CAS: 393870-04-7; (4'-Methyl-[1,1'-Biphenyl]-4-yl)Boronic Acid

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4-Bromophenylboronic acid Trimethyl borate 4-bromo-4'-methylbiphenyl 4-methylphenylboronic acid

📜4-溴苯硼酸置于palladium Diacetate,2-(二环己基膦基)联苯 Sodium Hydroxide,Potassium Phosphate体系中,用 四氢呋喃,二甲基亚砜,苯 作为反应溶剂,化学反应 24.17H,反应生成 4-甲基联苯硼酸
参考文献:小分子合成的简单模块化策略:B 保护卤代硼酸构建块的迭代 Suzuki-Miyaura 偶联
标题:小分子合成的简单模块化策略:B 保护卤代硼酸构建块的迭代 Suzuki-Miyaura 偶联
摘要:我们在此描述了一种简单且高度模块化的小分子合成策略,涉及 B 保护的双功能卤代硼酸的迭代交叉偶联.启用这种方法,我们新发现硼酸通过与三价配体 N-甲基亚氨基二乙酸络合的锥体化抑制了它们对交叉偶联的反应性.该配体对无水 Suzuki-Miyaura 条件非常稳定,但使用温和的碱水溶液(1 M Naoh/thf 水溶液,10 分钟,23oc 或饱和 Nahco3/meoh 水溶液,23°C,6 小时)易于裂解.尽管芳基,杂芳基,烯基和烷基硼酸的反应性可能会有很大差异,但该方法可有效保护和去保护所有四类亲核试剂.利用这种潜力,
DOI:10.1021/ja0716204

专利信息

专利号:US-9700543-B2
优先权日:2011-05-31
标题 :GLP-1 receptor stabilizers and modulators
发明人：BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; BRAHMACHARY ENUGURTHI; YEAGER ADAM RICHARD
权利人:CELGENE INT II SÀRL
摘要:Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.