GCC-AP0341

5-氨基-3-(4-氯苯基)-N-甲基-1,2,4-三唑-1-硫代甲酰胺Chemical Name: 5-Amino-3-(4-chlorophenyl)-N-methyl-1,2,4-triazole-1-carbothioamide
CAS No. 168893-29-6
项目整合开发状态: Preclinical
项目研究机构: Mitsubishi Pharma (Originator)
合成路线:The reaction of 4-chlorobenzoylhydrazide (I) with S-methyl isothiourea sulfate in aqueous NaOH gave guanidine (II) which,on heating at 220 C,was converted into aminotriazole (III).Subsequent condensation with methyl isothiocyanate in DMF gave thiocarbonyl triazole (IV).Finally,cyclization with diethoxymethyl acetate at 90 C provided the target triazolotriazine.
📌 参考资料/链接:
参考文献标题:Triazole derivs.and pharmaceutical use thereof
文献作者:Akahoshi,F.; Okada,T.; Takeda,S.; Naito,Y.; Fukaya,C.; Kuwahara,S.; Kajii,M.; Nishimura,H.; Sugiura,M.(Welfide Corporation)
参考来源:EP 0710654; JP 1995082270; JP 1995097321; JP 1995101942; US 5750545; WO 9503286

📄 详细内容


合成路线:The reaction of 4-chlorobenzoylhydrazide (I) with S-methyl isothiourea sulfate in aqueous NaOH gave guanidine (II) which,on heating at 220 C,was converted into aminotriazole (III).Subsequent condensation with methyl isothiocyanate in DMF gave thiocarbonyl triazole (IV).Finally,cyclization with diethoxymethyl acetate at 90 C provided the target triazolotriazine.

参考文献标题:Synthesis and pharmacological activity of triazole derivatives inhibiting eosinophilia
文献作者:Naito,Y.; Akahoshi,F.; Takeda,S.; Okada,T.; Kajii,M.; Nishimura,H.; Sugiura,M.; Fukaya,C.; Kagitani,Y.
参考来源:J Med Chem 1996,39(15),3019-3029


合成路线:The reaction of 4-chlorobenzoylhydrazide (I) with S-methyl isothiourea sulfate in aqueous NaOH gave guanidine (II) which,on heating at 220 C,was converted into aminotriazole (III).Subsequent condensation with methyl isothiocyanate in DMF gave thiocarbonyl triazole (IV).Finally,cyclization with diethoxymethyl acetate at 90 C provided the target triazolotriazine.
参考文献标题:Synthesis and pharmacological activity of triazolo[1,5-a]triazine derivatives inhibiting eosinophilia
文献作者:Akahoshi,F.; Takeda,S.; Okada,T.; Kajii,M.; Nishimura,H.; Sugiura,M.; Inoue,Y.; Fukaya,C.; Naito,Y.; Imagawa,T.; Nakamura,N.
参考来源:J Med Chem 1998,41(16),2985-2993


产品链接: CAS No. 168893-29-6››