CAS: 10421-85-9; 2-Chloromandelic Acid

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52950-19-3 52950-18-2 156276-21-0

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CAS号13312-84-0 2-氯-α-羟基苯基乙腈 | CAS号2142-68-9 邻氯苯乙酮 | CAS号67-66-3 氯仿 | CAS号89-98-5 邻氯苯甲醛 | CAS号74-90-8 氢氰酸 | CAS号75-25-2 三溴甲烷 | CAS号118-91-2 邻氯苯甲酸 | CAS号13011-88-6 3,4-Furandiol,2... | CAS号144664-09-5 (S)-2-氯扁桃酰胺 | CAS号89-98-5 邻氯苯甲醛 | CAS号118-91-2 邻氯苯甲酸 | CAS号85259-19-4 α-溴-氯苯乙酸甲酯 | CAS号90055-47-3 2,2'-二氯苯乙酸甲酯 | CAS号62123-75-5 2-(2-氯苯基)-2-氧代乙酸乙酯 | CAS号2444-36-2 2-氯苯乙酸 | CAS号32345-60-1 2-氯-L-扁桃酸甲酯 | CAS号34113-46-7 2-(2-氯苯基)-2-(4-... | CAS号29270-30-2 2-溴代-2-氯苯乙酸

邻氯苯乙酮置于水,溴,溶剂黄146,Sodium Hydroxide体系中,化学反应 19.75H,反应生成邻氯扁桃酸
参考文献:通过与手性 N-取代 2-氨基-2-苯基乙醇形成非对映体盐分离 2-卤扁桃酸的对映体
标题:通过与手性 N-取代 2-氨基-2-苯基乙醇形成非对映体盐分离 2-卤扁桃酸的对映体
摘要:手性n取代仲 1,2-氨基醇已开发用于通过非对映体盐形成原卤扁桃酸 ( O-X-Ma) 的对映体分离.两种结构异构体n-甲基-2-氨基-1,2-二苯基乙醇和n-苄基-2-氨基-2-苯基乙醇对o-X-Ma(x = Cl,Br,I)表现出较高的分离能力.通过难溶盐的晶体学分析阐明了手性识别机制.拆分剂氮原子上的取代基和结晶溶剂的包含稳定了盐并增强了它们的分离能力.
Doi:10.1002/chir.23630

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-11807883-B2
优先权日:2020-11-03
标 题:Polypeptide tag, highly soluble recombinant nitrilase and application thereof in synthesis of pharmaceutical chemicals
发明人：XUE YAPING; XIE DONG; XIONG NENG; ZHENG YUGUO
权利人:UNIV ZHEJIANG TECHNOLOGY
摘要:The present invention provides a polypeptide tag and its application in the synthesis of pharmaceutical chemicals, the recombinant nitrilase was obtained by connecting a polypeptide tag to the N-terminus of the amino acid sequence of the nitrilase; wherein amino acids at both ends of the polypeptide tag are uncharged glycine G, and the rest are a random combination of any one or more of glycine G, histidine H, glutamic acid E, aspartic acid D, lysine K and arginine R; The activity of the recombinant nitrilase in the preparation of 1-cyanocyclohexyl acetic acid is up to 3034.7 U/g dcw, the polypeptide tag significantly improves the soluble expression of nitrilase, and the whole cell catalyst hydrolyzes 1M substrate with the same concentration 30 minutes faster than the mother enzyme. The method provided by the present invention can also be used for the biocatalytic reaction of other pharmaceutical intermediates as the substrate catalyzed by the nitrilase, improving the activity of the whole cell catalyst in reaction, and also improving the solubility of other types of nitrilases and the activity of the corresponding whole cell catalysts.

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-8981121-B2
优先权日:2010-06-25
标 题 :Process for the preparation of nitrogen substituted aminotetralins derivatives
发明人：ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE
权利人:ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE; UCB PHARMA GMBH
摘要:The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).

专利号:US-10975096-B2
优先权日:2014-06-20
标题 :Synthesis of polycyclic-carbamoylpyridone compounds
发明人：CHIU ANNA; ENQUIST JR JOHN; GRIGGS NOLAN; HALE CHRISTOPHER; IKEMOTO NORIHIRO; KEATON KATIE ANN; KRAFT MATT; LAZERWITH SCOTT E; LEEMAN MICHEL; PENG ZHIHUI; SCHRIER KATE; TRINIDAD JONATHAN; VAN HERPT JOCHEM; WALTMAN ANDREW W
权利人:GILEAD SCIENCES INC
摘要:Methods of making compounds of Formula I are disclosed:

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.