反应详情

A stirred solution of (R)-5-(2benzenesulfonylethenyl)-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole (34.0 g) in acetone (200 mL) was treated with methanesulfonic acid (8.5871 g) then 5% palladium on carbon (50% wet) (34.0 g) added and the mixture exposed to hydrogen (50 psi) at ambient temperature. When conversion was judged to be complete the mixture was filtered (washing with acetone--85 mL--and mixed acetone/water--81 mL/4 mL). The combined filtrate and washings were diluted with water (800 mL) and the pH adjusted (with stirring) to about 11 by addition of 40% aqueous sodium hydroxide. After granulation of the precipitate the solids were collected by filtration to give the title compound (25.08 g) as that produced in Example 32).

1. filtrationwas filtered
2. wash(washing with acetone--85 mL--and mixed acetone/water--81 mL/4 mL)
3. additionThe combined filtrate and washings were diluted with water (800 mL)
4. additionby addition of 40% aqueous sodium hydroxide
5. filtrationAfter granulation of the precipitate the solids were collected by filtration