1-Phenethylamine, (-)- → HCID 86600301, compound

Participants

Reaction Conditions

Reaction Steps

To an RBF was added 7-(2-chloro-pyridin-4-yl)-5-[5-(2,2-difluoro-ethyl)-2,5-diaza-bicyclo[2.2.1]hept-2-yl]-imidazo[1,2-c]pyrimidine (40 mg, 0.10 mmol), 1 mL toluene, and (S)-α-methylbenzylamine (0.015 mL, 0.11 mmol). The mixture was degassed by bubbling nitrogen through solution for 1 h. After Pd(OAc)2 (2 mg, 0.01 mmol), rac-BINAP (6 mg, 0.01 mmol), and NaOtBu (0.20 mg, 0.21 mmol) were added, the mixture was warmed up to 90° C. and stirred for 3 h under nitrogen. The mixture was cooled down to ambient temperature, diluted with 50 mL DCM, washed with 20 mL sat. NaHCO3, and dried over anhydrous Na2SO4. After purification by preparatory TLC, the title compound was obtained. MS (ES+): 476 (M+H)+.

Provenance & Evidence