CAS: 398456-82-1; 3-Bromo-2,6-Difluorobenzaldehyde

上下游产品

CAS号348-57-2 2,4-二氟溴苯 | CAS号68-12-2 N,N-二甲基甲酰胺

1-溴-2,4-二氟苯置于盐酸,水体系中,用 苯 用作溶剂,化学反应 0.25H,反应生成3-溴-2,6-二氟苯甲醛
参考文献:苯二氨基甲基化中的潜在卡宾:机理和实际应用
标题:苯二氨基甲基化中的潜在卡宾:机理和实际应用
摘要:由于甲硅烷基团容易迁移,甲硅烷基甲脒1与其碳烯形式1'处于平衡状态.1与各种取代的氟苯的反应随着亲核卡宾1'的插入而进行在混合试剂后进入最酸性的 C-H 键,不需要任何催化剂.根据 Dft 计算,通过三元过渡态结构进行的插入反应的经典解释需要高活化能.相反,预计将芳香底物中酸性最强的质子转移到卡宾碳上的活化势垒较低.下一步,形成的离子对向产物的无障碍重排完成了该过程.取代苯在与甲硅烷基甲脒反应中的反应性可以通过计算的c-H 氢的p K A (Dmso) 值粗略评估.具有 P K A的苯衍生物约 少于 31 个可以进行 C-H 插入.该反应提供缩醛胺作为第一批产物,它可以很容易地通过酸水解转化为相应的醛.由于甲硅烷基甲脒1对许多官能团具有耐受性,该反应可应用于多种苯衍生物,使其成为有机合成应用的可靠策略.
Doi:10.1021/acs.Joc.3C00470

专利信息

专利号:US-8338451-B2
优先权日:2008-03-21
标 题 :Polysubstituted derivatives of 2-heteroaryl-6-phenylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof
发明人：DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; ALMARIO GARCIA ANTONIO
权利人:DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; ALMARIO GARCIA ANTONIO; SANOFI SA
摘要:Compounds of formula (I): n nwherein R, R 1 , R 2 , R 3 , R 4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

专利号:US-8148370-B2
优先权日:2008-03-21
标题 :Polysubstituted derivatives of 2-aryl-6-phenyl-imidazo[1,2-a]pyridines, and preparation and therapeutic use thereof
发明人：DE PERETTI DANIELLE; EVANNO YANNICK
权利人:DE PERETTI DANIELLE; EVANNO YANNICK; SANOFI AVENTIS
摘要:Compounds of formula (I): n nwherein R 1 , R 2 , R 3 , R 4 and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

专利号:US-11034695-B2
优先权日:2016-09-23
标 题:Dopamine-β-hydroxylase inhibitors
发明人：SOARES DA SILVA PATRÃ?CIO; ROSSI TINO; KISS LASZLO ERNO; BELIAEV ALEXANDER; LEAL PALMA PEDRO NUNO
权利人:BIAL—PORTELA & CA S A; BIAL—PORTELA & Cᵃ S A
摘要:This invention relates to: (a) compounds of Formula Ia (with R1, R4, R5, R6, n and A as defined herein) and pharmaceutically acceptable salts or solvates thereof that are useful as dopamine-β-hydroxylase inhibitors; (b) pharmaceutical compositions comprising such compounds, salts or solvates; (c) the use of such compounds, salts or solvates in therapy; (d) therapeutic methods of treatment using such compounds, salts or solvates; and (e) processes and intermediates useful for the synthesis of such compounds.

专利号:US-8507520-B2
优先权日:2008-03-21
标 题:Polysubstituted 2-aryl-6-phenylimidazo[1,2-A]pyridine derivatives, and preparation and therapeutic use thereof
发明人：DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; RAKOTOARISOA NATHALIE; GARCIA ANTONIO ALMARIO; MALANDA ANDRE
权利人:DE PERETTI DANIELLE; EVANNO YANNICK; LARDENOIS PATRICK; RAKOTOARISOA NATHALIE; GARCIA ANTONIO ALMARIO; MALANDA ANDRE; SANOFI SA
摘要:Compounds of formula (I): n nwherein R, R 1 , R 2 , R 3 , R 4 , and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

专利号:US-9446047-B2
优先权日:2013-09-10
标 题 :Substituted 2,3-dihydro-1H-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis
发明人：VANKAYALAPATI HARIPRASAD; YERRAMREDDY VENKATAKRISHNAREDDY
权利人:ARRIEN PHARMACEUTICALS LLC
摘要:The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor γt (RORγt)/RORγ. The compounds of the present invention are useful for modulating RORγt)/RORγ activity and for treating diseases or conditions mediated by RORγt)/RORγ such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.

专利号:US-8378104-B2
优先权日:2010-02-11
标 题 :7-aminofuropyridine derivatives
发明人：HORNBERGER KEITH R; BERGER DAN M; CHEN XIN; CREW ANDREW P; DONG HANQING; KLEINBERG ANDREW; LI AN-HU; MA LIFU; MULVIHILL MARK J; PANICKER BIJOY; SIU KAM W; STEINIG ARNO G; TARRANT JAMES G; WANG JING; WENG QINGHUA; SANGEM RAJARAM; GUPTA RAMESH C
权利人:OSI PHARMACEUTICALS LLC; HORNBERGER KEITH R; BERGER DAN M; CHEN XIN; CREW ANDREW P; DONG HANQING; KLEINBERG ANDREW; LI AN-HU; MA LIFU; MULVIHILL MARK J; PANICKER BIJOY; SIU KAM W; STEINIG ARNO G; TARRANT JAMES G; WANG JING; WENG QINGHUA; SANGEM RAJARAM; GUPTA RAMESH C
摘要:Compounds of Formula 1, as shown below and defined herein: n n n n n n n n n n n n pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.