Diethyl N--L-Glutamate置于palladium On Activated Charcoal 盐酸,氢气体系中,用 乙醇 用作溶剂,化学反应 3.0H,以80%的收率获得对甲胺基苯甲酰谷氨酸二乙酯 参考文献:A Pyrimidine-Based "Flexible" Bisubstrate Analog Inhibitor Of Human Thymidylate Synthase 标题:A Pyrimidine-Based "Flexible" Bisubstrate Analog Inhibitor Of Human Thymidylate Synthase 摘要:The Synthesis And Characterization Of Two "Flexible" Bisubstrate Analogues Of The Intermediate In The Thymidylate Synthase Reaction Are Reported. Steric Constraints Are Minimized And Diasteromeric Mixtures Avoided By Using A Pyrimidine-Based Analogue As The Folate Portion Of The Inhibitor While Retaining All Known Important Binding Sites. A Preliminary Assessment Of Certain Conformational Parameters By NMR Is Presented. The Compounds Are Shown To Be Potent Competitive Inhibitors With Respect To Dump Or 5,10-Ch2-H4Pteglu But Gave Mixed Kinetics With Respect To 5,10-Ch2-H4Pteglu5 For Human Thymidylate Synthase. Doi:10.1021/jm00119A012
专利号:US-4136101-A 优先权日:1978-02-03 标题:Process for preparing dialkyl (p-aminobenzoyl) glutamates 发明人:KAZAN JOHN 权利人:AMERICAN CYANAMID CO 摘要:A process for the preparation of dialkyl (p-aminobenzoyl) glutamates is disclosed. Dialkyl (p-Aminobenzoyl) glutamates are useful as intermediates in the synthesis of N-{p-([(2,4-diamino-6-pteridinyl)-methyl]methylamino)benzoyl} glutamic acid, also known as 4-amino-N 10 -methylpteroylglutamic acid. The compound zinc N-(p-methylaminobenzoyl)-L-(+)-glutamate, is also disclosed.
参考标题:Quinazoline Antifolate Thymidylate Synthase Inhibitors: Alkyl, Substituted Alkyl, And Aryl Substituents In The C-2 Position 作者:Leslie R. Hughes,Ann L. Jackman,John Oldfield,Rodney C. Smith,Kenneth D. Burrows,Peter R. Marsham,Joel A. M. Bishop,Terence R. Jones,Brigid M. O'Connor,A. Hilary Calvert |发布日期:1990.11 摘要:Thymidylate Synthase (Ts) Inhibitor N-[4-[n-[(2-Amino-3,4-Dihydro-4-Oxo-6-Quinazolinyl)Methyl]-N-Prop-2- Ynylamino]Benzoyl]-L-Glutamic Acid (1A) Has Led To The Synthesis Of Quinazoline Antifolates Bearing Alkyl, Substituted Alkyl, And Aryl Substituents At C2. In General The Synthetic Route Involved The Coupling Of The Appropriate Diethyl N-[4-(Alkylamino)Benzoyl]-L-Glutamate With A C2-Substituted 6-(Bromo-Methyl)-3