(4S,7R,10aS)-4-Amino-7-(trifluoromethyl)hexahydro-2H-pyrido[2,1-b][1,3]thiazepin-5(7H)-one → (2R,5R)-2,5-Dibenzyl-N1-((S)-1-(2-methoxyphenyl)-2-oxoazepan-3-yl)-N6-((4S,7R,10aS)-5-oxo-7-(trifluoromethyl)octahydro-2H-pyrido[2,1-b][1,3]thiazepin-4-yl)hexanediamide

Participants

Reaction Steps

(2R,5R)-2,5-Dibenzyl-N1-((S)-1-(2-methoxyphenyl)-2-oxoazepan-3-yl)-N6-((4S,7R,10aS)-5-oxo-7-(trifluoromethyl)octahydro-2H-pyrido[2,1-b][1,3]thiazepin-4-yl)hexanediamide was synthesized as described in General Procedure H using Intermediate 70 (21 mg, 0.039 mmol) and Intermediate 78 (10 mg, 0.037 mmol) to give a white solid (26 mg, 83% yield). Anal. Calcd. for C43H51F3N4O5S m/z 792.7. found: 793.4 (M+H)+; 1H NMR (400 MHz, CDCl3) δ ppm 7.37-6.99 (m, 12H), 6.99-6.86 (m, 3H), 6.77 (s, 1H), 5.27 (t, 1H), 5.02-4.80 (m, 2H), 4.75 (dd, J=10.2, 6.6 Hz, 1H), 3.96-3.81 (m, 1H), 3.80 (s, 3H), 3.38 (s, 1H), 3.24-3.07 (m, 1H), 2.91-2.46 (m, 7H), 2.36 (dd, J=12.8, 8.4 Hz, 4H), 2.14-1.58 (m, 9H), 1.58-1.20 (m, 5H).

Provenance & Evidence