📜苯基甘油醇置于三乙胺,三苯基膦,红铝,偶氮二甲酸二乙酯体系中,用 四氢呋喃,乙二醇二甲醚,乙醚,甲苯 用作溶剂,化学反应 13.0H,反应生成(3S)-N-甲基-3-(2-甲基苯氧基)-3-苯基丙烷-1-胺 参考文献:Asymmetric Synthesis Of Both Enantiomers Of Tomoxetine And Fluoxetine. Selective Reduction Of 2,3-Epoxycinnamyl Alcohol With Red-Al 标题:Asymmetric Synthesis Of Both Enantiomers Of Tomoxetine And Fluoxetine. Selective Reduction Of 2,3-Epoxycinnamyl Alcohol With Red-Al 摘要: Doi:10.1021/jo00252A036
专利信息
专利号:US-8367868-B2 优先权日:2006-10-16 标题:Process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine 发明人:BERTOLINI GIORGIO; VERZOLA BARBARA; VERGANI DOMENICO 权利人:ARCHIMICA SRL; BERTOLINI GIORGIO; VERZOLA BARBARA; VERGANI DOMENICO 摘要:The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: n nwhere: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:
专利号:US-7507861-B2 优先权日:2004-06-28 标题:Process for the preparation of atomoxetine hydrochloride 发明人:CASTELLI EUGENIO; LO MONACO GIUSEPPE; MANTOVANI SILVIA; DAVERIO PAOLA; RIVA PAOLO; VAILATI ALESSANDRA; BIANCHI STEFANO 权利人:TEVA PHARM FINE CHEMICALS SRL 摘要:The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water.
专利号:US-7439399-B2 优先权日:2004-06-28 标题:Processes for the preparation of atomoxetine hydrochloride 发明人:ARONHIME JUDITH; BIANCHI STEFANO; CASTELLI EUGENIO; DAVERIO PAOLA; MANTOVANI SILVIA; KOVACSNE-MEZEI ADRIENNE 权利人:TEVA PHARM FINE CHEMICALS SRL 摘要:The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(−)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water. In preferred embodiments, the atomoxetine hydrochloride produced is Form A.
专利号:EP-1673335-A2 优先权日:2004-06-28 标 题 :Process for the preparation of atomoxetine hydrochloride 发明人:CASTELLI EUGENIO; LO MONACO GIUSEPPE; MANTOVANI SILVIA; DAVERIO PAOLA; RIVA PAOLA; BIANCHI STEFANO 权利人:TEVA PHARM FINE CHEMICALS SRL 摘要:The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HC1 by adding HCl to a mixture of (R)-(-)-tomoxetine (S)-(+)Âmandelate with an organic solvent, with or without a base and water.
专利号:US-2010105942-A1 优先权日:2006-10-16 标题:Process for the Synthesis of Aryloxypropylamine and Heteroaryloxypropylamine
参考标题:Chemoenzymatic Synthesis Of The Non-Tricyclic Antidepressants Fluoxetine, Tomoxetine And Nisoxetine 作者:Hui-Ling Liu,Bård Helge Hoff,Thorleif Anthonsen 摘要:3-Chloro-1-Phenylpropan-1-Ol And The Corresponding Butanoate, 3-Chloro-1-Phenyl-1-Propyl Butanoate, Were Kinetically Resolved Using Lipase B From Candida Antarctica Catalysis By Transesterification And Hydrolysis Respectively. The Resulting Chiral Building Blocks (S)- And (R)-3-Chloro-1-Phenylpropanol Were Converted Into Both Enantiomers Of The Antidepressant Drugs, Fluoxetine, Tomoxetine And Nisoxetine.