N-PROP-2-YNYL CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS
申请人:ORION CORPORATION
公开号:US20150376130A1
公开(公告)日:2015-12-31
Compounds of formula I, wherein A, B, X, Z and R
1
-R
6
, are as defined in the claims, exhibit TRPA 1 activity and are thus useful as TRPA1 modulators.
Development of a Practical Synthesis of a p38 Kinase Inhibitor via a Safe and Robust Amination
作者:Zhongping Shi、Susanne Kiau、Paul Lobben、John Hynes、Hong Wu、Luca Parlanti、Robert Discordia、Wendel W. Doubleday、Katerina Leftheris、Alaric J. Dyckman、Stephen T. Wrobleski、Konstantinos Dambalas、Srinivas Tummala、Simon Leung、Ehrlic Lo
DOI:10.1021/op300181r
日期:2012.10.19
The development of a practical synthesis for a p38 kinase inhibitor is described. The key advances include an improved route to the key intermediate, a substituted pyrrole, and a subsequent animation utilizing O-(4-nitrobenzoyl)-hydroxylamine, which provides a safe, scalable, and robust amination method. The new protocol was successfully demonstrated to generate 1.6 kg of API in seven steps and 26% overall yield.
Preparation and reactions of novel O-acylhydroxylamines
作者:William N. Marmer、Gerhard Maerker
DOI:10.1021/jo00795a028
日期:1972.11
5-Oxo-2,5,-dihydro-1,2,4-triazines, methods for their production, herbicidal compositions comprising them, and their use as herbicides