1,2-Dichloroethane → HCID 131720983, compound

Participants

Reaction Steps

Analogously to Example 1, a solution of 0.964 g (1.5 mmol) of 1-[4-(pyridin-2-yl)-phenyl]-4(S)-hydroxy-2-amino-5(S)-N-(N-methoxycarbonyl-(L)-tert-leucyl)amino-6-phenyl-2-azahexane hydrochloride in 10 ml of DMF is added dropwise to a mixture of 0.42 g (2.4 mmol) of N-methoxycarbonyl-(L)-valine, 0.862 g (4.5 mmol) of EDC, 0.405 g (3 mmol) of HOBT and 1.26 ml of TEA in 10 ml of DMF. After working up, the crude product is digested in DIPE, filtered off and dried. Subsequent column chromatography (SiO2 ; hexane/ethyl acetate: 1/1 to 3/1) yields the pure title compound (TLC: Rf =0.35 (ethyl acetate); HPLC20-100 : tRet =10.9. FAB MS (M+H)+ =691.

Provenance & Evidence