CAS: 18184-75-3; 6-Benzyl-5,7-Dihydro-5,7-Dioxopyrrolo[3,4-B]Pyridine

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2-(甲氧基羰基)烟酸置于氯化亚砜,三乙胺体系中,化学反应 3.0H,反应生成6-苄基-6H-吡咯[3,4-B]吡啶-5,7-二酮
参考文献:Van Es,Theodorus; Staskun,Benjamin; Karuso,Peter,South African Journal Of Chemistry,2012,Vol. 65,P. 53-61
标题:Van Es,Theodorus; Staskun,Benjamin; Karuso,Peter,South African Journal Of Chemistry,2012,Vol. 65,P. 53-61

专利信息

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%.