Compounds having the formula I wherein R
1
, R
2
, R
3
, R
4a
, R
4b
, R
4c
, R
5
, R
6
, R
9
and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
A novel route for the direct synthesis of secondary amides from aldehydes
作者:Saad S. Elmorsy、Mohamed A. Nour、Ezzat M. Kandeel、Andrew Pelter
DOI:10.1016/s0040-4039(00)74340-1
日期:1991.4
We describe a unique, general redox process for the preparation of secondary amides by the interaction of aldehydes and nitriles in the presence of two equivalents of iodotrichlorosilane (ITCS).
acetyl and dimethylamine gas in the presence of N,N-carbonyldiimidazole (CDI). Addition of amines to the reaction mixture delivers the corresponding amides in good to excellent yields. The acetylation of amines reported herein, which relies on the in situ generation of N-acetylimidazole on warming of DMAc with CDI at 120–125 °C, serves as a convenient alternative to other acetylation methods.
The present invention provides a compound represented by the formula:
wherein R
1
is an acyl group, R
2
is a hydrocarbon group which may be substituted or the like, R
3
is a hydrocarbon group which may be substituted or the like, R
4
is a hydrocarbon group which may be substituted or the like, n is from 0 to 4, and X is an oxygen atom, a sulfur atom or the like, or a salt thereof. The invention also provides a compound which has a TGR23 antagonist activity and thus is useful for prevention and treatment of cancer.