TBSOTf-promoted versatile N-formylation using DMF at room temperature
摘要:
Hydrazides and amines were N-formylated by DMF in the presence of tert-butyldimethylsilyl triflate (TBSOTf) at room temperature, in good to excellent yields. (C) 2019 Elsevier Ltd. All rights reserved.
The present invention provides a pharmaceutical composition for use as art NPY Y5 receptor antagonist comprising a compound or the formula (I):
wherein R
1
is lower alkyl, cycloalkyl or the like,
R
2
is hydrogen, lower alkyl or the like,
n is 1 or 2,
X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like,
Y is CONR
7
, CSNR
7
, NR
7
CO, NR
7
CS or the like,
Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R
7
is hydrogen or lower alkyl,
prodrug, pharmaceutically acceptable salt or solvate thereof.
N-Heterocyclic carbene supported zinc catalysed <i>N</i>-formylation of diverse N–H functionalities with carbon dioxide under ambient conditions
作者:Sangita Sahoo、Subarna Manna、Arnab Rit
DOI:10.1039/d3cy00401e
日期:——
A heteroditopic NHC ligand supported Zn-catalysed RT N-formylation of diverse N–H moieties with CO2 (1 bar) using PhSiH3 was developed, which offers excellent functional group tolerance, chemoselectivity, and synthons for biologically relevant compounds.