Ammonia → HCID 58169884, compound

Participants

Reaction Steps

A solution of Methyl (5R,7R)-8-{[{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}(methyl)amino]carbonyl}-7-(4-fluoro-2-methylphenyl)-1,8-diazaspiro[4.5]decane-2-carboxylate (diastereoisomer 2) (Intermediate 8, 18 mg, 0.030 mmol) in 7N Ammonia in MeOH (5 mL, 35.0 mmol) was stirred at 25° C. for 1 day and then it was left still for 2 days. The solvent was evaporated to dryness and the crude was purified by SCX and silica cartridges (from 1:0 to 97.5:2.5 DCM/0.5 M NH3 in MeOH) to give two batches of the title compound as colourless oil (total amount: 14.9 mg, 0.025 mmol, 84% yield). 1H NMR (400 MHz, DMSO-d6) δ ppm 7.90-8.08 (m, 1H) 7.62-7.77 (m, 2H) 7.26-7.46 (m, 1H) 7.04-7.23 (m, 2H) 6.84-6.96 (m, 1H) 6.69-6.80 (m, 1H) 5.24-5.41 (m, 1H) 4.31-4.49 (m, 1H) 3.49-3.65 (m, 1H) 3.10-3.25 (m, 1H) 2.94-3.08 (m, 1H) 2.61-2.87 (m, 3H) 2.35 (s, 3H) 1.92-2.10 (m, 1H) 1.62-1.84 (m, 2H) 1.38-1.60 (m, 8H).

Provenance & Evidence