(S)-2-AMINOMETHYL-1-N-BOC-PIPERIDINE synthesis

Yield:-

Reaction Conditions:

with potassium carbonate in methanol for 16 h;

Steps:

4 Description 4: (S) 2-AMINOMETHYL-PIPERIDINE-L-CARBOXYLIC acid tert butyl ester
The product from D3 (18. 2g) was dissolved in methanol (500ML) and treated with potassium carbonate (16. 1g). After stirring for 16h solvent was removed at reduced pressure and the residue partitioned between dichloromethane/water. The organic phase was separated, washed with brine, dried and solvent removed at reduced pressure. the residue was column chromatographed (silica gel, 0-10% (9: 1 methanol/ammonia) in dichloromethane eluant) to give the title compound (8.82g). Mass spectrum (APt : Found 215 (1W). CLLH22N202 requires 214. [A] D-32. 2@ 28 c = 1% in chloroform. 1H NMR 8 : 1.20-1. 70 (8H, m), 1.46 (9H, s), 2.64-2. 80 (2H, m), 2.94 (1H, dd), 3.99 (1H, m) and 4.15 (1H, m).

References:

GLAXO GROUP LIMITED WO2004/41791, 2004, A1 Location in patent:Page 14-15