CAS: 6436-59-5; Ethyl 2-Methylthiazole-4-Carboxylate

2-Acetylamino-3-Oxo-Propionic Acid Ethyl Ester置于劳森试剂体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 12.0H,反应生成 2-甲基噻唑-4-甲酸乙酯
参考文献:使用c-甲酰化策略从常见的无环前体合成咪唑,恶唑,噻唑和2,5-二羧酸吡嗪二乙酯的取代酯
标题:使用c-甲酰化策略从常见的无环前体合成咪唑,恶唑,噻唑和2,5-二羧酸吡嗪二乙酯的取代酯
摘要:报道了一种通过甘氨酸乙酯盐酸盐的c-甲酰化反应合成咪唑,恶唑,噻唑和吡嗪-2,5-二羧酸二乙酯的取代酯的新颖合成途径.该方法简单,稳健,并且可以在一个或两个步骤中从常见的无环前体中很好地获得不同杂环酯的收率,并且适合大规模合成.
DOI:10.1016/j.Tetlet.2014.03.039

专利信息

专利号:US-9475814-B2
优先权日:2011-10-03
标题:Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
发明人：HOVEYDA HAMID R; DUTHEUIL GUILLAUME; FRASER GRAEME L; ROY MARIE-ODILE; EL BOUSMAQUI MOHAMED; BATT FREDERIC
权利人:EUROSCREEN SA
摘要:The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.

专利号:US-11267824-B2
优先权日:2017-08-17
标 题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase
发明人：BOSS CHRISTOPH; BUR DANIEL; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI
权利人:IDORSIA PHARMACEUTICALS LTD
摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in inter alia cancer is disclosed.

专利号:US-2003069277-A1
优先权日:1996-12-03
标 题 :Synthesis of epothilones, intermediates thereto and analogues thereof

专利号:US-11267820-B2
优先权日:2015-09-09
标 题 :Tricyclic fused pyridin-2-one derivatives and their use as BRD4 inhibitors
发明人：VADIVELU SARAVANAN; RAJAGOPAL SRIDHARAN; RAMAIAH MANJUNATHA M; GONDRALA PAVAN KUMAR; CHINNAPATTU MURUGAN; SIVANANDHAN DHANALAKSHMI; PARIKH PAYAL KIRAN; MULAKALA CHANDRIKA
权利人:JUBILANT BIOSYS LTD
摘要:The present disclosure describes heterocyclic compounds of Formula I or, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms and pharmaceutically active derivatives thereof and pharmaceutical compositions containing them as the active ingredient. The present disclosure also describes the synthesis and characterization of aforementioned compounds to exhibit high anticancer activity. The compounds of the present disclosure are useful as medicaments and their use in the manufacture of medicaments for treatment, prevention, or suppression of diseases, an conditions mediated b one or more BET family of bromodomains.

专利号:RU-2195454-C2
优先权日:1996-10-18
标 题 :Derivatives of anthranilic acid, methods of their synthesis and pharmaceutical composition based on thereof

专利号:MX-2014004057-A
优先权日:2011-10-03
标题:N-ACIL-5,6,7, (8-REPLACED) -TETRAHYDRO- [1,2,4] TRIAZOLO [4,3-A] PIRA QUIRAL ZINAS, NOVEDOSAS, AS SELECTIVE ANTAGONISTS OF NK-3 RECEPTOR; PHARMACEUTICAL COMPOSITION, METHODS FOR USE IN DISORDERS MEDIATED BY NK-3 RECEPTOR AND ITS CHIRAL SYNTHESIS.