1-Boc-3-pyrrolidinol → HCID 71255391, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of tert-butyl 3-hydroxypyrrolidine-1-carboxylate (134.7 mg, 0.72 mmol), 4-(4-bromo-6-methylquinolin-2-yl)-2,3,4,5-tetrahydro-1,4-benzothiazepine 1,1-dioxide (300 mg, 0.72 mmol, prepared in analogy to 4-(4-chloro-6-(trifluoromethoxy)quinolin-2-yl)-2,3,4,5-tetrahydro-1,4-benzothiazepine 1,1-dioxide in Example 17-1), 1,1′-bis(diphenylphosphino)ferrocene-palladium(II)dichloride (57.12 mg, 0.07 mmol), 1,1′-bis(diphenylphosphino)ferrocene (38.78 mg, 0.07 mmol) and sodium tert-butoxide (138.24 mg, 1.44 mmol) in 1,4-dioxane (5 mL) was heated with stirring in a sealed 10 mL of microwave process vial for 1 hour at 130° C. under microwave irradiation. The reaction mixture was concentrated in vacuo and the residue was purified by preparative HPLC to afford 20 mg of the desired product (yield was 5.3%).

Provenance & Evidence