(4S,8R,10aS)-4-Amino-8-(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,8R,10aS)-5-oxo-8-(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,8R,10aS)-5-oxo-8-(trifluoromethyl)octahydro-2H-pyrido[2,1-b][1,3]thiazepin-4-yl)hexanediamide was synthesized as described in General Procedure H using Intermediate 70 (12 mg, 0.022 mmol) and Intermediate 61 (5.0 mg, 0.019 mmol) to give a white solid (6.5 mg, 43% yield). Anal. Calcd. for C43H51F3N4O5S m/z 792.7. found: 793.6 (M+H)+; 1H NMR (400 MHz, CDCl3) δ ppm 7.44-7.04 (m, 11H), 6.96 (dd, J=17.4, 10.3 Hz, 3H), 5.34-5.13 (m, 2H), 4.89 (d, J=63.4 Hz, 3H), 4.47 (dd, J=13.3, 4.2 Hz, 2H), 3.95 (s, 2H), 3.79 (s, 3H), 3.46 (d, J=42.0 Hz, 2H), 3.05 (s, 2H), 2.98-2.66 (m, 5H), 2.64-2.21 (m, 4H), 2.19-1.87 (m, 4H), 1.87-1.37 (m, 8H).

Provenance & Evidence