Rys new asymmetric synthesis of warfarin and its analogs.

摘要

The present invention presents a new MAKING COMPOUNDS OF FORMULA (2A or 2B) or of their pharmaceutically acceptable salts, wherein R SUB 1} PROCESS is selected from the group consisting of phenyl and phenyl substituted with at least one group selected from NO SUB, 2} and halogen; R SUB, 2} is H; R SUB, 3} is selected from the group consisting of C SUB, 4/1} alkyl, phenyl and benzyl; YR SUB, 4} is selected from the group consisting of HY halogen; Comprising the steps of: a) oxidizing a RACEMADO of formula (2) or salt to form a compound DESHIDRATADO formula (3), wherein R SUB, 5} SELECTED FROM A GROUP FORMED BY H, CH SUB, 3}, benzyl, C SUB, 2/8} acyl, NA, LI YK; YB) HYDROGENATION ASYMMETRIC a compound of formula (3) in the presence of chiral phosphino CATALYST FOR FORMING A compound of formula (2a or 2b).