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

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.