CAS: 128740-14-7; 6-Benzyl-Octahydropyrrolo[3,4-B]Pyridine

相似化合物

151213-39-7 1196146-96-9 2102950-42-3

上下游产品

(R,R)-8-benzyl-2,8-diazabicyclo[4.3.0]nonane L-(+)-tartrate salt sodium hydroxide 8-benzyl-2,8-diazabicyclo[4.3.0]nonane (S,S)-8-benzyl-2,8-diazabicyclo[4.3.0]nonane-D-tartrate [R,R]-2,8-diazabicyclo[4.3.0]nonane [R,R]-8-benzyl-2,8-diazabicyclo[4.3.0]nonane (1S,6S)-2,8-diazabicyclo[4.3.0]nonane moxifloxacin

📜2,3-吡啶二酰亚胺置于5%-Palladium/activated Carbon,三乙胺体系中,用 四氢呋喃,N,N-二甲基甲酰胺 用作溶剂,化学反应 20.0H,反应生成苄基-11氢吡咯并[3,4-B]吡啶
参考文献:(S,S)-2,8-二氮杂双环[4.3.0]壬烷的制备方 法
标题:(S,S)-2,8-二氮杂双环[4.3.0]壬烷的制备方 法
摘要:本发明涉及一种(S,S)-2,8-二氮杂双环[4.3.0]壬烷的制备新方法,包括:2,3-吡啶二甲酸衍生物与氨基化物缩合生成2,3-吡啶二甲酰亚胺;经保护和氢化还原后制成8-取代-7,9-二氧代-2,8-二氮杂双环[4.3.0]壬烷;在硼氢化物还原体系中还原后得到8-取代2,8-二氮杂双环[4.3.0]壬烷,经光活性有机酸拆分,脱除8位保护基后得到最终产品;或2,3-吡啶二甲酰亚胺直接氢化还原得到7,9-二氧代-2,8-二氮杂双环[4.3.0]壬烷,在硼氢化物还原体系中直接还原为2,8-二氮杂双环[4.3.0]壬烷;2,8-二氮杂双环[4.3.0]壬烷经光活性有机酸拆分直接得到产品.本发明方法反应路线简单,原料价廉易得,反应条件温和易控制,适合工业化生产.

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