FMoc-Val-Cit-PAB

Fmoc-Val-Cit-PAB is a commonly used bridge for a degradable antibody-conjugated drug (ADC).

159858-21-6

623-04-1

159858-22-7

The general procedure for the synthesis of the target compound (CAS:159858-22-7) from (S)-2-((S)-2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-3-methylbutanoylamino) and p-aminobenzenemethanol (PABOH) was carried out as follows: 60 ml of dichloromethane (DCM) mixed with methanol (MeOH) in the ratio of 2:1, by volume of the Solvent was added to the reaction flask, followed by 4.2 mmol Fmoc-vc2g and 1.04 g (2 eq.) of PABOH. after stirring until complete dissolution, 2.0 g (2 eq.) of EEDQ was added. the reaction system was protected from light at room temperature, and the reaction was continuously stirred for 2.0 days. After completion of the reaction, the reaction mixture was concentrated under reduced pressure at 40 °C to give a white solid. The white solid was collected, 100 ml of methyl tert-butyl ether (MTBE) was added, stirred and filtered, and the filter cake was washed with methyl tert-butyl ether. The resulting white solid was dried under reduced pressure at 40 °C to give 2.2 g of the target product in about 88% yield.