CAS: 850222-40-1; (S)-3-(Dimethylamino)-1-(3-Methoxyphenyl)-2-Methylpropan-1-One

相似化合物

197145-37-2 37951-53-4 2125-49-7

上下游产品

CAS号850222-41-2 (S)-3-(二甲基氨基)-1... | CAS号197145-37-2 3-(二甲基氨基)-1-(3-... | CAS号3027-13-2 3-甲氧基苯基丙酮 | CAS号175591-22-7 (2R,3R)-3-(3-甲氧... | CAS号175591-23-8 他喷他多

3-甲氧基苯基丙酮置于二乙胺,三氟乙酸体系中,用 甲醇,甲基叔丁基醚,丙酮 作为反应溶剂,化学反应生成 (S)-3-(二甲基氨基)-1-(3-甲氧基苯基)-2-甲基-1-丙酮
参考文献:Prodrugs Of Opioids And Uses Thereof
标题:Prodrugs Of Opioids And Uses Thereof
摘要:本发明涉及阿片类镇痛药的前药以及含有此类前药的药物组合物.本发明提供了通过前述前药增加阿片类镇痛药的生物利用度,从而提供更一致的疼痛缓解方法.该发明还提供了减少阿片类镇痛药对胃肠道的副作用的方法.

专利信息

专利号:US-8791287-B2
优先权日:2010-07-02
标 题:Process for the synthesis of tapentadol and intermediates thereof
发明人：MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO; LANDONI NICOLA
权利人:MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO; LANDONI NICOLA; EUTICALS SPA
摘要:The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process. n A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention. n Still another object of the invention is represented by the crystalline forms I and II of the tapentadol free base. n A further object of the present invention is the mixture of the crystalline forms I and II of the tapentadol free base.

专利号:US-2013296608-A1
优先权日:2011-01-27
标 题 :Novel stereospecific synthesis of (-) (2s, 3s)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol
发明人：MOHAN RAO DODDA; KRISHNAREDDY PINGILI; RAMACHANDRAREDDY PINGILI; HARITHA KIRLA; SRINIVAS KOLLURU
权利人:MOHAN RAO DODDA; KRISHNAREDDY PINGILI; RAMACHANDRAREDDY PINGILI; HARITHA KIRLA; SRINIVAS KOLLURU; SYMED LABS LTD
摘要:The present invention relates to a novel stereospecific synthesis of (−)(2S,3S)-1-dimethylamino-3-(3-methoxyphenyl)-2-methyl pentan-3-ol an intermediate in the synthesis of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol.

专利号:US-8729308-B2
优先权日:2009-12-01
标 题:Process for the preparation of tapentadol and intermediates thereof
发明人：MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO
权利人:MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO; EUTICALS SPA
摘要:The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below n nusing the (2R,3R)—O,O′-dibenzoyltartaric chiral acid wherein said resolution is quantitative.n n The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.

专利号:US-2013178644-A1
优先权日:2010-07-02
标 题:Process for the synthesis of tapentadol and intermediates thereof

专利号:WO-2012001571-A1
优先权日:2010-07-02
标题 :New process for the synthesis of tapentadol and intermediates thereof

专利号:CN-102477016-A
优先权日:2010-11-26
标题:Synthesis and Application of Intermediates of Tapentadol