具有抗过敏活性的7－羟基－2－（1H－四氮唑－5－基）色酮的合成

Synthesis of an Antiallergic Compound 7-Hydroxy-2(1H-Tetrazole-5-yl)-4H-1-Benzopyran-4-One

具有抗过敏活性的７－羟基－２－（１Ｈ－四氮唑－５－基）色酮的合成李国青，李展，卢玉华（中国医学科学院药用植物研究所，北京１０００９４）许多色酮类化合物具有抗过敏活性，如治疗过敏性支气管哮喘等。色甘酸二钠是使用最广泛的平喘药物之一，但其缺点是口服无效［...

Hydroxy-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-4-one(4) possesses antiallergic activity.From resorcinol, methyl 7-hydroxy-4-oxa-4H-1-benzopyran-2-carboxylate(1) was prepared in 60% yield. After amination of(1) with ammonia, the obtained compound(2) was treated with SOCl2 in DMF to produce (3) in 82% yield. (2) was reacted with POCl3 in DMF to produce(3) and other products. Finally, (3) was reacted with NaN3 to yield(4).The total yield of(4) was 36%.