反应详情

In a manner similar to that described previously (Example 1), 2-amino-5-bromobenzaldehyde was sequentially reacted with 7-(4-fluorophenyl)-7-oxoheptanoic acid and TFAA-tBuOH. The resulting ester 5B was converted to 5C (Pd(OAc)2, dcpp-2(HBF)4, K2CO3, 5 atm CO, H2O-DMF, 100° C. overnight), coupled with (R)-1-(4-chlorophenyl)ethanamine (HATU, DIPEA) and deprotected with TFA to provide the title compound, 6-[[[1(R)-(4-chlorophenyl)ethyl]amino]carbonyl]-2-(4-fluorophenyl)-3-quinolinepentanoic acid, 5. LCMS (M+H)=505.