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Pyraoncozine, NSC-D-364834, C-8412843, NSC-364834-D

3-(2-氯乙基)-3,4-二氢-4-氧代吡唑并[5,1-d]-1,2,3,5-四嗪-8-甲酰胺Chemical Name: 3-(2-Chloroethyl)-3,4-dihydro-4-oxopyrazolo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide
CAS No. 90521-23-6
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:The pyrazolo[5,1-d]-1,2,3,5-tetrazine ring is synthesized according to the general method of Ege and Gilbert by the condensation of 3-diazopyrazole-4-carboxamide (I) with 2-chloroethyl isocyanate (II) in ethyl acetate at room temperature,followed by heating the reaction mixture at 50-60 C.The product may be purified through a silica gel column using ethyl acetate as the eluent.In contrast to the preparation of mitozolomide,the entire operation,including the preparation of the starting 3-diazo derivative,can be conducted under ordinary laboratory illumination.The dry product is stable under light even after 6 months.
📌 参考资料/链接:
参考文献标题:3-(Haloethyl)-4-oxopyrazolo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide compounds
文献作者:Cheng,C.C.(Pfizer Inc.)
参考来源:JP 60011489; US 4504475

📄 详细内容


合成路线:The pyrazolo[5,1-d]-1,2,3,5-tetrazine ring is synthesized according to the general method of Ege and Gilbert by the condensation of 3-diazopyrazole-4-carboxamide (I) with 2-chloroethyl isocyanate (II) in ethyl acetate at room temperature,followed by heating the reaction mixture at 50-60 C.The product may be purified through a silica gel column using ethyl acetate as the eluent.In contrast to the preparation of mitozolomide,the entire operation,including the preparation of the starting 3-diazo derivative,can be conducted under ordinary laboratory illumination.The dry product is stable under light even after 6 months.

参考文献标题:Pyraoncozine
文献作者:Zee-Cheng,R.K.-Y.; Cheng,C.C.
参考来源:Drugs Fut 1986,11(2),121


合成路线:The pyrazolo[5,1-d]-1,2,3,5-tetrazine ring is synthesized according to the general method of Ege and Gilbert by the condensation of 3-diazopyrazole-4-carboxamide (I) with 2-chloroethyl isocyanate (II) in ethyl acetate at room temperature,followed by heating the reaction mixture at 50-60 C.The product may be purified through a silica gel column using ethyl acetate as the eluent.In contrast to the preparation of mitozolomide,the entire operation,including the preparation of the starting 3-diazo derivative,can be conducted under ordinary laboratory illumination.The dry product is stable under light even after 6 months.

参考文献标题:
文献作者:Roberts,M.S.; Smith,K.J.
参考来源:Tetrahedron Lett 1979,113(4),4235-4256


合成路线:The pyrazolo[5,1-d]-1,2,3,5-tetrazine ring is synthesized according to the general method of Ege and Gilbert by the condensation of 3-diazopyrazole-4-carboxamide (I) with 2-chloroethyl isocyanate (II) in ethyl acetate at room temperature,followed by heating the reaction mixture at 50-60 C.The product may be purified through a silica gel column using ethyl acetate as the eluent.In contrast to the preparation of mitozolomide,the entire operation,including the preparation of the starting 3-diazo derivative,can be conducted under ordinary laboratory illumination.The dry product is stable under light even after 6 months.
参考文献标题:
文献作者:Zolopa,A.R.; Whitcomb,J.M.; Hughes,M.D.; Katzenstein,D.A.; Winters,M.S.; Shafer,R.W.; Bates,M.; Shulman,N.S.; Hellmann,N.S.
参考来源:J Pharm Sci 1968,57(2),1044-1045


产品链接: CAS No. 90521-23-6››