (VIII) (or their salts) involves biotechnological optical resolution of racemic 1-amino-4-(hydroxymethyl)-2-cyclopentene (I) using a hydrolase in presence of an acylating agent. Production of (1S,4R)- or (1R,4S)-1-amino-4-(hydroxymethyl)-2-cyclopentene of formula (VII) or (VIII) (or their salts) involves biotechnological optical resolution of racemic 1-amino-4-(hydroxymethyl)-2-cyclopentene of formula (I) using a hydrolase (specifically a lipase) in presence of an acylating agent.X, Y=H or acyl. Independent claims are included for: (1) preparation of (VII; X, Y= H) or (VIII; X, Y= H) (or their salts) comprising chemical hydrolysis of corresponding compounds in which at least one of X and Y is other than H; and (2) production of (VII; Y= H; X= COR) or (VII; Y= H; X= COR) by (a) reducing 2-azabicyclo-(2.2.1)-hept-5-en-3-one (II) (in racemic or optical isomer form) to racemic (I); (b) carrying out biotechnological optical resolution (I) using a hydrolase in presence of an acylating agent to give (VII; X,Y= H) or (VII; X,Y= H); and (c) acylating to give (VII; Y= H; X= COR) or (VII; Y= H; X= COR). R : 1-4C alkyl, 1-4C alkoxy, aryl or aryloxy. [Image].