Methanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) → HCID 86676364, compound

Participants

Reaction Steps

A mixture of (3R*,4R*)-3-(4-fluorophenyl)-1-phenethyl-piperidine-4-carboxylic acid (50 mg, 0.137 mmol, prepared according to the procedure disclosed in WO 2002/068387) and 4-chlorothiobenzamide (28.3 mg, 0.165 mmol) in CH2Cl2 (1.0 ml) was treated with HBTU (62.5 mg, 0.165 mmol) and DMAP (10 mg, 0.082 mmol) at rt. The mixture was stirred at rt for 6 h and then concentrated. The resulting residue was purified by RP-HPLC(C18, water, acetonitrile, 0.05% TFA) to afford the title compound, which was contaminated with 4-chlorothiobenzamide and was used in the next step without further purification. HPLC/MS: 481.3, 483.1 (M+1); Rt=1.14 (LC-2 HPLC conditions).

Provenance & Evidence