Substituted 4-Amino-Quinazoline Compounds with Metabotropic Glutamate Receptor Regulating Activity and Uses Thereof
申请人:REICH Melanie
公开号:US20090069320A1
公开(公告)日:2009-03-12
Substituted 4-amino-quinazoline compounds corresponding to formula I
methods for their production, pharmaceutical compositions containing these compounds as active agents, and the uses thereof for treating or inhibiting disorders or disease states.
Efficient conversion of acids and esters to amides and transamidation of primary amides using OSU-6
作者:Baskar Nammalwar、Nagendra Prasad Muddala、Field M. Watts、Richard A. Bunce
DOI:10.1016/j.tet.2015.10.016
日期:2015.12
with strong Bronsted acid properties, has been used to promote the high-yield conversion of carboxylic acids and esters to carboxamides as well as transamidations of primary amides in a one-pot solventless approach. A metal-free heterogeneous catalyst that promotes all of these processes has not been previously reported. OSU-6 enables these transformations to proceed in shorter times and at lower temperatures
The present invention relates to 1-[m-Carboxamido(hetero)aryl-methyl]-piperidine-4-carboxamide derivatives of formula (I)
wherein X, Ar
1
, R
1
, R
2
, R
3
, R
4
, R
5
and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
A compound according to Formula A:
or a pharmaceutically acceptable salt thereof, wherein
R
11
, G
1
and G
2
are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
Metal-Free Difunctionalization of Pyridines: Selective Construction of <i>N</i>-CF<sub>2</sub>H and <i>N</i>-CHO Dihydropyridines
作者:Sen Zhou、Ze-Ying Sun、Kongying Zhu、Wentao Zhao、Xiangyang Tang、Minjie Guo、Guangwei Wang
DOI:10.1021/acs.orglett.1c00352
日期:2021.3.19
N-difluoromethylpyridinium salts is seldom explored because of their instability and low availability. Here we present a novel nucleophilic addition of N-difluoromethylpyridinium salts with nitroalkanes to synthesize N-CF2H-dihydropyridines and N-CHO-dihydropyridines in a highly efficient and regioselective pathway. This protocol exhibits good functional group tolerance and good to excellent yields.