Process for the preparation of optical isomers of thiazolo (3,2-a) pyrimidines of the manufactured isomers, pharmaceutical compositions containing them and intermediates for implementing the method

摘要

Process for the preparation of optical isomers of products of formula (I) in which R = C6H5 or C6H5CH2 optionally substituted by one or more halogens, alkyl, alkoxy, alkylthio (1-4 C) or else R = alkyl (1-4 C) unsubstituted or substituted by 1 to 3 halogens, alkenyl (2-4 C) or cycloalkyl (3-6 C) and R1 = H or else R and R1, which are different, denote C6H5 or C6H5CH2 optionally substituted by 1 or more halogens, alkyl, alkoxy or alkylthio (1-4 C) or else denote alkyl (1-4 C) consisting in: a) opening the racemic product of formula (I) into racemic product (II), b) reacting the racemic product (II) with an optically active amine to obtain a product (III) in the form of a mixture of two diastereoisomeric forms, c) separating the mixture of the two diastereoisomeric forms of the product of formula (III), d) separately hydrolysing and cyclising each of these forms to obtain the optically active product (I). The invention also relates to the optically active isomers (I) obtained and the intermediates (II) needed for applying the process. IMAGE