Phenol → Esomeprazole BINOL

Participants

Reaction Conditions

Reaction Steps

BINOL (4.14 g; 14.47 mmol) and phenol (1.36 g; 14.47 mmol) were added to toluene (100 ml) at 20-30° C. and heated the mixture to 45° C. Omeprazole (5 g; 14.47 mmol) was added to the mixture and stirred at 40-45° C. for 30 min. The solution was cooled to 20-30° C. and stirred for 2 h to crystallize the product. Hexane (50 ml) was added to the reaction mass and stirred for 15 h at 20-30° C. for complete crystallization of title compound, which was filtered, washed with toluene-hexane mixture and dried to obtain white solid of inclusion complex of esomeprazole-BINOL.

Provenance & Evidence