CAS: 680596-79-6; 4,4,5,5-Tetramethyl-2-(1,4-Dioxaspiro[4.5]Dec-7-En-8-yl)-1,3,2-Dioxaborolane

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1,4-环己二酮单乙二醇缩酮置于(1,1'-Bis(Diphenylphosphino)Ferrocene)Palladium(II) Dichloride,2,6-二叔丁基-4-甲基吡啶,Potassium Acetate体系中,用 1,4-二氧六环,二氯甲烷 作为反应溶剂,化学反应 32.0H,反应生成 1,4-二氧杂-螺[4,5]癸-7-烯-8-硼酸频哪醇酯
参考文献:开发强效吲哚胺 2,3-双加氧酶 1 (Ido1) 抑制剂 Bmt-297376 的立体选择性和可扩展合成;n-((R)-1-((顺式)-4-(3-(二氟甲基)-2-甲氧基吡啶-4-基)环己基)丙基)-6-甲氧基烟酰胺
标题:开发强效吲哚胺 2,3-双加氧酶 1 (Ido1) 抑制剂 Bmt-297376 的立体选择性和可扩展合成;n-((R)-1-((顺式)-4-(3-(二氟甲基)-2-甲氧基吡啶-4-基)环己基)丙基)-6-甲氧基烟酰胺
摘要:目前的工作描述了一种立体选择性和可扩展的路线,用于n-((R)-1-((顺式)-4-(3-(二氟甲基)-2-甲氧基吡啶-4-基)环己基)丙基)-6-甲氧基烟酰胺 (1) 来自容易获得的 1,4-二氧杂螺[4.5] Decan-8-One.开发的工艺包括(反式)-4-(3-(二氟甲基)-2-甲氧基吡啶-4-基)环己基甲磺酸酯的有效 1,4-反式选择性合成作为关键中间体,并使用 Ellman 亚磺胺方法以立体选择性方式安装烷基胺.筛选了各种合成路线以实现立体选择性和可扩展的协议来访问标题化合物 (1).这一进步使得以对映选择性,安全,经济高效和可扩展的方式获得标题化合物的有效途径成为可能.
DOI:10.1021/acs.Oprd.1C00142

专利信息

专利号:US-9708336-B2
优先权日:2014-01-22
标题 :Metallo-beta-lactamase inhibitors
发明人：MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

专利号:US-9096624-B2
优先权日:2009-06-01
标 题:Amino pyrimidine anticancer compounds
发明人：CREW ANDREW P; SHERMAN DAN; APPARI RAMA DEVI; CHEN XIN; CHILUKURI RAMESH; DONG HANQING; FERRARO CATERINA; FOREMAN KENNETH; GUPTA RAMESH C; LI AN-HU; STOLZ KATHRYN M; VOLK BRIAN; ZAHLER ROBERT
权利人:OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula 1, as shown below and defined herein: n n n n n n n n n n n n and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.