CAS: 151213-39-7; (4As,7As)-6-Benzyloctahydro-1H-Pyrrolo[3,4-B]Pyridine

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上下游产品

(S,S)-8-benzyl-2,8-diazabicyclo[4.3.0]nonane-D-tartrate [1S,6R]-8-benzyl-7,9-dioxo-2,8-diazabicyclo[4.3.0]nonane (S,S)-8-benzyl-2,8-diazabicyclo[4.3.0]nonane tartrate salt (1S,6S)-2,8-diazabicyclo[4.3.0]nonane

📜(3S)-1-Benzyl-3-Amino-4-(3-Chloropropyl)Pyrrolidine置于potassium Tert-Butylate,四丁基碘化铵体系中,用 四氢呋喃 用作溶剂,化学反应 1.0H,以92.5%的收率获得(S,S)-6-苄基-八氢吡咯并[3,4-B]吡啶双盐酸盐
参考文献:一种3-氨基吡咯烷化合物及其合成方法和用 途
标题:一种3-氨基吡咯烷化合物及其合成方法和用 途
摘要:本发明涉及一种3‑氨基吡咯烷化合物及其合成方法和用途,是以3‑ 吡咯烷酮化合物( 化合物iiia或iiib)为底物,在转氨酶和氨基供体的作用下,发生转氨酶反应得到(S)－3－氨基吡咯烷化合物(化合物ii);再发生分子内关环,脱除氨基保护基得到(S,S)‑2,8‑二氮杂双环[4,3,0]壬烷(化合物i).本发明为莫西沙星中间体提供了一种成本低,工艺流程短,对环境友好的合成技术,将具有巨大的市场应用价值,适合大规模工业化生产.

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:CN-115073452-A
优先权日:2022-06-11
标 题:A method for continuous synthesis of moxifloxacin side chain intermediates by heterogeneous hydrogenation in a microreactor

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