左氯替西汀酰胺杂质盐酸盐置于盐酸体系中,用 水 用作溶剂,化学反应 4.0H,反应生成左西替利嗪 参考文献:Process For Preparing (S) And (R)-2-[4-(4-Chlorobenzhydryl)Piperazin-1-Yl]-Ethoxyacetamide 标题:Process For Preparing (S) And (R)-2-[4-(4-Chlorobenzhydryl)Piperazin-1-Yl]-Ethoxyacetamide 摘要:本发明涉及一种通过使用多柱色谱分离外消旋混合物来制备(S)-2-[4-(4-氯苯基)-1-哌嗪基]-乙氧基乙酰胺和(R)-2-[4-(4-氯苯基)-1-哌嗪基]-乙氧基乙酰胺的方法.
专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-7619085-B2 优先权日:2005-03-03 标 题 :Pyroglutamate salts and their use in the optical resolution of intermediates for the synthesis of dextrocetirizine and levocetirizine 发明人:PALACIO MAGALI; ATES CELAL 权利人:UCB PHARMA SA 摘要:The present invention relates to (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(S)-pyrrolidone-5-carboxylic acid salt; (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide-(R)-pyrrolidone-5-carboxylicacid salt; or (R)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxycetamide-(R)-pyrrolidone-5-carboxylic salt. The present invention relates also to a process for preparing (S)-2-[4-(4-chlorobenzhydryl)piperazin-1-yl]-ethoxyacetamide (I) and (R)-2-[4-(4-chlorobenzhydryl) piperazin-1-yl]-ethoxyacetamide (II) by chemical resolution of a mixture. These compounds are respectively intermediates for the synthesis of dextrocetirizine and levocetirizine.
专利号:US-7807837-B2 优先权日:2004-05-07 标 题 :Scalable synthesis of imidazole derivatives 发明人:JONES TODD K; MANI NEELAKANDHA 权利人:JANSSEN PHARMACEUTICA NV 摘要:Imidazole derivatives, compositions containing them, methods of preparing them, including regioselective scale-up synthetic methods, and methods of using them.
专利号:EP-1354593-B1 优先权日:2002-04-08 标题 :use of an extract of a non-photosynthetic filamentous bacterium as an agent for enhancing the endogenous synthesis of superoxide dismutase 发明人:MAHE YANN; MEYBECK ALAIN 权利人:OREAL 摘要:Promoting endogenous production of superoxide dismutase (SOD) comprises the use of an extract (I) of non-photosynthetic, non-fruiting filamentous bacteria in cosmetic, dermatological or pharmaceutical applications. Use of an extract (I) of non-photosynthetic, non-fruiting filamentous bacteria: (1) in a composition based on a cosmetic medium, as an agent for promoting endogenous production of superoxide dismutase (SOD); or (2) for production of a pharmaceutical or dermatological composition for promoting endogenous production of SOD. Independent claim are also included for: (1) a composition comprising a physiological medium containing Vitreoscilla filliformis extract (Ia) and lycopene (specifically at 0.000000001-0.1 wt. %) or a compound having catalase activity and/or a compound having peroxidase activity; and (2) cosmetic treatment methods for treating loss of firmness and/or elasticity of the skin or for treating skin exposed to sunlight, involving application of compositions containing (Ia).
专利号:US-2006111369-A1 优先权日:2004-11-10 标 题:Synthesis, characterization and biological action of optically active isomers of floxacins 发明人:SOMBERG JOHN C; RANADE VASANT V 权利人:SOMBERG JOHN C; RANADE VASANT V 摘要:Disclosed herein is the method for synthesis and separation of enantiospecific isomers of floxacins. These isomers can be used to study the antibacterial action, as well as cardiac effects, such as arrhythmogenic activity, QT internal prolongation and dispersion, and Ikr inhibition in humans. A method for the identification of chiral isolates of the floxacins that are devoid or possess less QT prolonging action and thus cause less arthropathy especially of the Torsades de pointes variety. Also disclosed are methods for assaying these isomeric compounds present in the biological fluids.
专利号:US-7381821-B2 优先权日:2003-01-23 标 题 :Piperazine derivatives and their use as synthesis intermediates 发明人:ATES CELAL; CAVOY EMILE; BOUVY DIDIER 权利人:UCB SA 摘要:The present invention relates to new enantiomerically pure piperazine derivatives of formula (I) wherein Y represents hydroxy or a leaving group and n is 1, 2, 3, 4 or 5, and to their use as synthesis intermediates, especially for the preparation of pharmaceutically active compounds
1: Weinberger M, Hendeles L. Nonprescription medications for respiratory symptoms: Facts and marketing fictions. Allergy Asthma Proc. 2018 May 1;39(3):169-176. doi: 10.2500/aap.2018.39.4117. doi: 10.1002/hup.2655. Epub 2018 Mar 13. 3: Domagała A, Szepietowski J, Reich A. Antihistamines in the treatment of pruritus in psoriasis. Postepy Dermatol Alergol. 2017 Oct;34(5):457-463. doi: 10.5114/ada.2017.71112. Epub 2017 Oct 31. 4: Okubo K, Uchida E, Terahara T, Akiyama K, Kobayashi S, Tanaka Y. Efficacy and safety of emedastine patch, a novel transdermal drug delivery system for allergic rhinitis: Phase III, multicenter, randomized, double-blinded, placebo-controlled, parallel-group comparative study in patients with seasonal allergic rhinitis. Allergol Int. 2018 Jan 29. pii: S1323-8930(17)30189-2. doi: 10.1016/j.alit.2017.12.005. [Epub ahead of print] doi: 10.4103/ijdvl.IJDVL_860_17. doi: 10.4103/ijd.IJD_710_16.
合成参考文献
参考文献:10.1159/000089035 摘要:Pitarch G, Torrijos A, Martínez-Menchón T, Sánchez-Carazo JL, Fortea JM. Familial aquagenic urticaria and bernard-soulier syndrome. Dermatology. 2006;212(1):96–7. doi: 10.1159/000089035. 参考文献:10.1007/s00213-011-2400-7 摘要:Verster JC, Roth T. Drivers can poorly predict their own driving impairment: a comparison between measurements of subjective and objective driving quality. Psychopharmacology (Berl). 2012 Feb;219(3):775–81.