CAS: 389621-80-1; 4-(N,N-Diethylaminocarbonyl)Phenylboronic Acid

上下游产品

CAS号14047-29-1 4-羧基苯硼酸 | CAS号109-89-7 二乙胺

4-羧基苯硼酸,二乙胺置于n,N-Diethanolaminomethyl Polystyrene,水,1-羟基苯并三唑,N,N'-二异丙基碳二亚胺体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 19.02H,以59%的收率获得产物4-(N,N-二乙氨甲酰基)苯硼酸
参考文献:通用固相方法用于硼酸的固定化,衍生化和树脂到树脂的转移反应.
标题:通用固相方法用于硼酸的固定化,衍生化和树脂到树脂的转移反应.
摘要:含硼酸的分子广泛用于生物学,医学和合成领域.然而,这些化合物往往难以通过溶液相方法处理.在此,该问题通过用于官能化硼酸的衍生化的第一种通用固相方法的开发来解决.该方法基于使用二乙醇胺树脂锚,该锚通过避免在酯化过程中彻底去除水的需要而促进了硼酸的固定.通过在室温下在无水溶剂中简单搅拌,可以在数分钟内将多种硼酸固定在n,N-二乙醇氨基甲基聚苯乙烯(deam-Ps,1)上.通过(1)deam-Ps负载的对甲苯基硼酸的(1)NMR分析显示了形成具有假定的nb配位的双环二乙醇胺硼酸酯的证据.通过紫外光谱研究了deam-Ps树脂对相同型号硼酸的水解裂解.水解和附着显示在快速达到的平衡下发生,并且需要大量过量的水(> 32当量)以实现从deam-Ps实际定量释放硼酸.尽管它们对水和醇具有相对的敏感性,但可以用甲酰基,溴甲基,羧基或氨基官能化的deam-Ps结合的芳基硼酸以非常好或极高的收率转化成各种胺,酰
DOI:10.1021/jo0106501

专利信息

专利号:US-6919382-B2
优先权日:2000-08-31
标 题 :Preparation and uses of conjugated solid supports for boronic acids
发明人：HALL DENNIS G
权利人:UNIV ALBERTA
摘要:The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.

专利号:WO-2022058896-A1
优先权日:2020-09-15
标 题 :Inhibitors of low molecular weight protein tyrosine phosphatase for management of metabolic disorder
发明人：SHARMA RAJIV; KUMAR SANJAY; SRIVASTAVA BRIJESH KUMAR; GITE SANJAY; SHEDAGE SANDEEP; KADAM PRAVIN; DHOLAKIA PARIND
权利人:CADILA HEALTHCARE LTD
摘要:The present invention relates to novel modulators of low molecular weight protein tyrosine phosphatases and their use for the treatment of diseases or conditions mediated by LMPTP. Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, their safe pre-mixtures with polymers such as HPMC, HPMC-AS, Copovidone and methods for using such compounds, and pharmaceutical compositions containing them.