CAS: 119835-88-0; (S)-2-(2,3-Dihydroxypropyl)Isoindoline-1,3-Dione

该化合物是具有异硫醇结构,具有由五人环组成的双环环,引信至六人环的双环系统,该化合物包含二元功能组,表明存在两个碳基(C=O)组,有助于其再活动及潜在的生物活动.替代体表2[2S)-2,3-二氧丙基 表明它有一个手性中心,它可能影响它与生物系统的互动,使其对医药化学感兴趣.氢氧基组的存在表明氢结合的潜力,提高极溶剂的溶性,并可能影响其药用动力特性.

结构式图片

上下游产品

S-(-)-4-Phthalimidomethyl-2,2-Dimethyl-1,3-Dioxolane 40137-25-5
邻苯二甲酸亚胺 Phthalimide 85-41-6

合成工艺路线路线简述

  • 合成目标产物 1H-Isoindole-1,3(2H)-Dione, 2-[(2S)-2,3-Dihydroxypropyl]- 主要起始原料 1H-Isoindol-1-One, 3-Hydroxy- And (R)-(-)-3-Chloro-1,2-Propanediol
  • (文献来源)合成步骤主要原料 1H-Isoindol-1-One, 3-Hydroxy- 和 (R)-(-)-3-Chloro-1,2-Propanediol
📜S-(-)-4-Phthalimidomethyl-2,2-Dimethyl-1,3-Dioxolane置于盐酸体系中,用 水 用作溶剂,化学反应 2.0H,以55.3 Kg的收率获得利伐沙班杂质151
参考文献:Pilot Scale Process Development Of Sl65.0102-10,An N-Diazabicyclo[2.2.2]-octylmethyl Benzamide
标题:Pilot Scale Process Development Of Sl65.0102-10,An N-Diazabicyclo[2.2.2]-octylmethyl Benzamide
摘要:The Process Development And Improvements For Route Selection,Adapted To Large Scale For The Pilot-Scale Preparation Of Sl65.0102-10,An N-Diazabicyclo[2.2.2]-octylmethyl Benzamide,A 5-Ht3 And 5-Ht4 Receptor Active Ligand For The Treatment Of Neurological Disorders Such As Cognition Impairment,Are Described In This Article. Notable Steps And Enhancements Are Compared To The Original Route,Including The Improvement Of A Chiral Epoxide Synthesis By Shortening The Number Of Chemical Steps,The Deprotection Of A Quaternary Ammonium Salt,And The Redesign Of The Final Amidification Coupling To Avoid Chromatography.
Doi:10.1021/acs.Oprd.6B00262

海关参考信息

专利信息


专利号:WO-2006031179-A1
优先权日:2004-09-13
标 题:Process for preparation of phtalimide
发明人:KRIG ANN-SOFIE; THELIN MATS
权利人:ASTRAZENECA AB; KRIG ANN-SOFIE; THELIN MATS
摘要:The present invention is directed to a novel process for the synthesis of (S) -glycidyl phthalimide and to novel intermediates in the process. The process comprises, reacting a (R) -3 -Chloro-1,2-propanediol and phtalimide salt. Then reacting the product with trimethylorthoacetate and an essentially water free acid. Then reacting the product with acetyl halogenide and do a basic ester hydrolysis.

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✅ COA系统入驻 | 共享模式

主要参考文献

参考标题: Process For Preparation Of Phtalimide Processus De Preparation De Phtalimide
摘要:The Present Invention Is Directed To A Novel Process For The Synthesis Of (S) -Glycidyl Phthalimide And To Novel Intermediates In The Process. The Process Comprises, Reacting A (R) -3 -Chloro-1,2-Propanediol And Phtalimide Salt. Then Reacting The Product With Trimethylorthoacetate And An Essentially Water Free Acid. Then Reacting The Product With Acetyl Halogenide And Do A Basic Ester Hydrolysis.
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