CAS: 376584-62-2; 5-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Isoindolin-1-One

该化合物是有机合成中常用的多功能中间体的异丙二醇衍生物,特别是在铃木-米亚乌拉交叉组合反应中,其稳定的四代二氧二氧基会同质会比免费的松酸能增加处理和储存,提供更好的空气和湿度稳定性.异丁酮核心提供硬性剑架,促进制药和材料化学应用的选择性功能化.该化合物因其与多种反应条件的兼容性及其在构建复杂循环框架中的作用而受到重视.其高纯度和清晰的结构使它成为精确合成工作流程的可靠试剂.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    📜4-溴-2-甲基苯甲酸置于四(三苯基膦)钯 盐酸,N-溴代丁二酰亚胺(Nbs),氨,Potassium Acetate,过氧化苯甲酰体系中,用 甲醇,四氯化碳,N,N-二甲基甲酰胺 用作溶剂,化学反应 52.17H,反应生成1-异吲哚酮-5-硼酸频哪醇酯
    参考文献: Biaryl Phosphodiesterase Inhibitors[fr] Inhibiteurs Biaryle Des Phosphodiestérases
    标题: Biaryl Phosphodiesterase Inhibitors[fr] Inhibiteurs Biaryle Des Phosphodiestérases
    摘要:具有磷酸二酯酶抑制活性的新型联苯化合物,其一般化学式为(i),其中r1,R2,R3,X,Y,Z1,Z2,Z3和z4具有本文中定义的含义,以及它们作为治疗炎症性疾病和症状的治疗剂的用途.

    海关参考信息

    专利信息


    专利号:US-11020399-B2
    优先权日:2011-05-04
    标 题:Intermediates useful in the synthesis of compounds as modulators of protein kinases

    专利号:US-9795613-B2
    优先权日:2014-12-10
    标题 :GLP-1 receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK
    权利人:CELGENE INT II SÀRL
    摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

    专利号:US-9187522-B2
    优先权日:2011-12-12
    标题 :GLP-1 receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL
    权利人:RECEPTOS INC
    摘要:The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

    专利号:US-9598430-B2
    优先权日:2013-06-11
    标 题 :GLP-1 receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL
    权利人:RECEPTOS INC; CELGENE INT II SÀRL
    摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

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