Disodium cromproxate, 78012, -Drug Synthesis Database

【结构式】

【药物名称】Disodium cromproxate, 78012

【化学名称】7,7'-[(2-Hydroxytrimethylene)dioxy]bis(4-oxo-4H-1-benzopyran-2-carboxylic acid) disodium salt
　　　　　　7,7'-[(2-Hydroxy-1,3-propanediyl)bis-(oxy)]bis[4-oxo-4H-1-benzopyran-2-carboxylic acid] disodium salt
　　　　　　1,3-Bis(2-carboxychromon-7-yloxy)-2-hydroxypropane disodium salt

【CA登记号】37092-38-9

【分子式】C₂₃H₁₄Na₂O₁₁

【分子量】512.34103

【开发单位】AstraZeneca (Originator), Institute of Materia Medica (Originator)

【药理作用】Antiallergy/Antiasthmatic Drugs, Asthma Therapy, RESPIRATORY DRUGS, Mediator Release Inhibitors

合成路线1

2,4-Dihydroxyacetophenone (I) is formed by the Friedel-Crafts acetylation of resorcinol. This compound is condensed with diethyl oxalate in sodium ethoxide solution, affording (II). Disodium cromproxate (IV) is conveniently prepared from (II) by treatment with epichlorohydrine in aqueous ethanolic alkaline solution. It is recrystallized from hot water.

参考文献中间体

【1】 Ruyun, J.; Disodium Cromproxate. Drugs Fut 1991, 16, 5, 422.
【2】 Liang, X.; Qi, J.; Lu, Y.; A simplified synthesis of 1,3-bis-(2-carboxychromone-7-oxy)-2-hydroxypropane disodium salt (78012). Acta Pharm Sin 1982, 17, 2, 143-5.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
	10146	Epichlorohydrin; 2-(Chloromethyl)oxirane	106-89-8	C₃H₅ClO	详情	详情
	10361	1,3-Dihydroxybenzene; m-Dihydroxybenzene; Resorcinol; Resorcin; 1,3-Benzenediol	108-46-3	C₆H₆O₂	详情	详情
(I)	13961	Resacetophenone; 1-(2,4-Dihydroxyphenyl)-1-ethanone	89-84-9	C₈H₈O₃	详情	详情
(II)	13962	ethyl 7-hydroxy-4-oxo-4H-chromene-2-carboxylate		C₁₂H₁₀O₅	详情	详情
(III)	13963	ethyl 7-(3-[[2-(ethoxycarbonyl)-4-oxo-4H-chromen-7-yl]oxy]-2-hydroxypropoxy)-4-oxo-4H-chromene-2-carboxylate		C₂₇H₂₄O₁₁	详情	详情

Extended Information