Tofisopam → HCID 13500543, compound

Participants

Reaction Steps

To a solution of 3.82 g (0.01 mole) of 1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine in 38 ml of glacial acetic acid a solution of 3 g of sodium borohydride in 10 ml of water is dropped within 2 hours at 3° to 8° C., under stirring. Then the reaction mixture is stirred further for 5 hours at 20° to 25° C. and evaporated in vacuo. The residue (18 g) is dissolved in 30 ml of water, and 10 ml of a 40% sodium hydroxide solution are added. The product separated in soft form crystallizes after cooling. Yield: 3.1 g. The product shrinks from 75° C. The pure compound can be obtained by proceeding as described in Example 2. Yield: 2.29 g. M.p.: 120° to 122° C. Molecular formula: C22H28N2O4.

Provenance & Evidence