亚苯甲基丙二酸二乙酯置于palladium On Activated Charcoal 盐酸,氢气,三乙胺体系中,用 甲醇,水,甲苯 用作溶剂,60.0 °C,275.79 Kpa 条件下,反应生成4-苯基-2-吡咯烷酮 参考文献:Inhibition Of Cyclic Adenosine-3',5'-Monophosphate Phosphodiesterase From Vascular Smooth Muscle By Rolipram Analogs 标题:Inhibition Of Cyclic Adenosine-3',5'-Monophosphate Phosphodiesterase From Vascular Smooth Muscle By Rolipram Analogs 摘要:Rolipram [(R,S)-4-[3-(Cyclopentyloxy)-4-Methoxyphenyl]-2-Pyrrolidone] Has Been Shown To Inhibit Selectively The Camp Phosphodiesterase (Pde) Of Vascular Smooth Muscle. In Order To Further Explore The Structural Requirements For Selective Pde Inhibition,We Synthesized A Series Of Rolipram Derivatives Differently Substituted Either At The Pyrrolidinone Or At The Aromatic Ring. Among These Compounds,Rolipram Was The Most Active Compound. Semirigid Analogues Were Prepared And Used For An Evaluation Of The Active Conformation Of Rolipram. Structural Comparison With Two Other Potent And Chemically Different Smooth Muscle Camp-Pde Inhibitors,Trequinsin And Ro 20-1724,Allows Us To Propose A First Topological Model Of The Smooth Muscle Camp-Pde Pharmacophore. Doi:10.1021/jm00127A009
专利号:WO-2016075082-A1 优先权日:2014-11-10 标题:Stereoselective reductive amination of alpha-chiral aldehydes using omega-transaminases for the synthesis of precursors of pregabalin and brivaracetam 发明人:ZEPECK FERDINAND; NERDINGER SVEN; KROUTIL WOLFGANG; FUCHS CHRISTINE; SIMON ROBERT 权利人:SANDOZ AG 摘要:The present invention relates to processes comprising a combined racemization and stereoselective reductive amination step in which an aldehyde compound of formula (I) is contacted with an (R)-selective ω-transaminase or an (S)-selective ω-transaminase to racemize the compound of formula (I) and obtain an amine compound of formula (II). These processes are useful for the preparation of precursors of pharmaceutically active agents such as brivaracetam and pregabalin.
专利号:US-5021568-A 优先权日:1988-04-22 标题:Lactam-1-acetic acid carbalkoxymethyl esters and method for preparing same 发明人:SHIPOV ALEXANDR G; KRAMAROVA EVGENIA P; ORLOVA NATALIA A; BAUKOV JURY I; ZIEMELIS KRISTAP M 权利人:SHIPOV ALEXANDR G; KRAMAROVA EVGENIA P; ORLOVA NATALIA A; BAUKOV JURY I; ZIEMELIS KRISTAP M 摘要:The present invention relates to organic chemistry. Lactam-1-acetic acid carbalkoxymethyl esters have the following general formula: ##STR1## wherein with R=H, n=1 or 3; with R=phenyl, n=1; R 1 is an alkyl. A method for preparing said compounds comprises reacting lactams of the general formula: ##STR2## wherein with R=H, n=1 or 3, with R=phenyl n=1, with an alkali in a medium of aprotic solvents at a temperature of from 70° to 130° C., followed by the addition of an alkyl ester of a monohalcacetic acid to the resulting mixture and isolation of the desired product. n The compounds according to the present invention are intermediate products in the synthesis of known biologically active substances.
专利号:RU-2711655-C1 优先权日:2019-09-13 标题 :Method for large-scale synthesis of potassium salt of 2-[2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamido]ethane sulphonic acid