CAS: 136434-34-9; (S)-Duloxetine Hydrochloride

上下游产品

Duloxetine (S)-(+)-N,N-dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine, phosphoric acid salt phenyl chloroformate N-methyl-(S)-duloxetineduloxetine succinamide duloxetine phthalamide 2-(N-methyl-propanamine)-3-(2-naphthol)thiophene Duloxetine

度洛西汀置于盐酸体系中,用 乙酸乙酯 用作溶剂,以80%的收率获得盐酸度洛西汀
参考文献:一种新型酮胺酶促不对称羰基还原反应合成(S)-度洛西汀盐酸盐的改进方法
标题:一种新型酮胺酶促不对称羰基还原反应合成(S)-度洛西汀盐酸盐的改进方法
摘要:(S)-盐酸度洛西汀 1 是一种用于治疗重度抑郁症,广泛性焦虑症,纤维肌痛和神经性疼痛的药物(图 1).1,2 由于其在 D...
Doi:10.1080/00304948.2020.1818527

专利信息

专利号:US-5491243-A
优先权日:1993-10-12
标题 :Intermediate useful for the asymmetric synthesis of duloxetine
发明人：BERGLUND RICHARD A
权利人:LILLY CO ELI
摘要:This invention provides a stereospecific process for the synthesis of (S)-(+)-N,N-dimethyl-3-(1-naphthalenyloxy)-3-(2-thienyl)propanamine, a key intermediate in the synthesis of duloxetine.

专利号:US-7538232-B2
优先权日:2006-01-19
标 题 :Process for the asymmetric synthesis of duloxetine
发明人：BUTCHKO MARK ANTHONY; MERSCHAERT ALAIN; MODER KENNETH PHILIP
权利人:LILLY CO ELI
摘要:This invention provides an improved asymmetric process for the synthesis of duloxetine involving arylation of Compounds of Formula I.

专利号:US-8269023-B2
优先权日:2007-03-05
标题 :Process for preparation of duloxetine hydrochloride
发明人：SIYAN RAJINDER SINGH; GOHEL SUNIL KUMAR VINUBHAI; SINGH GIRIJ PAL
权利人:SIYAN RAJINDER SINGH; GOHEL SUNIL KUMAR VINUBHAI; SINGH GIRIJ PAL; LUPIN LTD
摘要:An improved process for synthesis of duloxetine hydrochloride (1) having chiral purity greater than 99.9% that is characterized by the following:n (i) preparation of racemic condensed compound (RS)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (4) by reaction of racemic hydroxy compound (2) with 1-fluoronaphthalene (3) in presence of a base such as sodamide, potassium amide or potassium bis(trimethylsilyl)amide (KHDMS) in polar aprotic solvent, (ii) optical resolution of racemic condensed compound (5a+5b) with di-benzoyl-L-tartaric acid (7, DBTA, R=H) or di-para-anisoyl-L-tartaric acid (7, DATA, R=OCH 3 ) to obtain crude (S)—N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine dibenzoyl tartarate salt (8a) or (S)—N.N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine di-p-anisoyl tartarate salt (9a) respectively, (iii) optionally purification of crude tartarate salts (8a or 9a) by crystallization, (iv) optionally purification of duloxetine hydrochloride (1) by crystallization and (v) racemization of undesired (R)—N,N-di methyl-3-(1-naphthyloxy)-3-(2-thienyl)propanamine (5b) by treatment with base potassium bis(trimethylsilyl)amide (KHDMS) to obtain racemic mixture of condensed compounds (5a and 5b).

专利号:US-2005171360-A1
优先权日:2002-02-22
标题:Preparation of n-methyl-3-hydroxy- 3-(2-thienyl)propylamine via novel thiophene derivatives containing carbamate groups as intermediates
发明人：REICHERT DIETMAR; ALMENA PEREA JUAN J; SCHWARM MICHAEL; DRAUZ KARLHEINZ; KRIMMER HANS-PETER
摘要:A novel route is described for the synthesis of N-methyl-3-hydroxy-3-(2-thienyl)propylamine IV, which can be used as a starting compound for the preparation of duloxetine. N-methyl-3-hydroxy-3-(2-thienyl)propylamine is synthesized via novel thiophene derivatives containing carbamate groups, I and IIa, as intermediates.

专利号:US-2011040105-A1
优先权日:2008-04-16
标题 :Processes useful for the synthesis of (r)-1--2-methyl-pyrrolidine
发明人：HUBER CHRISTIAN H; KHULMAN YOUNG MI; TANDEL SAGUN K; JOHANNSEN STEPHEN R; WANG TINGMIN; ANGELL PAUL
权利人:ARENA PHARM INC
摘要:Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.

专利号:EP-1857451-B1
优先权日:2006-05-05
标 题:A process for the preparation of an intermediate useful for the asymmetric synthesis of (+)duloxetine
发明人：POGGIALI ANDREA; PIZZOCARO FRANCESCO; TUBERTINI PAOLO
权利人:FIDIA FARMACEUTICI
摘要:A process for the preparation of (+)duloxetine, or an acid addition salt thereof, comprising: n(i) Resolving racemic (±)N-methyl duloxetine with a less than stoichiometric amount of a chiral acid in combination with suitable amounts of a hydrohalogen acid to give a salt of the chiral acid and (+)N-methyl duloxetine, substantially free from (-)N-methyl duloxetine; n(ii) Demethylating the (+)N-methyl duloxetine prepared in step (i) to give (+)duloxetine or another acid addition salt in enantiomerically pure form.