CAS: 1352492-08-0; Methyl 4'-(Dibromomethyl)-[1,1'-Biphenyl]-2-Carboxylate

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4'-甲基联苯-2-羧酸甲酯 Methyl 4'-Methylbiphenyl-2-Carboxylate 114772-34-8

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    📜4'-甲基联苯-2-羧酸甲酯置于1,3-二溴-5,5-二甲基海因,偶氮二异丁腈体系中,用 氯仿 用作溶剂,以92.6%的收率获得4'-溴甲基-2-甲酸甲酯联苯
    参考文献:An Efficient And Impurity-Free Process For Telmisartan: An Antihypertensive Drug
    标题:An Efficient And Impurity-Free Process For Telmisartan: An Antihypertensive Drug
    摘要:Telmisartan (1),A Substituted Dibenzimidazole Derivative,Is An Antihypertensive Drug,Essentially Used To Control Blood Pressure. An Improved,Cost-Effective,And Impurity-Free Process For Telmisartan (1) Suitable For Large-Scale Production Is Described Here By Addressing Various Process Development Issues. The Overall Yield Obtained From This Newly Developed Process Is Around 50% (Over Five Steps) Compared To The Literature Reported Process (21%,Over Eight Steps).
    Doi:10.1021/op060200G

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    专利信息


    专利号:US-11566004-B2
    优先权日:2018-07-23
    标题 :Process for the preparation of bromodomain inhibitor
    发明人:TRAVERSE JOHN FITZGERALD; YONG KELVIN HIN-YEONG; FERRETTI ANTONIO CHRISTIAN; ALITE HEKLA; MOSELEY JONATHAN; RUDA ANTONIO MARIA; PRIMER DAVID; PHILP STEVEN
    权利人:CELGENE QUANTICEL RES INC
    摘要:The present invention provides processes of synthesis and purification of a bromodomain inhibitor, Compound 1, which compound includes crystalline forms, amorphous forms, solvates, and hydrates thereof. Embodiments of the disclosure relate to chemical synthesis routes of Compound 1 that provide a scalable method that results in highly pure final product. A further embodiment relates to methods to isolate the most stable polymorph of Compound 1 by crystallization from formic acid and water.

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