4-羟甲基苯甲酸置于氯化亚砜体系中,化学反应 18.0H,反应生成 4-氯甲基苯甲酸甲酯 参考文献:Development Of Potent And Selective Plasmin And Plasma Kallikrein Inhibitors And Studies On The Structure-Activity Relationship. 标题:Development Of Potent And Selective Plasmin And Plasma Kallikrein Inhibitors And Studies On The Structure-Activity Relationship. 摘要:基于结构-活性关系研究,我们设计和合成了纤溶酶(pl)和血浆激肽释放酶(pk)抑制剂.反式-(4-氨基甲基环己烷羰基)-酪氨酸(邻吡啶甲酸)-辛酰胺对pl,Pk,尿激酶(uk)和凝血酶(th)的ic50值分别为0.53,30,5.3和>400μm.反式-(4-氨基甲基环己烷羰基)-酪氨酸(2-嘧啶)-4-羧基苯胺对pl,Pk,Uk和th的ic50值分别为36,0.56,440和>1000μm. DOI:10.1248/cpb.48.1964
专利号:US-12129222-B2 优先权日:2016-08-11 标题:Production of bitter principle derivatives 发明人:WYRWA RALF; RODE CLAUDIA; SEEMANN THOMAS; MEINEL LORENZ; RITZER JENNIFER; SCHNABELRAUCH MATTHIAS 权利人:UNIV WUERZBURG J MAXIMILIANS; JULIUS MAXIMILIANS UNIV 摘要:It is an object of the present invention to introduce carboxylic acid-functionalities suitable for coupling into the denatonium structure by means of simple synthesis, namely the synthesis of bitter principle derivatives based on the denatonium structure according to formula 1:For example, according to the invention, lidocaine derivatives may be reacted with carboxylated benzyl halogenides. The carboxylated denatonium derivatives of the present invention are especially applied in medicine, biology, medical engineering as well as cosmetics, the pharmaceutical, chemical, and foodstuff industry.
专利号:US-4719053-A 优先权日:1980-08-01 标题 :Beta-chloroethylsulfonylmethyl-benzoic halides as intermediates 发明人:SCHLAEFER LUDWIG; HAEHNLE REINHARD 权利人:HOECHST AG 摘要:New beta -chloroethylsuflonylmethyl-benzoic acid halides which can serve as fibre-reactive anchors for thesynthesis of novel organic, water-soluble compounds, preferably dyestuffs, having fibre-reactive and fibre-finishing properties, such as preferably dyestuff properties, and containing, as a fibre-reactive group, one or two beta -chloroethylsufonylmethylbenzoic acid amide groups. For the synthesis of these novel fibre-finishing compounds, said new beta -chloroethylsulfonylmethyl-benzoic acid halide compounds are reacted with an organic, water-soluble compound having fibre-finishing properties and continuing one or two amino groups. Also precursors of the fibre-finishing, fibre-reactive compounds, containing said beta -chloroethylsulfonylmethyl-benzxoic acid amid grouping, can be employed for their synthesis. The novel fibre-finishing compounds can be applied onto suitable fibre materials, such as especially cellulose fibre material and natural or synthetic polyamide fibre materials, and fixed on these fibre materials in a manner similar to application and fixation methods usual in the technique for fibre-reactive compounds. The fibre-finished material, such as dyed material, shows very good wet fastnesses.
专利号:US-7781470-B2 优先权日:1999-09-13 标题:Aminodicarboxylic acid derivatives having pharmaceutical properties 发明人:ALONSO-ALIJA CRISTINA; HEIL MARKUS; FLUBACHER DIETMAR; NAAB PAUL; PERNERSTORFER JOSEF; STASCH JOHANNES-PETER; WUNDER FRANK; DEMBOWSKY KLAUS; PERZBORN ELIZABETH; STAHL ELKE 权利人:BAYER SCHERING PHARMA AG 摘要:The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, n nwherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.
专利号:US-5532408-A 优先权日:1992-10-05 标 题 :α-chain-modified isocarbacyclins and process for the production thereof 发明人:KOGA MASAHIRO; TANAKA TOSHIO; FUJII TAKAO; MASEGI TSUKIO 权利人:TEIJIN LTD 摘要:PCT No. pct/jp93/01407 Sec. 371 Date Apr. 5, 1995 Sec. 102(e) Date Apr. 5, 1995 PCT Filed Oct. 1, 1993 PCT Pub. No. wo94/07838 PCT Pub. Date Apr. 14, 1995.Provided are alpha -chain-modified isocarbacyclins of which the alpha -chain is modified with a phenylene group, a cycloalkylene group or a thiophendiyl group, and these alpha -chain-modified isocarbacyclins show the activity for inhibiting the DNA synthesis of human smooth muscle cell and are expected to be capable of inhibiting the hypertrophy of a blood vessel.
专利号:US-5081138-A 优先权日:1986-12-17 标题:3-hetero-substituted-n-benzyl-indoles and prevention of leucotriene synthesis therewith 发明人:GILLARD JOHN W; MORTON HOWARD E; FORTIN REJEAN; GUINDON YVAN 权利人:MERCK FROSST CANADA INC 摘要:Compounds having the formula: are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
专利号:CN-115557837-A 优先权日:2022-09-23 标题 :A process optimization for the synthesis of p-chloromethylbenzoic acid