4-甲基吡啶氧化物置于盐酸体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 2-氨基-4-甲基吡啶 参考文献:Substituted 2-Aminopyridines As Inhibitors Of Nitric Oxide Synthases 标题:Substituted 2-Aminopyridines As Inhibitors Of Nitric Oxide Synthases 摘要:A Series Of Substituted 2-Aminopyridines Was Prepared And Evaluated As Inhibitors Of Human Nitric Oxide Synthases (Nos). 4,6-Disubstitution Enhanced Both Potency And Specificity For The Inducible Nos With The Most Potent Compound Having An Ic50 Of 28 Nm. (C) 2000 Elsevier Science Ltd. All Rights Reserved. DOI:10.1016/s0960-894X(00)00389-9
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-4557866-A 优先权日:1984-05-15 标 题 :Process for the synthesis of pyrido-imidazo rifamycins 发明人:CANNATA VINCENZO; TAMAGNONE GIAN F 权利人:ALFA FARMACEUTICI SPA 摘要:A new process for the synthesis of pyrido-imidazo-rifamycins of formula I wherein R is hydrogen or acetyl, R1 and R2 independently represent hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)-alkylamino-(C1-4)-alkyl, (C1-3)-alkoxy-(C1-4)-alkyl, hydroxymethyl, hydroxy-(C2-4)-alkyl, cyano, halogen, nitro, mercapto, (C1-4)-alkylthio, phenylthio, carbamoyl, mono- or di-(C1-4)-alkyl-carbamoyl, or R1 and R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups. The process comprises reacting the rifamycin O of formula II with a 2-aminopyridine of formula III wherein R1 and R2 have the same meanings as before.
专利号:US-2008242866-A1 优先权日:2007-03-30 标 题 :Synthesis of anthranilamides 发明人:SCHMEES NORBERT; PETROV ORLIN 权利人:SCHMEES NORBERT; PETROV ORLIN 摘要:The present invention relates to a novel method of preparing anthranilamides of formula I: n n n n n n n n n n in which R 1 , R 2 , R 3 , A, E, Q, X, and W are defined in the claims, to a novel intermediate compound, and to the use of said novel intermediate compound for the preparation of said anthranilamides of formula I.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.
专利号:US-3992392-A 优先权日:1973-04-27 标题:Synthesis of indoles from anilines and intermediates therein 发明人:GASSMAN PAUL G 权利人:UNIV OHIO STATE RES FOUND 摘要:Preparing indoles and intermediates therefor by reacting an N-haloaniline with a β-carbonylic hydrocarbon sulfide to form an azasulfonium halide, reacting the azasulfonium halide with a strong base to form a thio-ether indole derivative, and then reducing the thio-ether indole, e.g. with Raney nickel, to form the indole compound. When an acetal or ketal of the β-carbonyl hydrocarbon sulfide is used, the azasulfonium salt is treated with a base, and then with an acid to form the thio-ether indole derivative. When an α-ethyl-β -carbonylic hydrocarbon sulfide is used, the resulting azosulfonium salt reacts with strong base to form a thio-ether indolenine derivative, which on reduction with Raney nickel or complex metal hydrides yields 3-substituted indoles. The aniline may be an aminopyridine to form an aza-indole compound in the process. The azasulfonium salts and thio-ether indole or thio-ether indolenine derivatives can be isolated and recovered from their respective reaction mixtures. The thio-ether-indole and thio-ether indolenine derivatives are useful as intermediates to make the indoles without the thio-ether group. The indoles are known compounds having a wide variety of uses, e.g., in making perfumes, dyes, amino acids, pharmaceuticals, agricultural chemicals and the like.
专利号:US-9150590-B2 优先权日:2011-05-19 标 题 :Process for the synthesis of rifaximin and a new pseudo-crystalline form of rifaximin obtained thereby 发明人:MAZZOLA DISMA; MOIANA SILVIA; COPPI GERMANO 权利人:MAZZOLA DISMA; MOIANA SILVIA; COPPI GERMANO; FRIULCHEM SPA 摘要:Process for the preparation of rifaximin, pseudo-crystalline rifaximin and a new pseudo-crystalline form of rifaximin with fewer impurities obtained thereby.
参考文献:10.1107/s1600536811009287 摘要:Aghabozorg H, Foroughian M, Foroumadi A, Bruno G, Amiri Rudbari H. N1,N1-Dimethylpropane-1,2-diaminium bis(6-carboxypyridine-2-carboxylate) monohydrate. Acta Crystallogr E Struct Rep Online. 2011 Mar 19;67(4):o932–3. doi: 10.1107/s1600536811009287.