METHOD OF PRODUCING CLOPIDOGREL AND DERIVATIVES THEREOF Russian patent published in 2012 - IPC C07D495/04 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing (S)-2-clopidogrel and salts thereof, which involves the following steps: (a) enzymatic hydrolysis of a racemic 2-chlorophenylglycine alkyl ester of formula 9 using an enzyme which is efficient for aqueous solution or aqueous phase hydrolysis to obtain an optically active compound of formula 10 ; (b) reaction of the formed optically active compound of formula 10 with a compound of formula 11 to obtain a compound of formula 12 and (c) cyclisation of the compound of formula 12 with a formulating agent in the presence of acid, where R₁ denotes H, substituted or unsubstituted C₁-C₈-alkyl, substituted or unsubstituted C₁-C₈-alkenyl, benzyl or C₃-C₆-cycloalkyl; and X denotes a halogen atom selected from a group consisting of fluorine (F), chlorine (Cl), bromine (Br) and iodine (I), or -OSO₂R₂ (where R₂ denotes a substituted or unsubstituted C₁-C₈-alkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heteroarylalkyl).

EFFECT: novel method of producing clopidogrel which does not involve use of chiral resolving agents, which reduces the cost of preparations while maintaining high output of the product.

7 cl, 4 ex