Benzyl Alcohol → 2-[(Benzyloxycarbonyl)(methyl)amino]-6-chloro-1-oxo-4-phenyl-1,2-dihydroisoquinoline-3-carboxylic acid benzyl ester

Participants

Reaction Steps

To a mixture of 2-[(benzyloxycarbonyl)(methyl)amino]-6-chloro-1-oxo-4-phenyl-1,2-dihydroisoquinoline-3-carboxylic acid (190 mg), triphenylphosphine (130 mg), benzyl alcohol (52 μl) and THF (6.0 ml) was added diethyl azodicarboxylate (86 μl) at 0° C. with stirring, and the mixture was stirred at room temperature for 2 hrs. The reaction mixture was concentrated under reduced pressure, the residue was purified by medium pressure preparative LC (hexane/ethyl acetate=9/1-3/2) to give 2-[(benzyloxycarbonyl)(methyl)amino]-6-chloro-1-oxo-4-phenyl-1,2-dihydroisoquinoline-3-carboxylic acid benzyl ester as a colorless powder.

Provenance & Evidence