| 摘要 |
PROBLEM TO BE SOLVED: To provide a method for synthesis of carbamoylpyridone HIV integrase inhibitors.SOLUTION: The present invention provides a method for synthesis of carbamoylpyridone HIV integrase inhibitors, including the steps of obtaining brominated compound II-II by a reaction of the following scheme, and forming 2,4-difluorophenyl CH2-NH-C(O)- side chain for debenzylation [R is -CHO, -CH(OH)2, -CH(OH)(OR4), -CH(OH)-CH2OH or -CH(OR5)(OR6); P1 is H or a hydroxyl protecting group; P3 is H or a carboxy protecting group; R4 is a C1-6 alkyl; R5 and R6 are a C1-6 alkyl or a C1-6 alkyl and together form a 5-, 6- or 7-membered ring].SELECTED DRAWING: None |
