NS-398
NS-398(COX-2抑制剂)Chemical Name: N-[2-(Cyclohexyloxy)-4-nitrophenyl]methanesulfonamide
CAS No. 123653-11-2, 123653-43-0 (Ca salt), 123653-44-1 (Na salt)
项目整合开发状态: Preclinical
项目研究机构: Taisho (Originator)
合成路线:The condensation of 2-fluoronitrobenzene (I) with cyclohexanol (II) by means of NaH gives 2-(cyclohexyloxy)nitrobenzene (III),which is reduced with H2 over Pd/C in methanol yielding 2-(cyclohexyloxy)aniline (IV).The acylation of (IV) with methanesulfonyl chloride (V) in pyridine affords N-(2-cyclohexyloxy phenyl)methanesulfonamide (VI),which is finally nitrated with concentrated HNO3 in hot acetic acid.
📌 参考资料/链接：
参考文献标题:Sulfoanilide cpds
文献作者:Yoshikawa,K.; Ohuchi,Y.; Sekiuchi,K.; Saito,S.; Hatayama,K.; Sota,K.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0317332; JP 1990000268
📄 详细内容
合成路线:The condensation of 2-fluoronitrobenzene (I) with cyclohexanol (II) by means of NaH gives 2-(cyclohexyloxy)nitrobenzene (III),which is reduced with H2 over Pd/C in methanol yielding 2-(cyclohexyloxy)aniline (IV).The acylation of (IV) with methanesulfonyl chloride (V) in pyridine affords N-(2-cyclohexyloxy phenyl)methanesulfonamide (VI),which is finally nitrated with concentrated HNO3 in hot acetic acid.
参考文献标题:Antiinflammatories,analgesics and antipyretics
文献作者:Yoshikawa,K.; Ohuchi,H.; Saito,H.; Nakajima,Y.; Hatayama,K.; Soda,H.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:JP 1990300122
合成路线:The condensation of 2-fluoronitrobenzene (I) with cyclohexanol (II) by means of NaH gives 2-(cyclohexyloxy)nitrobenzene (III),which is reduced with H2 over Pd/C in methanol yielding 2-(cyclohexyloxy)aniline (IV).The acylation of (IV) with methanesulfonyl chloride (V) in pyridine affords N-(2-cyclohexyloxy phenyl)methanesulfonamide (VI),which is finally nitrated with concentrated HNO3 in hot acetic acid.
参考文献标题:NS-398
文献作者:Prous,J.; Castar,J.; Mealy,N.
参考来源:Drugs Fut 1993,18(7),603
产品链接: CAS No. 123653-11-2››