chinoin 123

Originator

Acitemate ,Onbio Inc.

Manufacturing Process

23.6 g of 3-ethoxycarbonyl-7-methyl-4-oxo-6,7,8,9-tetrahydro-4Hpyrido[ 1,2a]pyrimidine and 10.0 g of glyoxylic acid monohydrate are reacted and the obtained 3-ethoxycarbonyl-7-methyl-9-carboxy(hydroxymethyl)-4- oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2a]pyrimidine is heated in 150 ml ethanol under stirring for 3 h. After cooling the crystals are filtered off and recrystallized from ethanol. Thus 3-ethoxycarbonyl-7-methyl-9- (carboxymethylene)-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2a]pyrimidine melting point 110°-112°C, is obtained (yield: 51%).
55.6 g of 3-ethoxycarbonyl-9-(carboxymethylene)-4-oxo-6,7,8,9-tetrahydro- 4H-pyrido[1,2a]pyrimidine are hydrogenated in 500 ml of ethanol in the presence of 20.0 g of 9% by weight Pd/C catalyst containing metal. When 1 mole of hydrogen has been used up, the catalyst is removed from the reaction mixture by filtration and the solution is evaporated under reduced pressure. The 3-ethoxycarbonyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-9- acetic acid is obtained (yield: 57%), melting point 156°-157°C (recrystallized from ethanol).

Therapeutic Function

Platelet aggregation inhibitor, Antihyperlipidemic