Acitemate, Chinoin-123, -Drug Synthesis Database

【结构式】

【药物名称】Acitemate, Chinoin-123

【化学名称】(±)-cis-3-Ethoxycarbonyl-9-carboxymethyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine
　　　　　　(±)-cis-3-Ethoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-9-acetic acid
　　　　　　(±)-cis-3-Carboxy-6,7,8,9-tetrahydro-6-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidine-9-acetic acid 3-ethyl ester

【CA登记号】101197-99-3, 64405-61-4 (Mg salt), 64405-40-9 (undefined stereoch.)

【分子式】C₁₄H₁₈N₂O₅

【分子量】294.30996

【开发单位】Chinoin (Originator)

【药理作用】Lipoprotein Disorders, Treatment of , METABOLIC DRUGS

合成路线1

The reaction of 3-ethoxycarbonyl-6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido [1,2-a]pyrimidine (I) with glyoxilic acid (II) in ethanolic HCl gives 3-ethoxycarbonyl-6-methyl-4-oxo-9-carboxymethylen-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine (IIIa-b), which is reduced with H2 over Pd/C in ethanol.

参考文献中间体

【1】 Hermecz, I.; et al.; US 4123533 .
【2】 Paton, D.M.; Castaner, J.; CHINOIN-123. Drugs Fut 1979, 4, 11, 788.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(IIIa)	39529	(Z)-2-[3-(ethoxycarbonyl)-6-methyl-4-oxo-7,8-dihydro-4H-pyrido[1,2-a]pyrimidin-9(6H)-ylidene]acetic acid		C₁₄H₁₆N₂O₅	详情	详情
(IIIb)	39530	(E)-2-[3-(ethoxycarbonyl)-6-methyl-4-oxo-7,8-dihydro-4H-pyrido[1,2-a]pyrimidin-9(6H)-ylidene]acetic acid		C₁₄H₁₆N₂O₅	详情	详情
(I)	36161	ethyl 6-methyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidine-3-carboxylate		C₁₂H₁₆N₂O₃	详情	详情
(II)	15618	2-Oxoacetic acid; Glyoxylic Acid	298-12-4	C₂H₂O₃	详情	详情

Extended Information