Synthesis of 1-Substituted Cyclopropylamines via Formal Tertiary C<sub>sp<sup>3</sup></sub>–H Amination of Cyclopropanes
作者:Kui Liu、Shao-Jie Cheng、Gen Luo、Zhi-Shi Ye
DOI:10.1021/acs.orglett.1c03687
日期:2021.12.3
A novel and facile approach to synthesis of 1-substituted cyclopropylamines via phosphine-catalyzed formal tertiary Csp3–H amination of cyclopropanes was described. The indoles, pyrroles, imidazoles, uracils, 2-pyridone, pyrimidin-4(3H)-one, and phthalimide had been proven as good aminating partners. The present protocol features transition-metal-free, excellent regioselectivity, high-atom-economy
描述了一种通过膦催化环丙烷的形式叔 C sp 3 -H 胺化合成 1-取代环丙胺的新方法。吲哚类、吡咯类、咪唑类、尿嘧啶类、2-吡啶酮、pyrimidin-4(3 H)-one,邻苯二甲酰亚胺已被证明是良好的胺化伙伴。本协议具有无过渡金属、优异的区域选择性、高原子经济性、温和的反应条件和广泛的底物。该协议的实用性还可以通过生物活性分子的后期修饰、放大反应和发散衍生化来证明。值得注意的是,该方法已用于激素敏感性脂肪酶 (HSL) 抑制剂的正式合成。通过实验和计算研究阐明了机械方面。
PPAR active compounds
申请人:Lin Jack
公开号:US20060116416A1
公开(公告)日:2006-06-01
Compounds are described that are active on at least one of PPARα, PPARδ, and PPARγ, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPARα, PPARδ, and PPARγ.
INDOLE DERIVATIVES FOR USE AS PPAR ACTIVE COMPOUNDS
申请人:PLEXXIKON, INC.
公开号:EP1819673A2
公开(公告)日:2007-08-22
US7531568B2
申请人:——
公开号:US7531568B2
公开(公告)日:2009-05-12
[EN] PPAR ACTIVE COMPOUNDS<br/>[FR] COMPOSES ACTIFS SUR LES PPAR
申请人:PLEXXIKON INC
公开号:WO2006060456A2
公开(公告)日:2006-06-08
[EN] Compounds are described that are active on at least one of PPARa, PPARd, and PPAR?, which are useful for therapeutic and /or prophylactic methods involving modulation of at least one of PPARa, PPARd, and PPAR?. [FR] L'invention concerne des composés qui sont actifs sur au moins un des éléments suivants : PPARa, PPARd et PPAR?. Ces composés sont destinés à être utilisés dans des méthodes de traitement et/ou de prévention impliquant une modulation d'au moins un desdits éléments, à savoir : PPARa, PPARd et PPAR?.