A procedure for the chiral resolution of 1,3-oxathiolanes substituted in position 2 and substituted in position 4

摘要

A process for producing a compound of the general formula (II), comprising the steps of: (a) formation of a substituted 1,3-oxathiolane in position 2 and substituted in position 4 of the general formulas (II) and (III ): ** Formula ** wherein R2 is H, C (O) C1-6 alkyl, C (O) O C1-6 alkyl, C (O) C6-12 aryl, C (O) O aryl C6-12, C (O) C6-12 alkyl aryl, C (O) O C6-12 alkyl aryl, C (O) C1-6-aryl alkyl, C (O) O C1 alkyl -6-aryl, or a silyl protecting group of the general formula SiR7R8R9 wherein R7, R8 and R9 are each independently selected from C1-6 alkyl, aryl or C1-6-aryl alkyl; R3 and R4 are the same or different and each of them is individually selected from H or C (O) -R6; R6 is C6-12 aryl or C1-6-aryl alkyl, wherein the C1-6-aryl alkyl is preferably a C1-6-aryl alkyl of C6-12; and R5 is H, Br, Cl, F, I or CF3; and (b) a selective recrystallization of the compound of the general formula (II) from a solvent, wherein the solvent is a C1-6 alcohol or mixtures of C1-6 alcohols.