تفاعل #2360792

معادلة التفاعل

( 8 )

(S)-Tert-Butyl 2-(4-(4′-(4-((4-(propylsulfonyl)piperazin-1-yl)methyl)phenylcarbamoyl)biphenyl-4-yl)-1H-imidazol-2-yl)pyrrolidine-1-carboxylate

L-val-OH

TFA

HATU

→

title compound

Methyl(S)-3-methyl-1-oxo-1-((5)-2-(4-(4′-(4-((4-(propylsulfonyl)piperazin-1-yl)methyl)phenylcarbamoyl)biphenyl-4-Yl)-1H-imidazol-2-yl)pyrrolidin-1-yl)butan-2-ylcarbamate

ظروف التفاعل

المعالجة

1. 1
   أخرىoutlined above for the preparation of 5

الإجراء التجريبي

The title compound is prepared from (8) (above) and Moc-L-val-OH using the two-step TFA deprotection and HATU coupling sequence outlined above for the preparation of 5. Yield: 60.5 mg (81%, 2 steps). HPLC: tR1.82 min (method 1); tR 2.17 min, 97.6% purity (method 2). LC-MS m/z calcd for C41H51N7O6S ([M]+), 769. found, 770 ([M+H]+). 1H NMR (CDCl3, 50° C.): δ 0.88 (d, J=6.5 Hz, 6H), 1.06 (t, J=7.5 Hz, 3H), 1.84 (m, 2H), 1.90-2.42 (m, 4H), 2.56 (m, 4H), 2.87 (m, 2H), 3.05 (m, 1H), 3.32 (m, 4H), 3.57 (s, 2H), 3.62 (m, 1H), 3.70 (s, 3H), 3.82 (m, 1H), 4.32 (dd, J=9.0 Hz, 6.5 Hz, 1H), 5.26 (m, 1H), 5.32 (d, J=9.0 Hz, 1H), 7.24 (s, 1H), 7.32 (m, 2H), 7.61 (m, 4H), 7.67-7.87 (m, 4H), 7.93 (m, 2H).

المصدر