Preparation of 3, 3', 5, 5'-tetrakis(1-methyl)biphenyl-4,4'-diol ( 4) Propofol (1) (5 g, 28 mmol) was charged into water (150 mL) followed by addition of FeCl 3 (5.6 g, 30.3 mmol) and the reaction mixture was heated at 90 o C for 1 h. Reaction mixture was allowed to cool to room temperature and extracted with ethyl acetate (2 × 75 mL). Combined organic layer was dried over sodium sulphate, filtered and concentrated to give the crude product which was used as such for the next step. To a solution of crude residue in THF (45 mL) and MeOH (5 mL), was added sodium borohydride (3.2 g, 84 mmol) and reaction mixture was stirred
Darifenacin is a potent and competitive M 3 selective receptor antagonist (M 3 SRA), and its hydrobromide salt (1) is the active ingredient of pharmaceutical formulations for oral treatment of urinary incontinence. The present work demonstrates an efficient, commercial manufacturing process for darifenacin hydrobromide (1).
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