梁晓天, 卢玉华, 祁建新. 1,3-双(2-羧基色酮-7氧基)2-羟基丙烷二钠盐(78012)的简易合成方法J. 药学学报, 1982, 17(2): 143-145.
引用本文: 梁晓天, 卢玉华, 祁建新. 1,3-双(2-羧基色酮-7氧基)2-羟基丙烷二钠盐(78012)的简易合成方法J. 药学学报, 1982, 17(2): 143-145.
LIANG Xiao-tian, LU Yu-hua , QI Jian-xin, . A SIMPLIFIED SYNTHESIS OF 1,3-BIS (2-CARBOXYCHROMONE-7-OXY)-2-HYDROXYPROPANE DISODIUM SALT(78012)J. Acta Pharmaceutica Sinica, 1982, 17(2): 143-145.
Citation: LIANG Xiao-tian, LU Yu-hua , QI Jian-xin, . A SIMPLIFIED SYNTHESIS OF 1,3-BIS (2-CARBOXYCHROMONE-7-OXY)-2-HYDROXYPROPANE DISODIUM SALT(78012)J. Acta Pharmaceutica Sinica, 1982, 17(2): 143-145.

1,3-双(2-羧基色酮-7氧基)2-羟基丙烷二钠盐(78012)的简易合成方法

A SIMPLIFIED SYNTHESIS OF 1,3-BIS (2-CARBOXYCHROMONE-7-OXY)-2-HYDROXYPROPANE DISODIUM SALT(78012)

  • Abstract: This paper gives a simplified synthesis of "78012", 1,3-bis (2-carboxychromone-7-oxy)-2-hydroxypropane disodium salt, which has similar antiallergic activity as DSCG (disodium chromoglycate). Resoreinol, on Fridel-Crafts acetylation, gave 2,4-dihydroxyacetophenone. When refluxed with diethyl oxalate in sodium ethoxide or sodium methoxide solutions 2,4-dihydroxyacetophenone gave Ⅲ or Ⅱ, respectively. 78012 (Ⅳ) is conveniently prepared from Ⅱ or Ⅲ by treatment with epichlorohydrin in aqueous ethanolic alkaline solution. The overall yield of 78012 from resacetophenone is about 30%. This sodium salt is being examined in Clinical trials for the treatment of allergic rhinitis and asthma.

     

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