相似化合物
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CAS号600-21-5 N-甲基-DL-丙氨酸 | CAS号56428-90-1 Alanine, N-meth... | CAS号16752-54-8 2-(甲基氨基)丙腈 | CAS号600-21-5 N-甲基-DL-丙氨酸 | CAS号95455-39-3 4-Imidazolidino...📜N-Methylalanin置于氨体系中,用 甲醇 作为反应溶剂,化学反应生成 N~2~-甲基丙氨酸酰胺
参考文献:ω-(对硝基苯基)-乙内酰胺酰胺环化的动力学和机理:质子转移的位阻导致速率变化10(4)倍.
标题:ω-(对硝基苯基)-乙内酰胺酰胺环化的动力学和机理:质子转移的位阻导致速率变化10(4)倍.
摘要:环化2,3-二甲基和2,2,3-三甲基乙内酰胺(分别为2-Uam和3-Uam)的ph速率曲线与相应的n-甲基化酰胺2环化的ph速率曲线显着不同2-Muam和3-Muam; 其中水反应占主导地位,跨越约6个ph单位.对于uam的环化,平台期不超过两个ph单位.差异是由于n-甲基酰胺的碱催化环化较慢.该氢氧化物催化的反应的溶剂动力学同位素效应接近1.2,这与带负电荷的四面体中间体的氨基的水质子化缓慢相一致.使用最多8个pkbh的碱可以观测到一般的碱催化作用.brønstedbeta与gbc的氢键作用机理兼容.在宝石二甲基化合物3中,离去基团的两侧是取代基.3-Muam中的n-甲基会阻碍质子的正面进入,从而导致速率降低14000倍.这是在2位上有一个甲基的化合物中的3800倍.
DOI:10.1039/b211040G
专利信息
专利号:US-2024066133-A1
优先权日:2020-03-06
标 题 :Therapeutic agents and conjugates thereof
发明人:SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.