Morpholine → (S)-2-((S)-3,3-Dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-7-((3R,5S)-1-((S)-3,3-dimethyl-2-((S)-2-(methylamino)propanamido)butanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)-N-((S)-1-morpholino-1-oxo-3-phenylpropan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide

Participants

Reaction Steps

Following procedures analogous to those described for the preparation of Example 42, (S)-2-((S)-2-((S)-2-((S)-2-((tert-butoxycarbonyl)(methyl)amino)propanamido)-3,3-dimethylbutanoyl)-7-((3R,5S)-1-((S)-2-((S)-2-((tert-butoxycarbonyl)(methyl)amino)propanamido)-3,3-dimethylbutanoyl)-5-(((R)-1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)pyrrolidin-3-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamido)-3-phenylpropanoic acid (Compound B of Example 41, 25 mg, 0.021 mmol) and morpholine (Aldrich, 3 mg, 0.032 mmol) were converted to the title compound (8 mg, 37% over 2 steps). MS (ESI+) m/z 1032.7 (M+H)+.

Provenance & Evidence