METHYL 2-(BOC-PIPERAZIN-1-YL)-5-NITROBE& synthesis

Yield:-

Reaction Conditions:

with hydrogen;palladium 10% on activated carbon in methanol at 20; for 2 h;

Steps:

147

[0306] To a solution of 4-(2-methoxycarbonyl-4-nitro-phenyl)-piperazine-l-carboxylic acid fert-butyl ester (1.0 g, 2.7 mmol) in MeOH (30 mL) was added 10 wt% Pd/C (0.1 equiv by wt) under argon atmosphere. The mixture was evacuated and then refilled with hydrogen (3 cycles) and stirred at room temperature for 2 h. The heterogeneous reaction mixture was filtered through a pad of Celite, washed with MeOH and concentrated in vacuo. The crude amino-compound was used in the next step without purification. MS (ES+): m/z 336 (M+H)⁺.

References:

WO2007/53452,2007,A1 Location in patent:Page/Page column 157