Acetone → N-(1-cyclopentyl-2-pyrrolidinyl methyl)-2,4-dimethoxy-5-methylsulphonyl benzamide

Participants

Reaction Steps

91 g of 2,4-dimethoxy-5-methylsulphonyl benzoic acid, 400 ml of acetone, 130 ml of water and 48.6 ml of triethylamine are placed in a liter flask fitted with an agitator, a thermometer and a dropping funnel. 47.6 g of isobutyl chloroformate is dripped into the solution obtained, at about 10° C. It is agitated for 40 minutes, then 58.8 g of 1-cyclopentyl-2-aminomethyl-pyrrolidine is poured in drop by drop at about 0° C. A precipitate appears after 30 minutes of agitation at room temperature. It is allowed to react then the precipitate is filtered off, washed with water and dried. 74 g of a crude version of the product is obtained, melting at 198° C.

Provenance & Evidence