2-Amino-5-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]cinnamic acid → Vesnarinone

Participants

Reaction Steps

2-Amino-5-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]cinnamic acid (5 g) was dissolved in DMF (50 ml), and 5% palladium-carbon (0.5 g) was added to the solution. The mixture was reacted at 80° C. for 4 hours using Parr's apparatus at a hydrogen gas pressure of 3 kg/cm2. After removing hydrogen gas, the content was taken out. After removing the catalyst, the reaction mixture was concentrated to half the original volume and poured into a large volume of water. Crystals which precipitated were collected by filtration and recrystallized from ethanol-chloroform to give 2.9 g of 6-[4-(3,4-dimethoxybenzoyl)-1-piperazinyl]-3,4-dihydrocarbostyril, m.p. 238°-239.5° C., colorless granules.

Provenance & Evidence