CAS: 132335-44-5; (S)-N,N-Dimethyl-3-Hydroxy-3-(2-Thienyl)Propanamine

上下游产品

CAS号13196-35-5 3-二甲基氨基-1-(2-噻吩... | CAS号5424-47-5 3-(二甲氨基)-1-(2-噻... | CAS号287737-72-8 (2S)-HYDROXY(PH... | CAS号88-15-3 2-乙酰基噻吩 | CAS号132335-49-0 R-3-(二甲基氨基)-1-(... | CAS号13636-02-7 1-(2-噻吩基)-3-(二甲... | CAS号116539-60-7 R-(-)-度洛西汀 | CAS号116539-58-3 duloxetine | CAS号132335-46-7 S-(+)-N,N-二甲基-3... | CAS号878757-08-5 (R)-(-)-N,N-dim... | 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... | CAS号161005-84-1 (S)-N,N-Dimethy...

3-二甲基氨基-1-(2-噻吩基)-1-丙酮置于rucl2(1,1'-Bis(Diphenyphosphino)Ferrocene)[(1S,1'S)-6,6'-Dibromo-1,1'-Biisoindoline],Potassium Tert-Butylate,氢气体系中,用 丙醇 用作溶剂,20.0 °C,5.07 Mpa 条件下,反应 30.0H,反应生成S-(-)-N,N-二甲基-3-羟基-3-(2-噻吩)丙胺
参考文献:含刚性手性二胺和非手性二膦的钌催化剂用于芳族酮的高对映选择性加氢
标题:含刚性手性二胺和非手性二膦的钌催化剂用于芳族酮的高对映选择性加氢
摘要:一个手性元素就足够了:一种含有刚性手性二胺(bidn)和可商购的廉价非手性膦(dppf)的新型钌催化剂对于酮的对映选择性氢化非常有效(请参阅方案).获得了高反应活性(s / C高达100000)和出色的对映选择性(高达99% Ee).
Doi:10.1002/chem.201100820

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-7659409-B2
优先权日:2002-03-19
标 题 :3-Hydroxy-3-(2-thienyl) propionamides and production method thereof, and production method of 3-amino-1-(2-thienyl)-1-propanols using the same
发明人：TAKEHARA JUN; QU JINGPING; KANNO KAZUAKI; KAWABATA HIROSHI; DEKISHIMA YASUMASA; UEDA MAKOTO; ENDO KYOKO; MURAKAMI TAKESHI; SASAKI TOMOKO; UEHARA HISATOSHI; MATSUMOTO YOUICHI; SUZUKI SHIHOMI
权利人:MITSUBISHI CHEM CORP
摘要:The object of the present invention is to provide 3-hydroxy-3-(2-thienyl)propionamides useful as synthesis intermediates of pharmaceutical preparations and the like and a method for obtaining optically active 3-amino-1-(2-thienyl)-1-propanols using the same with high reaction yield, high optical yield and industrially low cost. n According to the present invention, 3-amino-1-(2-thienyl)-1-propanols are obtained by carrying out asymmetric reduction of a β-ketocarbonyl compound having thiophene ring in the presence of a catalyst constituted from a compound of a group VIII or IX metal in the periodic table (e.g., a ruthenium compound) and an asymmetric ligand represented by a specified optically active diamine derivative (e.g., a diphenylethylenediamine derivative), or using a cell, a treated product of said cell or the like of a microorganism, and as occasion demands, carrying out amidation of the ester group and then carrying out reduction of the amido group. n n(each of the substituents is as described in claim 1 ).

专利号:US-2007167636-A1
优先权日:2006-01-19
标题 :Improved process for the asymmetric synthesis of duloxetine