CAS: 13636-02-7; 3-(Dimethylamino)-1-(2-Thienyl)-1-Propanol

上下游产品

CAS号5424-47-5 3-(二甲氨基)-1-(2-噻... | CAS号13196-35-5 3-二甲基氨基-1-(2-噻吩... | CAS号132335-49-0 R-3-(二甲基氨基)-1-(... | CAS号34772-98-0 3-二甲氨基-1-(2-噻吩基... | CAS号88-15-3 2-乙酰基噻吩 | CAS号116817-11-9 (RS)-度洛西汀盐酸盐 | CAS号132335-46-7 S-(+)-N,N-二甲基-3... | CAS号132335-44-5 (S)-(-)-N,N-二甲基... | CAS号132335-47-8 二甲基草酸盐 | CAS号136434-34-9 盐酸度洛西汀 | CAS号116539-55-0 3-甲基氨基-1-(2-噻吩基...

3-二甲基氨基-1-(2-噻吩基)-1-丙酮置于三乙酰氧基硼氢化钠体系中,用 四氢呋喃 用作溶剂,化学反应 12.0H,以94.2%的收率获得3-(二甲基氨基)-1-(2-噻吩基)-1-丙醇
参考文献:一种s-(+)盐酸度洛西汀中间体的制备方法
标题:一种s-(+)盐酸度洛西汀中间体的制备方法
摘要:本发明公开了一种化合物式b的制备方法,所述制备方法包括将式a化合物溶于溶剂中,通过还原剂作用发生反应.所述还原剂包括硼氢化钠,三乙酰氧基硼氢化钠等还原剂.进一步的,反应在络合物二茂铁参与下还原得到式b的化合物ee值高达98%以上;本发明提供的制备方法简易可行,无需拆分或手性催化诱导,产品收率及手性纯度高,适用于s‑(+)‑盐酸度洛西汀的工业化生产.

专利信息

专利号:US-2004249170-A1
优先权日:2002-01-24
标 题 :Process for preparing an intermediate useful for the asymmetric synthesis of duloxetine
发明人：BORGHESE ALFIO
摘要:This invention provides a process for the synthesis of(S)-3-Methylamino-1-2-thienyl)-1-propanol, a key intermediate in the synthesis of duloxetine.

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: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.