1-(Piperidin-4-yl)-1,3-diazinan-2-one → N-[2-(3,4-Difluorophenyl)-4-[4-[tetrahydro-2-oxo-1(2H)-pyrimidinyl]-1-piperidinyl]butyl]-N-methyl-3-nitro-1-naphthamide Citrate

Participants

Reaction Steps

Using standard reductive amination conditions 4-(tetrahydro-2-oxo-1(2H)-pyrimidinyl)piperidine (Miller, S C; Jacobs, R T; Shenvi, A B. EP 739891) was reacted with N-[2-(3,4-difluorophenyl)-4-oxobutyl]-N-methyl-3-nitro-1-naphthamide [Example 13] and converted to the citrate salt. MS m/z 580 (M+H); analysis for C31H35F2N5O4.1.07 C6H8O7.1.06 H2O: calculated: C, 55.88; H, 5.72; N, 8.71. found: C, 55.94; H, 5.54; N 8.51.

Provenance & Evidence