📜Alpha-[2-(1-吡咯烷基)乙基]-Alpha-(对甲苯基)吡啶-2-甲醇置于硫酸,Sodium Hydroxide体系中,用 水 作为反应溶剂,化学反应 4.0H,以82%的收率获得产物曲普立定 参考文献: A Process For Preparation Of E-Isomer Of 1-(4-Methylphenyl)-1-(2-Pyrid yl)-3-Pyrrolidino Prop-1-Ene And Acid Addition Salts Thereof[fr] Procédé De Préparation De L'Isomère E Du 1-(4-Méthylphényl)-1-(2-Pyridyl)-3-Pyrrolidino-Prop-1-ène Et De Ses Sels D'Addition D'Acide 标题: A Process For Preparation Of E-Isomer Of 1-(4-Methylphenyl)-1-(2-Pyrid yl)-3-Pyrrolidino Prop-1-Ene And Acid Addition Salts Thereof[fr] Procédé De Préparation De L'Isomère E Du 1-(4-Méthylphényl)-1-(2-Pyridyl)-3-Pyrrolidino-Prop-1-ène Et De Ses Sels D'Addition D'Acide 摘要:一种制备formula-I中1-(4-甲基苯基)-1-(2-吡啶基)-3-吡咯烷基丙-1-烯的e-异构体及其酸盐的方法,该方法包括:脱水formula Iii中的1-(4-甲基苯基)-1-(2-吡啶基)-3-吡咯烷基丙醇,然后加入碱溶液以获得1-(4-甲基苯基)-1-(2-吡啶基)-3-吡咯烷基丙-1-烯的e和z异构体混合物,将该混合物用水洗涤以溶解z异构体并获得formula I中1-(4-甲基苯基)-1-(2-吡啶基)-3-吡咯烷基丙-1-烯的e-异构体,该异构体基本不含z异构体.
专利号:WO-2007141803-A3 优先权日:2006-06-08 标 题:A process for the synthesis of (e) -2-[1 - (4 - methyl phenyl) -3-(1-pyrronyl)-1 - propenyl] pyridine (triprolidine) 发明人:RAO GUDAPATI VENKATESWARA; SWAMY BHADRAPPA NARAYANA; KUSH ANIL KUMAR; REDDY GOUKANAPALLI CHANDRASEKARA 权利人:VITTAL MALLYA SCIENT RES FOUND; RAO GUDAPATI VENKATESWARA; SWAMY BHADRAPPA NARAYANA; KUSH ANIL KUMAR; REDDY GOUKANAPALLI CHANDRASEKA 摘要:A Process for the synthesis of (E) - 2 - [1 - (4 - methyl phenyl) -3- (1- pyrrolidinyl)-l- propenyl] pyridine (TRIPROLIDINE) by reacting 2-(l-pyrrolidino)ethyl triphenyl phosphonium bromide with 2-(p-toluoyl) pyridine in presence of aprotic solvent and a base, isomeising in presence of acid catalyst.
专利号:WO-9614060-A1 优先权日:1994-11-04 标题 :Use of receptor agonists to stimulate superoxide dismutase activity 发明人:MARKLUND STEFAN L; STRAALIN PONTUS 权利人:MARKLUND STEFAN L; STRAALIN PONTUS 摘要:The present invention relates to the use of a substance for the manufacture of a composition for stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells. In particular, the invention relates to the use of a substance for the manufacture of a composition for prophylaxis or treatment of a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical. Further, the invention relates to a method for determining the effect of a substance with respect to stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells and to substances which have been selected by said method. Within the scope of the invention is a method of preventing, diminishing, controlling or inhibiting a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical in a patient who has been established to have a high risk of developing a such disease or disorder, or who has developed a such disease or disorder, the method comprising administering an effective amount of a substance which is capable of stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells.
专利号:US-7919505-B2 优先权日:2006-07-11 标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound 发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N 权利人:SCHERING CORP 摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
专利号:US-2011003780-A1 优先权日:2007-07-10 标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof 发明人:ZHU MAN 权利人:SCHERING CORP 摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109
专利号:US-5426196-A 优先权日:1993-12-22 标题 :Synthesis of diaryl methanes 发明人:FANG FRANCIS G 权利人:GLAXO INC 摘要:The present Invention includes synthetic steps and intermediates involved in the following reaction scheme a of converting compounds of Formula (II) to the diarylmethanes of Formula (I): ##STR1## wherein: Y is oxygen or sulfur; n A, B, C, D, and E are carbon or 1, 2 or 3 of A, B, C, D, and E are independently nitrogen, and the others are carbon; and n wherein n R 1 through R 10 are selected independently from the group consisting of: hydrogen, hydroxy, alkyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy alkyl, perhalo-alkyl, amino, nitro, nitrile, halo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, heteroaryl, or aryl or heteroaryl, mono, di, or tri substituted with one or more hydrogen, hydroxy, alkyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkyl alkyl, alkenyl, hydroxy alkyl, alkoxy alkyl, perhaloalkyl, amino, nitro, nitrile, halo, carboxyl, sulfonyl, acyl, formyl, carbamoyl, trifluoromethyl, aminomethyl, azido, amido, hydrazino, aryl, aryloxy, or heteroaryl groups and; n the pharmaceutically acceptable salts and solvates thereof.
1: Xuan X, Huang L, Pan X, Li N. [Simultaneous determination of five cold medicine ingredients in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by pH/organic solvent double-gradient high performance liquid chromatography]. Se Pu. 2013 Feb;31(2):133-8. Chinese. doi: 10.1208/s12249-011-9738-3. Epub 2011 Dec 20. 3: Sandhya B, Hegde AH, Kalanur SS, Katrahalli U, Seetharamappa J. Interaction of triprolidine hydrochloride with serum albumins: thermodynamic and binding characteristics, and influence of site probes. J Pharm Biomed Anal. 2011 Apr 5;54(5):1180-6. doi: 10.1016/j.jpba.2010.12.012. Epub 2010 Dec 16. doi: 10.1016/j.jpba.2009.10.024. Epub 2009 Nov 10. doi: 10.1016/j.jchromb.2009.10.021. Epub 2009 Oct 31.
合成参考文献
摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 摘要:HANSCH,C ET AL. (1995) 摘要:Tested as SID 103223987 in AID 781329: 参考文献:10.1007/s00011-004-1247-3 摘要:Lipnik-Stangelj M, Carman-Krzan M. Activation of histamine H1-receptor enhances neurotrophic factor secretion from cultured astrocytes. Inflamm Res. 2004 Jun;53(6):245–52. doi: 10.1007/s00011-004-1247-3. 参考文献:10.1007/bf02968592 摘要:Yang JH, Kim DK, Yun MY, Kim TY, Shin SC. Transdermal delivery system of triamcinolone acetonide from a gel using phonophoresis. Arch Pharm Res. 2006 May;29(5):412–7. doi: 10.1007/bf02968592.