Carbon Nanotube-Gold Nanohybrid Catalyzed N-Formylation of Amines by using Aqueous Formaldehyde
作者:Nimesh Shah、Edmond Gravel、Dhanaji V. Jawale、Eric Doris、Irishi N. N. Namboothiri
DOI:10.1002/cctc.201402225
日期:2014.8
of a variety of primary and secondary amines by using aqueous formaldehyde at room temperature in open air affords the corresponding formamides in excellent yield under the catalytic influence of a gold–carbon nanotube nanohybrid. The reaction is also marked by excellent chemoselectivity, low catalyst loading, and recyclability of the catalyst.
Abstract A practical sodium tert-butoxide (NaOtBu)-mediated protocol is disclosed for the transamidation of various N,N-dimethyl amides with primary amines to afford the corresponding amides in moderate to good yields at room temperature under solvent-free conditions. This protocol features a facile work-up procedure and good functional group compatibility, especially for N,N-dimethyl amides with long-chain
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.
A novel method for the synthesis of formamides through the decarboxylative N-formylation of amines with glyoxylic acid has been developed. This transformation provides an efficient protocol for the synthesis of various formamides with moderate to excellent yields, and it can accommodate a wide range of functional groups under metal free and base free conditions. In addition, the large-scale experiments
The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I):
wherein R1 is lower alkyl, cycloalkyl or the like,
R2 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 CONR7, CSNR7, NR7CO, NR7CS or the like,
Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl,
prodrug, pharmaceutically acceptable salt or solvate thereof
本发明提供了一种用作 NPY Y5 受体拮抗剂的药物组合物,该组合物由式(I)化合物组成:
其中 R1 是低级烷基、环烷基或类似物、
R2 是氢、低级烷基或类似物、
n 是 1 或 2、
X 是低级烯烃、低级烯烃、芳基、环烷烃或类似物、
Y 是 CONR7、CSNR7、NR7CO、NR7CS 或类似物、
Z 是低级烷基、任选取代的碳环烷基、任选取代的杂环烷基或类似物,R7 是氢或低级烷基、
其原药、药学上可接受的盐或溶液