[摘要]：An efficient synthesis of HIV integrase inhibitor I via a unique asym. hydrogenation of a mixt. of imines/enamine is described. Hydrogenation of the imines/enamine by a Rh(I)-Josiphos complex afforded II in 90% yield and 90% ee. Amide formation completed the synthesis of I in 58% overall yield from III, which is readily available from 3,4-dihydro-2H-pyran in a seven-step sequence. A deuterium labeling study suggests the asym. hydrogenation proceeds predominantly via the enamine tautomer.
