NSC-350386(hydrochloride hydrate), NSC-370147
N-(5-氨基-9-甲基-8-苯基-4,7,10-三氮杂双环[4.4.0]十-1,3,5,7-四烯-3-基)氨基甲酸乙酯Chemical Name: 5-Amino-1,2-dihydro-2-methyl-3-phenylpyrido[3,4-b]pyrazin-7-ylcarbamic acid ethyl ester 2-hydroxyethylsulfonate hydrate
CAS No. 83269-10-7 (free base)
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator), Southern Research Institute (Originator)
合成路线:A number of 1-deaza-7,8-dihydropteridines with antimitotic activity have been prepared by the route shown in the scheme for NSC-350386 (1,2).Reaction of 2-aminopropiophenone oxime with ethyl 6-amino-4-chloro-5-nitropyridin-2-ylcarbamate (I) gave (II),which was hydrolyzed in a mixture of dioxane and hydrochloric acid to give the ketone (III).Reductive cyclization of (III) was effected with Raney Nickel and hydrogen.
📌 参考资料/链接：
参考文献标题:1,2-Dihydropyrido[3,4-b]pyrazines: Structure-activity relationships
文献作者:Temple,C.Jr.; et al.
参考来源:J Med Chem 1983,26(1),91
📄 详细内容
合成路线:A number of 1-deaza-7,8-dihydropteridines with antimitotic activity have been prepared by the route shown in the scheme for NSC-350386 (1,2).Reaction of 2-aminopropiophenone oxime with ethyl 6-amino-4-chloro-5-nitropyridin-2-ylcarbamate (I) gave (II),which was hydrolyzed in a mixture of dioxane and hydrochloric acid to give the ketone (III).Reductive cyclization of (III) was effected with Raney Nickel and hydrogen.
参考文献标题:New anticancer agents agents: Synthesis of 1,2-dihydropyrido[3,4-b]pyrazines (1-deaza-7,8-dihydropteridines)
文献作者:Temple,C.Jr.; Wheeler,G.P.; Elliot,R.D.; Rose,J.D.; Kussner,C.L.; Comber,R.N.; Montgomery,J.A.
参考来源:J Med Chem 1982,25(9),1045
合成路线:A number of 1-deaza-7,8-dihydropteridines with antimitotic activity have been prepared by the route shown in the scheme for NSC-350386 (1,2).Reaction of 2-aminopropiophenone oxime with ethyl 6-amino-4-chloro-5-nitropyridin-2-ylcarbamate (I) gave (II),which was hydrolyzed in a mixture of dioxane and hydrochloric acid to give the ketone (III).Reductive cyclization of (III) was effected with Raney Nickel and hydrogen.
参考文献标题:NSC-350386
文献作者:Wheeler,G.P.; Temple,C.Jr.
参考来源:Drugs Fut 1983,8(11),927
产品链接: CAS No. 83269-10-7››