Trifluoroacetic acid → HCID 57265579, compound

Participants

Reaction Steps

A solution of 478 mg (1.01 mmol) of 4(R)-[[t-butoxycarbonyl][(1R,2S)-1,2-diphenyl-2-hydroxyethyl]]amino-2,3,4,5-tetrahydro-1H-2-benzazepin-3-one (Example 1, Step B) in 5 mL of methylene chloride at room temperature was treated with 0.5 mL of trifluoroacetic acid. The mixture was stired at room temperature for 3 hours then all volatiles removed under vacuum. The residue was dissolved in 5 mL of water and the solution made basic (pH 10-11) by the addition of solid sodium carbonate. The mixture was extracted with chloroform (5×) and the combined extracts dried over anhydrous potassium carbonate, filtered and solvents removed under vacuum to give 372 mg (1.00 mmol, 99%) of 4(R)-[[(1R,2S)-1,2-diphenyl-2-hydroxyethyl]]amino-2,3,4,5-tetrahydro-1H-2-benzazepin-3-one which was used in the next step without purification.

Provenance & Evidence