SUBSTITUTED PYRAZOLES AS HUMAN PLASMA KALLIKREIN INHIBITORS
申请人:BioCryst Pharmaceuticals, Inc.
公开号:EP3828173A1
公开(公告)日:2021-06-02
Disclosed are compounds of formula (I), as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention and the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Visible-Light-Mediated Umpolung Reactivity of Imines: Ketimine Reductions with Cy<sub>2</sub>NMe and Water
作者:Rui Wang、Mengyue Ma、Xu Gong、Grace B. Panetti、Xinyuan Fan、Patrick J. Walsh
DOI:10.1021/acs.orglett.8b00778
日期:2018.4.20
carbanionic reactivity of imines mediated by photoredox catalysis is demonstrated. The umpolung imine reactivity is exemplified by proton abstraction from water as a key step in the reduction of benzophenone ketimines to amines (up to 98% yield). Deuterium is introduced into amines efficiently using D2O as an inexpensive deuterium source (≥95% D ratio). The mechanism of this unusual transformation