通过使用碘基苯作为无毒的碘(III)基氧化剂和碘化铵作为廉价的碘原子源,开发了一种用于亲电子碘化苯酚的氧化方法。通过用K 3 PO 4缓冲反应介质来实现完全受控的单碘化。在温和的温度下,在开放的烧瓶中,该方案以较短的反应时间进行,并且通常收率很高。用富电子和贫电子的酚以及杂环探索了革兰氏反应以及该方案的范围。量子化学计算显示,PhII(OH)·NH 3是最可能的碘化活性物质,呈反应性“ I +synthon。鉴于碘代芳烃部分的相关性,我们在本文中提出了实用,有效和简单的方法,其具有允许进入碘代芳烃核心单元的宽泛的官能团范围。
[EN] INDOLE-DERIVATIVE MODULATORS OF STEROID HORMONE NUCLEAR RECEPTORS<br/>[FR] MODULATEURS A BASE DE DERIVES INDOLIQUES DES RECEPTEURS NUCLEAIRES DES HORMONES STEROIDES
申请人:LILLY CO ELI
公开号:WO2004067529A1
公开(公告)日:2004-08-12
The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient, and methods for treating physiological disorders, particularly congestive heart disease, comprising administering to a patient in thereof an effective amount of a compound of Formula I.
MACROLIDE DERIVATIVES, PREPARATION METHOD AND APPLICATION THEREOF
申请人:Zhejiang Hisun Pharmaceutical Co., Ltd.
公开号:EP3974434A1
公开(公告)日:2022-03-30
Provided are a macrolide derivative represented by formula (I), a preparation method thereof, and an application of the macrolide derivative as an inhibitor of one or more protein kinases of TRK, ALK and ROS1,
[EN] MACROLIDE DERIVATIVES, PREPARATION METHOD AND APPLICATION THEREOF<br/>[FR] DÉRIVÉS DE MACROLIDES, LEUR PROCÉDÉ DE PRÉPARATION ET LEUR APPLICATION<br/>[ZH] 大环类衍生物、及其制备方法和用途