发明名称 Process for obtaining a derivative of 2-amino-1- phenylpropan-1-ol.
摘要 Process for obtaining a derivative of 2-amino-1- phenylpropan-1-ol. Process for the industrial preparation of a 2-amino-1- phenylpropan-1-ol derivative, specifically (-)-erythro- N,N-[2-(10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5- ylidine)ethyl]methyl-2-amino-1-phenylpropan-1-ol I, also known as WAS-4304 or Trecadrine, characterised in that the (10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidine) acetaldehyde is caused to react with (-)-ephedrine to obtain a 1,3-oxazolidine derivative as an intermediate, which may or may not be isolated and which is converted into Trecadrine I by reduction. The solvents used in preparation of the intermediate are not strongly polar, such as hydrocarbons, ethers or chlorinated solvents. The reduction may be performed by catalytic hydrogenation, treatment with hydrides or treatment with aluminium or sodium amalgam. Product I obtained is useful as a pharmaceutically active ingredient for the treatment of ulcers. <IMAGE>
申请公布号 ES2017278(A6) 申请公布日期 1991.01.16
申请号 ES19890003187 申请日期 1989.09.21
申请人 SOCIEDAD ESPANOLA DE ESPECIALIDADES FARMACOTERAPEUTICAS, S.A. 发明人 FORNE ERNESTO;ANDREOLI ROMEO;CEPERO RICARDO
分类号 A61K31/135;C07C215/38;(IPC1-7):C07C215/38 主分类号 A61K31/135
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