4-Methylmorpholine → HCID 86751081, compound

Participants

Reaction Steps

A solution of 8-2 (0.44 g, 2 mmoles) in DMF (25 ml) was treated with N-(CBZ-4-piperidinyl)methyl amine (0.53 g, 2 mmoles) (8-3), HOBT (0.3 g, 2.2 mmoles) EDC (0.44 g, 2.3 mmoles) followed by NMM (0.4 g, 4 mmoles) and the resulting solution was stirred for 16 hours. The solvent was removed and the residue was taken up in H2O and extracted with EtOAc. The organic extract was washed with 10% KHSO4 solution, brine, saturated NaHCO3 solution, brine and dried (Na2SO4). Solvent removal gave a residue that was purified by flash chromatography on silica gel eluting with CHCl3 (97)/MeOH(3) to give pure 8-4. Rf 0.35 (silica, CHCl3 (95)/MeOH(5). ##STR55##

Provenance & Evidence