新しい非ステロイド系抗炎症剤(第2報)2-置換-5-ベンゾチアゾール酢酸とその誘導体の新合成法

概要

論文の詳細を見る
An industrially advantageous synthetic method to obtain 2-substituted 5-benzothiazoleacetic acids (12), which have a strong antiinflammatory activity and low toxicity, was investigated. Consequently, 12 was easily obtained by only two steps using 4-chloro-3-nitrophenylacetic acid (8) as a starting material. After 8 was heated under reflux with sodium sulfide nonahydrate in water, bis-(2-amino-4-carboxymethylphenyl) disulfide (9) was obtained by acidification of the mixture with acetic acid. 9 was reacted with the corresponding aromatic aldehyde in pyridine in a mild condition to form 12 in a high yield. 12 and its esters were also synthesized by three other methods.
公益社団法人日本薬学会の論文
1974-08-25