发明授权
US07449583B2 Process for the preparation of 4-(8-chloro-5 6-dihydro-11h-benzo-(5 6)-cyclohepta-(1 2b)-pyridin-11-ylidene-1-piperidiniecarboxylic acid ethyl ester (loratadine)
失效
制备4-(8-氯-5,6-二氢-11h - 苯并 - (5,6) - 环庚烷 - (1 2b) - 吡啶-11-亚基-1-哌啶甲酸乙酯(氯雷他定)的方法,
- 专利标题: Process for the preparation of 4-(8-chloro-5 6-dihydro-11h-benzo-(5 6)-cyclohepta-(1 2b)-pyridin-11-ylidene-1-piperidiniecarboxylic acid ethyl ester (loratadine)
- 专利标题(中): 制备4-(8-氯-5,6-二氢-11h - 苯并 - (5,6) - 环庚烷 - (1 2b) - 吡啶-11-亚基-1-哌啶甲酸乙酯(氯雷他定)的方法,
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申请号: US10493314申请日: 2002-10-29
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公开(公告)号: US07449583B2公开(公告)日: 2008-11-11
- 发明人: Vincenzo Cannata , Livius Cotarca , Ivan Michieletto , Stefano Poli
- 申请人: Vincenzo Cannata , Livius Cotarca , Ivan Michieletto , Stefano Poli
- 申请人地址: IT Bresso
- 专利权人: ZaCh System S.p.A.
- 当前专利权人: ZaCh System S.p.A.
- 当前专利权人地址: IT Bresso
- 代理机构: Oblon, Spivak, McClelland, Maier & Neustadt, P.C.
- 优先权: ITMI2001A2308 20011105
- 国际申请: PCT/EP02/12056 WO 20021029
- 国际公布: WO03/040140 WO 20030515
- 主分类号: C07D413/04
- IPC分类号: C07D413/04
摘要:
A process and new oxazolinic intermediates for the preparation of 4-(8-chloro-5,6-dihydro-11H-benzo-[5,6]-cyclohepta-[1,2-b]-pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester (loratadine) is described. The process starts from 2-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)-3-methyl-pyridine, a new intermediate to obtain loratadine. 2-(4,4-dimethyl-4, 5-dihydrooxazol-2-yl)-3-methyl-pyridine is condensed with 3-chloro-benzyl-chloride and the resultant product is treated with Grignard reagent of 4-chloro-N-methyl-piperidine. [3-(2-(3-chloro-phenyl)-ethyl]-pyridin-2-yl]-1-(methyl-piperidin-4-yl)-methanone is obtained for subsequent hydrolysis. Starting from this last compound it is possible to obtain loratadine with known methods.
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