Hydrochloric Acid → Gly-L-Leu-L-Met-NH2

Participants

Reaction Steps

Condensation of BocGlyOPFP (7.2 g.) and HLeu-MetNH2 hydrochloride salt (Example 1, 10.2 g.) by the actived ester method gave BocGly-Leu-MetNH2 in 73% yield. De-t-butoxycarbonylation of BocGly-Leu-MetNH2 (9.38 g.) using hydrogen chloride in acetic acid gave HGly-Leu-MetNH2 in 77% yield. Condensation of BocD, LBpaOH (1.6 g.) and H-Gly-Leu-MetNH2 (2.13 g.) by the mixed anhydride method using diphenylphosphinyl chloride gave BocD,LBpa-Gly-Leu-MetNH2, de-t-butoxycarbonylation of which (1.1 g.) using hydrogen chloride in acetic acid gave HD, LBpa-Gly-Leu-MetNH2 in 30% overall yield.

Provenance & Evidence