📜间二三氟甲苯置于lithium Diisopropyl Amide体系中,用 四氢呋喃,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 2,4-双(三氟甲基)苯甲醛 参考文献:Process For Lithiation Of 1,3-Bis(Trifluoromethyl)Benzene 标题:Process For Lithiation Of 1,3-Bis(Trifluoromethyl)Benzene 摘要:描述了一种在溶剂中对1,3-双(三氟甲基)苯进行锂化的新工艺,该工艺包括使用通式r.Sup.1 R.Sup.2 Nh I的胺的锂盐进行锂化,其中r.Sup.1和r.Sup.2是次级或三级低级烷基或由低级烷基或低级环烷基或由低级烷基取代的低级环烷基取代的次级或三级低级烷基,或者r.Sup.1和r.Sup.2共同形成一个c.Sub.6-14-亚烷基基团,其中与氮原子连接的两个碳原子是次级或三级,并且彼此之间由2至4个碳原子隔开.所获得的锂化1,3-双(三氟甲基)苯溶液可以与适合取代锂代苯衍生物的亲电子体反应,从而获得具有以下公式的化合物##str1##,其中r.Sup.3表示适合取代锂代苯衍生物的亲电子体的残基.
专利号:US-9597327-B2 优先权日:2005-05-25 标 题:Synthesis of (R)-N-methylnaltrexone 发明人:DOSHAN HAROLD D; PEREZ JULIO 权利人:PROGENICS PHARM INC 摘要:This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
专利号:US-2022064167-A1 优先权日:2018-05-17 标 题 :Imidazo-pyrazole carboxamide derivatives as anticancer agents and the synthesis thereof 发明人:DEMJÉN ANDRÃ?S; Puskás László; KANIZSAI IVAN; SZEBENI GÃ?BOR; ANGYAL ANIKÓ; GYURIS Márió; Hackler László 权利人:AVIDIN KFT 摘要:The present invention relates to novel imidazo[1,2-b]pyrazole carboxamide and carbothioamide derivatives of general formula (V), and the advantageous derivatives and pharmaceutically acceptable salts thereof, the synthesis thereof, and medicinal and/or pharmaceutical composition comprising these compounds thereof and synthesis thereof, and for use as a medicament, for use in the treatment of different diseases, advantageously of cancer. The subject compounds are advantageously for use in the treatment of solid malignancies, advantageously breast, lung, melanoma, gliomas, and myeloproliferative and myelodysplastic neoplasms, acute myelogenous/myeloid leukemias and colon cancer by the differentiation and subsequent apoptosis of pre-matured myeloid leukemic cells or myeloid-derived suppressor cells and/or by direct effect on solid tumors.
专利号:US-7674904-B2 优先权日:2005-05-25 标 题 :Synthesis of R-N-methylnaltrexone
专利号:US-2007099946-A1 优先权日:2005-05-25 标 题:Synthesis of R-N-methylnaltrexone
专利号:US-4035405-A 优先权日:1976-07-09 标题 :Novel synthesis for preparing the hydrochloride salt of selected catecholamine derivatives 发明人:BODOR NICOLAE S; YUAN SUN-SHINE 权利人:INTERX RESEARCH CORP 摘要:Compounds of the formula: ##STR1## wherein R represents a straight or branched C 1 -C 5 alkyl group; and R 1 in each occurrence represents an acyl member which is alkanoyl having 1-22 carbon atoms, alkenoyl having one or two double bonds and having 4-22 carbon atoms, ##STR2## having a total of 4-10 carbon atoms of which 3-7 are ring carbon atoms in cycloalkyl and wherein n is zero, one, or two, phenoxyacetyl, naphthalenecarbonyl, pyridinecarbonyl, ##STR3## wherein n is zero, one or two and phenyl is unsubstituted or is substituted by 1-3 alkyl having 1-4 carbon atoms, alkoxy having 1-4 carbon atoms, halo, trifluoromethyl, dialkylamino having 2-8 carbon atoms, or alkanoylamino having 1-6 carbon atoms groups; are prepared in substantial purity and yield, using as the chloride ion donor, cesium chloride (CsCl). n The compounds prepared by the process claimed herein exhibit sympathomimetic activity and are thus useful in eliciting sympathomimetic responses in warm-blooded animals, e.g., reduction in intraocular pressure, miosis, mydriasis, bronchodilation, etc.
专利号:US-2013323286-A1 优先权日:2005-05-25 标题 :Synthesis of r-n-methylnaltrexone
[参考文献]: Albrecht Berkessel, Et Al. Umpolung By N-Heterocyclic Carbenes: Generation And Reactivity Of The Elusive 2,2-Diamino Enols (Breslow Intermediates). Angew Chem Int Ed Engl. 2012 Dec 3;51(49):12370-4.
合成参考文献
摘要:Davies, A. T.; Smith, A. D., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 2, 405. 参考文献:10.1107/s1600536810025493 摘要:Naveenkumar HS, Sadikun A, Ibrahim P, Yeap CS, Fun HK. Bis{(E)-N'-[2,4-bis(trifluoro-meth-yl)benzyl-idene]isonicotinohydrazide} monohydrate. Acta Crystallogr Sect E Struct Rep Online. 2010 Jul 03;66(Pt 8):o1918–9.