1,2-Dichloroethane → methyl N-[(1S,2S)-1-[[(1S,2S)-1-benzyl-2-hydroxy-3-[[[(2S)-2-(methoxycarbonylamino)-3-methyl-butanoyl]amino]-[(4-thiazol-5-ylphenyl)methyl]amino]propyl]carbamoyl]-2-methyl-butyl]carbamate

Participants

Reaction Steps

Analogously to Example 7, 140 mg (0.80 mmol) of N-methoxycarbonyl-(L)-valine, 288 mg (1.5 mmol) of EDC and 135 mg (1.0 mmol) of HOBT in 2 ml of DMF and 418 μL of TEA are reacted with 0.5 mmol of 1-[4-(thiazol-5-yl)-phenyl]-4(S)-hydroxy-2-amino-5(S)-N-(N-methoxycarbonyl-(L)-iso-leucyl)amino-6-phenyl-2-azahexane in 5 ml of DMF to form the title compound: m.p: 202-204° C.; HPLC20-100: tRet=14.0; FAB MS (M+H)+=697.

Provenance & Evidence