反应详情

Prepared using (S)-glycidyl methanesulfonate (Intermediate H, Step 1) in place of (R)-glycidyl methanesulfonate (Intermediate F, Step 1), and morpholine in place of piperidine in Step 1, and 1,3-thiazole-5-carboxylic acid in place of nicotinic acid in Step 2 (42.0 mg, 41%): TLC (9:1 CH2Cl2/MeOH+1% NH4OH in MeOH)Rf 0.43; HPLC ret. time 0.81 min.; 1H NMR (DMSO-d6+1 drop TFA-d) δ 3.11-3.0 (m, 4H), 3.43-3.52 (m, 2H), 3.69 (app t, J=11.8 Hz, 1H), 3.78 (app t, J=11.6 Hz, 1H) 3.88-4.00 (m, 2H), 4.01 (s, 3H), 4.16-4.27 (m, 4H), 4.37-4.51 (m, 3H), 7.45 (d, J=9.1 Hz, 1H), 8.01 (d, J=9.1 Hz, 1H), 8.60 (s, 1H), 9.31 (s, 1H); mass spectrum m/z 487 ((M+1)+, 4.6%).

1. customPrepared