1,2-Dichloroethane → methyl N-[(2S)-1-[[(2S,3S)-4-[[[(2S)-2-(ethoxycarbonylamino)-3-methylbutanoyl]amino]-[[4-(1,3-thiazol-2-yl)phenyl]methyl]amino]-3-hydroxy-1-phenylbutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamate

Participants

Reaction Steps

Analogously to Example 7,106 mg (0.56 mmol) of N-ethoxycarbonyl-(L)-valine, 201 mg (1.05 mmol) of EDC and 95 mg (0.7 mmol) of HOBT in 4.6 ml of DMF and 293 μl (2.1 mmol) of TEA are reacted with 0.35 mmol of 1-[4-(thiazol-2-yl)-phenyl]-4(S)-hydroxy-2-amino-5(S)-N-(N-methoxycarbonyl-(L)-valyl)amino-6-phenyl-2-azahexane to form the title compound: Anal. (C35H48N6O7S (0.20 H2O)) calc. C, 60.01, H, 6.96, N, 12.00, S, 4.58, H2O 0.51: found C, 60.07, H, 6.78, N, 11.93, S, 4.70, H2O 0.52; HPLC20-100: tRet=14.6; FAB MS (M+H)+=697.

Provenance & Evidence