CGP-28014
N-(2-吡啶酮-6-基)-N',N'-二-N-丙基甲脒Chemical Name: N-(6-Oxo-1,6-dihydro-2-pyridyl)-N',N'-dipropylformamidine; N-(2-Hydroxy-6-pyridyl)-N',N'-dipropylformamidine; N-(6-Hydroxy-2-pyridyl)-N',N'-dipropylformamidine; N'-(1,6-Dihydro-6-oxo-2-pyridinyl)-N,N-dipropylmethanimidamide
CAS No. 111757-17-6
项目整合开发状态: Phase II
项目研究机构: Novartis (Originator)
合成路线:The hydrolysis of 2,6-diaminopyridine (I) in 36% aqueous hydrochloric acid leads to 2-amino-6-hydroxypyridine (II),which can be converted by several ways to the final product CGP 28014.Two are described here:a) Conversion of 2-amino-6-hydroxypyridine (II) with N,N-dimethylformamide diethylacetal gives the N-(2-oxopyridin-6-yl)-N',N'-dimethylformamidine (IV),which is transaminated with dipropylamine to CGP 28014.b) Reaction of 2-amino-6-hydroxypyridine (II) with ethyl-N-cyanoformimidate (2) yields N-(2-oxopyridin-6-yl)-N'-cyanoformamidine (III),which is heated with dipropylamine to give CGP 28014.
📌 参考资料/链接：
参考文献标题:Pyridine derivs
文献作者:Von Sprecher,G.; Waldmeier,P.(Novartis AG)
参考来源:EP 0239533; JP 1987226959; US 4683938
📄 详细内容
合成路线:The hydrolysis of 2,6-diaminopyridine (I) in 36% aqueous hydrochloric acid leads to 2-amino-6-hydroxypyridine (II),which can be converted by several ways to the final product CGP 28014.Two are described here:a) Conversion of 2-amino-6-hydroxypyridine (II) with N,N-dimethylformamide diethylacetal gives the N-(2-oxopyridin-6-yl)-N',N'-dimethylformamidine (IV),which is transaminated with dipropylamine to CGP 28014.b) Reaction of 2-amino-6-hydroxypyridine (II) with ethyl-N-cyanoformimidate (2) yields N-(2-oxopyridin-6-yl)-N'-cyanoformamidine (III),which is heated with dipropylamine to give CGP 28014.
参考文献标题:CGP 28014
文献作者:M鯾ius,H.J.; Waldmeier,P.C.; Von Sprecher,G.
参考来源:Drugs Fut 1992,17(4),275
合成路线:The hydrolysis of 2,6-diaminopyridine (I) in 36% aqueous hydrochloric acid leads to 2-amino-6-hydroxypyridine (II),which can be converted by several ways to the final product CGP 28014.Two are described here:a) Conversion of 2-amino-6-hydroxypyridine (II) with N,N-dimethylformamide diethylacetal gives the N-(2-oxopyridin-6-yl)-N',N'-dimethylformamidine (IV),which is transaminated with dipropylamine to CGP 28014.b) Reaction of 2-amino-6-hydroxypyridine (II) with ethyl-N-cyanoformimidate (2) yields N-(2-oxopyridin-6-yl)-N'-cyanoformamidine (III),which is heated with dipropylamine to give CGP 28014.
参考文献标题:A new convenient synthesis of H2-aryl-H1-alkylformamidines and N2-aryl-N1,N1-dialkylformamidines
文献作者:Donetti,A.; Bellora,E.; Cereda,E.
参考来源:Synthesis 1986,288-91
产品链接: CAS No. 111757-17-6››