Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphate → (R)-tert-Butyl 2-(4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)benzamido)-4-(thiophen-2-yl)phenylcarbamate

Participants

Reaction Steps

A solution of acid 7 (0.20 g, 0.62 mmol), amine 4 (0.164 g, 0.56 mmol) and BOP reagent (0.30 g, 0.68 mmol) in pyridine (4 mL) was stirred for 18 h, concentrated, diluted with AcOEt, washed with aqueous sodium bicarbonate (NaHCO3), brine, dried over MgSO4, filtered and concentrated. Flash chromatography purification of the residue (eluent: 1:1 MeOH:AcOEt with 1% triethylamine) gave compound 8 (0.198 g, 67% yield).

Provenance & Evidence