A METHOD FOR THE PREPARATION OF (S)-N-METHYL-3-(l-
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专利名称：A METHOD FOR THE PREPARATION OF (S)-N-METHYL-3-(l-NAPHTHYLOXY)-3-(2-
THIENYL)PROPYLAMINE HYDROCHLORIDE
(DULOXETINE)
发明人：RIDVAN, Ludek,JARRAH, Kamal,CINIBULK, Josef,ZATOPKOVA, Monika,PLACEK, Lukas
申请号：EP06840860.8
申请日：20061222
公开号：EP1968965A2
公开日：
20080917
专利内容由知识产权出版社提供
摘要：A method of preparation of (S)-N-methyl-3-(l-naphthyloxy)-3-(2-
mienyl)propylamine of Formula(l) and its pharmaceutically acceptable salts, comprising a) reaction of (RS)-N, N-dimethyl-3-(l-naρhthyloxy)-3-(2-th1enyl)propylamine with optically active D-tartaric acid or an acid salt derived from D-tartaric acid forming a mixture of diastereoisomeric salts of N,N-dimethyl-3-(l-naphthyloxy)- 3-(2-thienyl)propylamine and D- tartaric acid (2:1), b) isolation of the salt (S)-N, N-dimethyl-3-(naphthyloxy)-3-(2-thienyl)propylamine/D- tartrate (2:1) from the mixture of diastereoisomeric salts in an organic solvent, water or a mixture thereof and release of (S)-N, N-dimethyl-3-(l-naphthyloxy)-3-(2-thienyl) propylamine by action of an inorganic or organic base, c) demethylation of (S)-N,N-dimethyl-3-(1-naphthyloxy)-3-(2- thienyl) propylamine by action of an alkylchloroformate of formula C1COOR (R=C1-C5 alkyl, or C6-C12 aryl or alkylraryl), especially phenyl, ethyl or methyl chloroformate, and d) hydrolytic release of the duloxetine base of formula I and optionally conversion of the base to a salt with the
respective acid, or salt of a weak base.
申请人：Zentiva, a.s.
地址：U kabelovny 130, Dolni Mecholupy 102 37 Praha 10 CZ 国籍：CZ
代理机构：Jirotkova, Ivana
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