PD-164387
Chemical Name: 2,6-Di-tert-butyl-4-[5-(ethylsulfanyl)-1,3,4-thiadiazol-2-yl]phenol
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The reaction of 2,6-di(tert-butyl)phenol (I) with CS2 and ethyl chloroacetate gives the dithiobenzoate (II),which is treated with hydrazine in ethanol yielding the thiobenzoyl hydrazide (III).The cyclization of (III) with CS2 in refluxing ethanol affords the thiadiazolethione (IV),which is finally condensed with ethyl iodide and NaOH in THF.
📌 参考资料/链接：
参考文献标题:Synthesis,structure-activity relationships,and in vivo evaluations of substituted di-tert-butylphenols as a novel class of potent,selective,and orally active cyclooxygenase-2 inhibitors.2.1,3,4- and 1,2,4-thiadiazole series
文献作者:Song,Y.; Connor,D.T.; Sercel,A.D.; Sorenson,R.J.; Doubleday,R.; Unangst,P.C.; Roth,B.D.; Beylin,V.G.; Gilbertsen,R.B.; Chan,K.; Schrier,D.J.; Guglietta,A.; Bornemeier,D.A.; Dyer,R.D.
参考来源:J Med Chem 1999,42(7),1161