📜Pteroyl Azide置于盐酸,1,1,2,3-四甲基胍体系中,用 四氢呋喃,二甲基亚砜 作为反应溶剂,化学反应 22.5H,反应生成 N10-三氟乙酰基蝶酸
参考文献:Efficient Syntheses Of Pyrofolic Acid And Pteroyl Azide,Reagents For The Production Of Carboxyl-Differentiated Derivatives Of Folic Acid
标题:Efficient Syntheses Of Pyrofolic Acid And Pteroyl Azide,Reagents For The Production Of Carboxyl-Differentiated Derivatives Of Folic Acid
摘要:Reaction Of Folic Acid (1) With Excess Trifluoroacetic Anhydride Provides Access To Both The Previously Unknown N-10-(Trifluoroacetyl)Pyrofolic Acid (8) And Pyrofolic Acid (9). Reaction Of Either Of These Materials With Hydrazine Selectively Affords Pteroyl Hydrazide (13),Which May Be Oxidized To Pteroyl Azide (27) On A Large Scale (62% Overall From 1 Without The Need For Chromatography). Treatment Of 27 With Differentially Protected Glutamates Provides A Convenient And High-Yielding Synthesis Of Differentially Protected,Optically Pure Folates.
DOI:10.1021/ja971568J