CAS: 402960-38-7; 5-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Pyrimidin-2-Amine

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2-氨基-5-溴嘧啶,联硼酸频那醇酯置于吩噻嗪,Caesium Carbonate体系中,用 乙腈 作为反应溶剂,化学反应 48.0H,以71%的收率获得产物2-氨基嘧啶-5-硼酸频哪酯
参考文献:C-O,C-N 和 C-X 键的可见光诱导硼化
标题:C-O,C-N 和 C-X 键的可见光诱导硼化
摘要:硼酸是中心重要的功能基序和合成前体.可见光诱导的硼酸化可以提供结构多样化的硼酸盐,但一种广泛有效的光催化硼酸化方法可以影响包括强 C-O 键在内的多种底物的硼化,仍然难以实现.在此,我们报告了一种通用的,无金属的可见光诱导光催化硼化平台,该平台能够对苯酚和苯胺,氯芳烃以及其他卤代芳烃的富电子衍生物进行硼化.该反应表现出优异的官能团耐受性,正如一系列结构复杂底物的硼化反应所证明的那样.值得注意的是,该反应是由吩噻嗪催化的,这是一种简单的有机光催化剂,Mw< 200通过质子耦合电子转移机制介导了以前无法实现的可见光诱导的苯酚衍生物单电子还原,还原电位为~-3 V Vs Sce.机理研究指出了光催化剂-碱相互作用的关键作用.
DOI:10.1021/jacs.9B12519

专利信息

专利号:US-2024199637-A1
优先权日:2021-04-21
标题 :Improved process for the preparation of 7-(morpholinyl)-2-(n-piperazinyl)methylthieno[2, 3-c]pyridine derivatives
发明人：KOMPELLA AMALA; VAGICHERLA KAMESWARA RAO; LANKI REDDY TIRUMALA REDDY; PESARU NARMADA; MUDDASANI PULLA REDDY; NANNAPANENI VENKAIAH CHOWDARY
权利人:NATCO PHARMA LTD
摘要:The present invention describes an improved second generation process for the synthesis of NRC-1111 (1,5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-7-(4-morpholinyl)thieno[2,3-c] pyridine-5-yl]-2-pyrimidinamine) dimethane sulfonate and NRC-1109 (II, 5-[3-methyl-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-7-morpholino-thieno[2,3-c]pyridin-5-yl]pyrimidin-2-amine) dimethane sulfonate. This process is cost effective, high yielding and industrially feasible process for the synthesis of compounds of formulae I and II with high purity. Formula (I) Formula (I): Râ•?H for NRC-1111 and Formula (II): Râ•?CH3 for NRC-1109 NRC-1111 and NRC-1109 are potential anti-cancer agents.