2-氯烟酸,3-氯-2-甲基苯胺置于对甲苯磺酸一水合物,Potassium Hydroxide体系中,用 水 用作溶剂,以72.1 %的收率获得2-(3-氯邻甲苯氨基)烟酸 参考文献: Sting Modulators,Compositions,And Methods Of Use[fr] Modulateurs De Sting,Compositions Et Méthodes D'Utilisation 标题: Sting Modulators,Compositions,And Methods Of Use[fr] Modulateurs De Sting,Compositions Et Méthodes D'Utilisation 摘要:The Present Disclosure Is Directed To Compounds Of Formula (I),Or Pharmaceutically Acceptable Salts Thereof And Compounds Of Formula (II),Or Pharmaceutically Acceptable Salts Thereof,That Modulate Stimulator Of Interferon Genes (Sting),Compositions Comprising Such Compounds,And Methods Of Using Same For The Treatment Of Disorders Such As Cancer And Autoimmune Disease.
专利号:WO-2024262824-A1 优先权日:2023-06-20 标 题 :Novel process for synthesis of polysubstituted pyridine derivatives 发明人:PARK SEUNG BUM; YI SIHYEONG 权利人:SEOUL NAT UNIV R&DB FOUNDATION 摘要:The present invention relates to a novel method for synthesizing a polysubstituted pyridine derivative and, more specifically, to a method for synthesizing a 2,3,5-substituted pyridine derivative through a specific ring cleavage reaction. In the synthesis method of the present invention, an enamine structure is formed in situ by using beta keto ester/sulfone/phosphonic acid ester and ammonium acetate and subjected to an aldol condensation reaction with 3-formyl (aza) indole/benzofuran, a cyclization reaction, and a ring-cleavage reaction in that order to synthesize a characteristic pyridine structure having an alkyl/aryl substituent attached to the 2-position thereof, an ester/sulfone/phosphonic acid ester attached to the 3-position thereof, and ortho-aminoaryl/phenol including various substituents attached to the 5-position thereof. In particular, (aza)indole/benzofuran and beta keto ester/sulfone/phosphonic acid ester, which are reaction substrates, are substrates having very high accessibility, and enable the introduction of various substituents, thereby constructing a pyridine skeleton having high biocompatibility into which ortho-aminoaryl or phenol substituents having various substituents are introduced.
专利号:US-9051302-B2 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents 发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN 权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG 摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
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-4255581-A 优先权日:1979-08-13 标题 :Process for the preparation of alkyl and aryl esters of 3'-substituted and 2', 3'-disubstituted 2-anilino-3-pyridinecarboxylic acids 发明人:LOS MARIO A 权利人:LAB BAGO S A 摘要:In this disclosure, the synthesis of alkyl and aryl esters of substituted 2-anilino-3-pyridinecarboxylic acids is described. This preparation is performed reacting a previously obtained alkyl or aryl ester of 2-chloro-3-pyridinecarboxylic acid, with 3,2 or 3-substituted aniline.
专利号:WO-0049038-A9 优先权日:1999-02-19 标题 :Synthetic peptide of regulatory virus protein r (vpr) of human immunodeficiency virus type 1 (hiv-1) and the utilization thereof 发明人:SCHUBERT ULRICH; HENKLEIN PETER; WRAY VICTOR 权利人:SCHUBERT ULRICH; HENKLEIN PETER; WRAY VICTOR 摘要:The invention relates to synthetic (s) peptides of regulatory virus protein R (Vpr) of human immunodeficiency virus type 1(HIV-1), especially the total chemical synthesis of 96 aminoacid long Vpr protein (sVpr1-96), a 47 aminoacid long N terminal fragment (sVpr1-47) and a 49 aminoacid long C terminal fragment thereof (sVpr48-96) and to fragments sVpr1-20 and sVpr21-40, in addition to other fragments with approximately 15 aminoacids. Said products are used as HIV-1 regulatory proteins in biological assays and in the analysis of molecular structure and physico-chemical properties of Vpr and its domains or in the production of antibodies directed against Vpr-peptide sequences.
1: Russmann S, Dilger K, Trenk D, Nagyivanyi P, Jähnchen E. Effect of lysine clonixinate on the pharmacokinetics and anticoagulant activity of phenprocoumon. Arzneimittelforschung. 2001 Nov;51(11):891-5. 8: Noronha VR, Gurgel GD, Alves LC, Noman-Ferreira LC, Mendonça LL, Aguiar EG, Abdo EN. Analgesic efficacy of lysine clonixinate, paracetamol and dipyrone in lower third molar extraction: a randomized controlled trial. Med Oral Patol Oral Cir Bucal. 2009 Aug 1;14(8):e411-5. Portuguese.
合成参考文献
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