📜四氢吡喃酮置于5%-Palladium/activated Carbon,氢气,Potassium Carbonate,三乙胺体系中,用 甲醇,N,N-二甲基甲酰胺 用作溶剂,60.0 °C,500.01 Kpa 条件下,反应 6.0H,反应生成N-甲基四氢-2H-吡喃-4-胺
参考文献:Process Development Of 4-[n-Methyl-N-(Tetrahydropyran-4-yl)Aminomethyl]Aniline Dihydrochloride: A Key Intermediate For Tak-779,A Small-Molecule Nonpeptide Ccr5 Antagonist
标题:Process Development Of 4-[n-Methyl-N-(Tetrahydropyran-4-yl)Aminomethyl]Aniline Dihydrochloride: A Key Intermediate For Tak-779,A Small-Molecule Nonpeptide Ccr5 Antagonist
摘要:A New And Efficient Synthesis Of 4-[n-Methyl-N-(Tetrahydropyran-4-yl)Aminomethyl]Aniline Dihydrochloride,A Key Intermediate For The Ccr5 Antagonist Tak-779,Is Described. Reductive Alkylation Of Methylamine With Tetrahydro-4H-Pyran-4-One Followed By Alkylation Of N-Methyl-N-(Tetrahydropyran-4-yl)Amine With 4-Nitrobenzylbromide And Reduction Of N-(4-Nitrobenzyl)-N-(Tetrahydropyran-4-yl)Amine Results In A 78% Isolated Yield From The Starting Materials By A Scalable Method,Using Only Commercially Available Reagents.
Doi:10.1021/op010052O