N-0861
Chemical Name: (?-N6-(endo-2-Norbornyl)-9-methyladenine; (?-N6-(Bicyclo[2.2.1]hept-2-yl)-9-methyladenine; (?-endo-N-(Bicyclo[2.2.1]hept-2-yl)-9-methyl-9H-purin-6-amine
CAS No. 121252-55-9, 121241-87-0 (undefined isomer)
项目整合开发状态: Phase III
项目研究机构: Aderis (Originator)
合成路线:The overall synthetic approach to N-0861 is described in Scheme 17807901a:Reduction of 4,6-dichloro-5-nitropyrimidine (I) followed by reaction with methylamine gives 5-amino-6-chloro-4-methylaminopyrimidine (III).Cyclization with triethylorthoformate under acidic conditions results in 9-methyl-6-chloropurine (IV).Reaction of (?-endo-2-aminonorbornane (V) with 9-methyl-6-chloropurine (IV) provides N-0861.
📌 参考资料/链接：
参考文献标题:N-0861
文献作者:Peck,J.V.; Cusack,N.J.
参考来源:Drugs Fut 1993,18(5),433
📄 详细内容
合成路线:The overall synthetic approach to N-0861 is described in Scheme 17807901a:Reduction of 4,6-dichloro-5-nitropyrimidine (I) followed by reaction with methylamine gives 5-amino-6-chloro-4-methylaminopyrimidine (III).Cyclization with triethylorthoformate under acidic conditions results in 9-methyl-6-chloropurine (IV).Reaction of (?-endo-2-aminonorbornane (V) with 9-methyl-6-chloropurine (IV) provides N-0861.
参考文献标题:Non-xanthine heterocycles: Activity as antagonists of A1- and A2-adenosine receptors
文献作者:Daly,J.; Hong,O.; Padgett,W.; Shamim,M.; Jacobson,K.; Ukena,D.
参考来源:Biochem Pharmacol 1988,37(4),655-54
合成路线:The overall synthetic approach to N-0861 is described in Scheme 17807901a:Reduction of 4,6-dichloro-5-nitropyrimidine (I) followed by reaction with methylamine gives 5-amino-6-chloro-4-methylaminopyrimidine (III).Cyclization with triethylorthoformate under acidic conditions results in 9-methyl-6-chloropurine (IV).Reaction of (?-endo-2-aminonorbornane (V) with 9-methyl-6-chloropurine (IV) provides N-0861.
参考文献标题:Adenosine receptors: Pharmacology,structure-activity relationships,and therapeutic potential
文献作者:Jacobson,K.; van Galen,P.; Williams,M.
参考来源:J Med Chem 1992,35(3),407-22
产品链接: CAS No. 121252-55-9›› 产品链接: CAS No.121241-87-0››