CAS: 128740-13-6; 6-Benzylhexahydro-5H-Pyrrolo[3,4-B]Pyridine-5,7(6H)-Dione

该化合物是一种化学化合物,其特点是复杂的双环结构,其中包括一个环虫球框架;该化合物具有四氢结构,表明存在饱和环系统,并含有一个有助于其芳香特性的苯甲基组;结构中存在两个碳基(二)组),表明它具有潜在的再活动性能和参加各种化学反应的能力,例如核生殖添加或凝聚反应;该化合物的独特结构可能带来具体的生物活动,使其对药用化学和药物开发具有兴趣;该化合物的溶性,稳定性和再活性可因环境条件和功能组的存在而变化;

结构式图片

相似化合物

1214169-98-8 151213-41-1 161594-55-4

上下游产品

(1R,6S)-8-Benzyl-7,9-Dioxo-2,8-Diazabicyclo[4.3.0]Nonane 151213-44-4

合成工艺路线路线简述

    📜2,3-吡啶二酰亚胺置于palladium 10% On Activated Carbon,氢气体系中,化学反应 8.5H,反应生成6-苄基-5,7-二氧代-八氢吡咯并[3,4B]吡啶
    参考文献:氢硅烷对锌催化的环状酰亚胺的选择性还原:ω-羟基内酰胺的合成
    标题:氢硅烷对锌催化的环状酰亚胺的选择性还原:ω-羟基内酰胺的合成
    摘要:环状酰亚胺进行选择性地还原成高产量与相应的ω-Hydroxylactams(eto)3的sih(三乙氧基硅烷)或下的催化pmhs(聚甲基)二乙酸锌水合物[锌(oac)2 ⋅2ħ 2 O](10%)和四甲基乙二胺(tmeda)(10%).该催化方案对带有邻近羰基的配位基团的不对称酰亚胺显示出非常好的官能团耐受性和优异的区域选择性.
    Doi:10.1002/adsc.201400961

    海关参考信息

    专利信息


    专利号:US-8680276-B2
    优先权日:2009-03-06
    标题 :Synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine
    发明人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO
    权利人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO
    摘要:The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.

    专利号:WO-2012131629-A1
    优先权日:2011-03-31
    标题 :A process for preparation of intermediate of moxifloxacin
    发明人:WANKHEDE KARUNA; JAGTAP ASHUTOSH; ROY MITA; HARIHARAN SIVARAMAKRISHNAN; KUMBHAR AJAY
    权利人:PIRAMAL HEALTHCARE LTD; WANKHEDE KARUNA; JAGTAP ASHUTOSH; ROY MITA; HARIHARAN SIVARAMAKRISHNAN; KUMBHAR AJAY
    摘要:The present invention provides a process for the preparation of racemic or chiral octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine of formula I, a key intermediate in the synthesis of moxifloxacin or its pharmaceutically acceptable salts. The process comprises reaction of racemic or chiral tetrahydro-6-(phenylmethyl)-1H- pyrrolo[3,4-b]pyridine-5,7(6H)-dione of formula II with a reducing agent, which is a mixture of two agents, that is mixture of dimethyl sulphate and sodium borohydride or aluminum chloride and sodium borohydride used in a molar ratio ranging from 1:1 to 1: 4, in the presence of a polar solvent at a temperature ranging from 15°C to 45°C 10 to obtain racemic or chiral octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine of formula I having purity ≥ 96%.

    专利号:US-2011137036-A1
    优先权日:2009-03-06
    标题 :SYNTHESIS OF (4aS,7aS)-OCTAHYDRO-1H-PYRROLO[3,4-b]PYRIDINE

    专利号:WO-2010100215-A1
    优先权日:2009-03-06
    标题:SYNTHESIS OF (4aS,7aS)-OCTAHYDRO-1H-PYRROLO[3,4-b]PYRIDINE

    专利号:EP-2403831-B1
    优先权日:2009-03-06
    标题 :SYNTHESIS OF (4aS,7aS)-OCTAHYDRO-1H-PYRROLOÃ?3,4-b¨PYRIDINE

    专利号:EP-2403831-A1
    优先权日:2009-03-06
    标 题 :SYNTHESIS OF (4aS,7aS)-OCTAHYDRO-1H-PYRROLOÃ?3,4-b¨PYRIDINE

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