光气 反应生成 硫光气 参考文献:3-(1,2-Benzisothiazol-And Isoxazol-5-Y1)-2,4(1H,3H)-Pyrimidinedione Or Thione And 3-(1,2-Benzisothiazol-And Isoxazol-5-Y1)-4(3H)-Pyrimidinone Or Thione Herbicidal Agents 标题:3-(1,2-Benzisothiazol-And Isoxazol-5-Y1)-2,4(1H,3H)-Pyrimidinedione Or Thione And 3-(1,2-Benzisothiazol-And Isoxazol-5-Y1)-4(3H)-Pyrimidinone Or Thione Herbicidal Agents
专利号:US-9446995-B2 优先权日:2012-05-21 标 题:Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN-SOON; ILLINOIS INST OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-6207858-B1 优先权日:1999-03-03 标 题 :Regioselective synthesis of DTPA derivatives 发明人:CHINN PAUL; GYORKOS ALBERT; LABARRE MICHAEL J; RUHL STEVE; RYSKAMP THOMAS 权利人:IDEC PHARMA CORP 摘要:The present invention provides a process for high yield regioselective synthesis of DTPA derivatives that eliminates the need for ion exchange chromotographic separation of intermediates. Moreover, as this process yields a single regioisomer of the chelate, it provides for the regiospecific synthesis of desired chelates useful as radiolabeling agents.
专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-8835477-B2 优先权日:2009-10-06 标题 :Method for the synthesis of 2-thiohistidine and the like 发明人:ERDELMEIER IRÈNE; DAUNAY SYLVAIN 权利人:ERDELMEIER IRÈNE; DAUNAY SYLVAIN; TETRAHEDRON 摘要:Methods for the synthesis of 2-thiohistidine or a derivative thereof of the formula (I), or of a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions thereof, from a compound of the formula (II) or a physiologically acceptable salt, a tautomer, a stereoisomer or a mixture of stereoisomers in any proportions thereof, by cleavage reaction in the presence of a thiol at a temperature higher than or equal to 60° C. The invention also relates to compounds of the formula (II) and a method for the synthesis thereof.
摘要:Braverman, S.; Cherkinsky, M., Science of Synthesis Knowledge Updates, (2014) 3, 287. 摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2018) 3, 304. 摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2018) 3, 308. 摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2018) 3, 343. 摘要:Aitken, R. A., Science of Synthesis Knowledge Updates, (2018) 3, 354.