Oxalic Diamides and <i>tert</i>-Butoxide: Two Types of Ligands Enabling Practical Access to Alkyl Aryl Ethers via Cu-Catalyzed Coupling Reaction
作者:Zhixiang Chen、Yongwen Jiang、Li Zhang、Yinlong Guo、Dawei Ma
DOI:10.1021/jacs.8b12142
日期:2019.2.27
A robust and practical protocol for preparing alkyl aryl ethers has been developed, which relies on using two types of ligands to promote Cu-catalyzed alkoxylation of (hetero)aryl halides. The reaction scope is very general for a variety of coupling partners, particularly for challenging secondary alcohols and (hetero)aryl chlorides. In case of coupling with aryl chlorides and bromides, two oxalic
已经开发了一种用于制备烷基芳基醚的稳健实用的方案,该方案依赖于使用两种类型的配体来促进 Cu 催化的(杂)芳基卤化物的烷氧基化。反应范围非常适用于各种偶联伙伴,尤其是具有挑战性的仲醇和(杂)芳基氯。在与芳基氯化物和溴化物偶联的情况下,两个草酸二酰胺作为强大的配体。叔丁醇首先被证明是铜催化偶联反应的配体,导致芳基碘化物在室温下完成烷氧基化。此外,许多碳水化合物衍生物适用于该偶联反应,以 29-98% 的产率提供相应的碳水化合物-芳基醚。
The compounds of Formula (I) wherein R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
The compounds of Formula (I),
in which R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
申请人:THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
公开号:US20160194340A1
公开(公告)日:2016-07-07
The present invention is directed to arginase inhibitor compounds of formula IA or formula IB:
or a pharmaceutically acceptable salt thereof, compositions containing these compounds, and methods of their use for the treatment and diagnosis of conditions characterized by upregulation of arginase, abnormally high arginase activity, or by abnormally low nitric oxide synthase activity.
The compounds of Formula (I),
in which R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.