CAS: 1198-97-6; 4-Phenyl-2-Pyrrolidone

该化合物是一种多功能性热循环化合物,在4点位置用苯基组取代了丙烯基酮核心,这种结构具有独特的反应性和功能性群体兼容性,使其作为制药和农用化学合成的中间体具有价值.它的晶体元素提供了进一步衍生的场所,有助于构建复杂的分子框架.该化合物的稳定性和定义明确的立体化学加强了其在非对称合成和药用化学应用中的效用.此外,其芳香苯基在目标互动中有助于有利的溶性与结合性. 4-Phenylpillololin-2-one由于其平衡的脂性性和结构僵硬性,在生物活性分子(包括CNS目标物剂)的开发中特别有用.

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CAS号34687-03-1 β-(硝基甲基)苯丙酸甲酯 | CAS号866789-27-7 (+/-)-4-nitro-3... | CAS号103-26-4 肉桂酸甲酯 | CAS号14025-83-3 3-cyano-3-pheny... | CAS号41441-40-1 ethyl 4-nitro-3... | CAS号5292-53-5 苯亚甲基丙二酸二乙酯 | CAS号77519-55-2 2-氧代-4-苯吡咯烷-3-羧酸 | CAS号52450-32-5 2-氧代-4-苯基吡咯烷-3-甲酸乙酯 | CAS号98-80-6 苯硼酸 | CAS号103-36-6 肉桂酸乙酯 | CAS号1078-21-3 非尼布特 | CAS号22349-30-0 3-phenyl-3,4-di... | CAS号3060-41-1 3-苯基-4-氨基丁酸盐酸盐 | CAS号77472-70-9 卡非多 | CAS号67118-34-7 (2-氧代-4-苯基吡咯烷-1-基)乙酸 | CAS号70291-40-6 2-Oxo-4-phenyl-... | CAS号76696-74-7 3H-Pyrrolo(1,2-... | CAS号76696-77-0 2,5,6,7-Tetrahy... | CAS号76696-79-2 2,5,6,7-Tetrahy... | CAS号76696-81-6 2,5,6,7-Tetrahy...

合成工艺路线路线简述

    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

    海关参考信息

    专利信息


    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
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    合成参考文献


    摘要:Simon, R. C.; Busto, E.; Fischereder, E.-M.; Fuchs, C. S.; Pressnitz, D.; Richter, N.; Kroutil, W., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 410.
    摘要:Archivum Immunologiae et Therapiae Experimentalis., 23(733), 1975 []
    摘要:Russian Pharmacology and Toxicology, 44(22), 1981
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