FR-188582
3-氯-5-(4-甲基磺酰基苯基)-1-苯基吡唑Chemical Name: 3-Chloro-5-[4-(methylsulfonyl)phenyl]-1-phenyl-1H-pyrazole
CAS No. 189699-82-9
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:The cyclization of phenylhydrazine (I) with 3-[4-(methylsulfanyl)phenyl]acrylonitrile (II) by means of NaOEt in refluxing ethanol gives the aminopyrazoline (III),which is dehydrogenated by means of MnO2 in dichloromethane to yield the 3-aminopyrazole (IV).The diazotation of (IV) with NaNO2 and HCl in water,followed by a treatment with Cu2Cl2,affords the 3-chloropyrazole (V),which is finally oxidized to the target sulfone by means of MCPBA in dichloromethane.
📌 参考资料/链接:
参考文献标题:1,3,5-Trisubstd.pyrazoles for treatment of inflammation
文献作者:Matsuo,M.; Okumura,K.; Ogino,T.; Nakamura,K.; Nishimura,H.; Harada,K.; Hotta,Y.; Tsuji,K.(Fujisawa Pharmaceutical Co.,Ltd.)
参考来源:EP 0856000; JP 1999513403; WO 9713755