METHOD FOR CHIRAL RESOLUTION OF 2,4-DISUBSTITUTED 1,3-OXATHIOLANES Russian patent published in 2013 - IPC C07D411/04 A61K31/506 A61P31/12 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing compounds of formula (II) comprising the steps: (a) forming 2,4-disubstituted 1,3-oxathiolane of formula (II) and (III) where the substitutes are as defined in the claim; (b) selective recrystallisation of the compound of general formula (II) from a C₁-C₆ alcohol or a mixture of C₁-C₆ alcohols. The invention also relates to a method of producing a compound of formula (VI) comprising the steps: (a) forming 2,4-disubstituted 1,3-oxathiolane of formula (II) and (III); (b) selective recrystallisation of the compound of formula (II) from a C₁-C₆ alcohol or a mixture of C₁-C₆ alcohols; and (c) removing protective groups in the compound of formula (II) to obtain a compound of formula (VI). The invention also relates to compounds of formulae (VIII) and (IX) where R2 is C(O)phenyl; each of R3 and R4 is independently selected from H or benzoyl under the condition that when R3 is H, R4 is not H; and when R4 is H, R3 is not H; and R5 is H, Br, Cl, F, I or CF₃.

EFFECT: improved methods of producing 2,4-disubstituted 1,3-oxathiolanes and intermediate compounds for production thereof.

23 cl, 5 ex, 23 tbl, 12 ex