2-Hydroxyethanesulphonyl chloride: a sulphonyl chloride with a primary hydroxy-group
作者:James F. King、John H. Hillhouse
DOI:10.1039/c39810000295
日期:——
The preparation of 2-hydroxyethanesulphonylchloride (1), the first example of compound containing both sulphonylchloride and primary alcohol functions, is described; reaction of (1) with base gives products evidently derived from the sulphene (4) and the β-sultone (6).
The present invention provides a novel piperidine derivative and a tachykinin receptor antagonist containing same, as well as a compound represented by the formula:
wherein R
1
is carbamoylmethyl, methylsulfonylethylcarbonyl and the like; R
2
is methyl or cyclopropyl; R
3
is a hydrogen atom or methyl; R
4
is a chlorine atom or trifluoromethyl; R
5
is a chlorine atom or trifluoromethyl; and a group represented by the formula:
is a group represented by the formula:
wherein R
6
is a hydrogen atom, methyl, ethyl or isopropyl; R
7
is a hydrogen atom, methyl or a chlorine atom; and R
8
is a hydrogen atom, a fluorine atom, a chlorine atom or methyl; or 3-methylthiophen-2-yl, and a salt thereof.
A compound of the formula (I):
1
wherein R
1
is hydrogen or lower alkyl;
R
2
is lower alkyl, etc.;
R
3
is lower alkoxy, etc.;
R
4
is hydroxy, etc.;
X is O, S, etc.;
Y is CH or N;
Z is lower alkylene or lower alkenylene; and
m is 0 or 1; or salts thereof, which are useful as a medicament.
[EN] 1 H-PYRAZOLO[4,3-G]ISOQUINOLINE AND 1 H-PYRAZOLO[4,3-G]QUINOLINE DERIVATIVES AS ALPHA-1 -ANTITRYPSIN MODULATORS FOR TREATING ALPHA-1 -ANTITRYPSIN DEFICIENCY (AATD)<br/>[FR] DÉRIVÉS DE 1H-PYRAZOLO [4,3-G] ISOQUINOLÉINE ET DE 1H-PYRAZOLO [4,3-G] QUINOLÉINE EN TANT QUE MODULATEURS D'ALPHA-1-ANTITRYPSINE POUR TRAITER UNE DÉFICIENCE EN ALPHA-1-ANTITRYPSINE (AATD)
申请人:VERTEX PHARMA
公开号:WO2021203025A1
公开(公告)日:2021-10-07
1H-pyrazolo[4,3-g]isoquinoline and 1H-pyrazolo[4,3-g]quinoline derivatives as alpha-1-antitrypsin modulators for treating alpha-1- antitrypsin deficiency (AATD).
The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR enzyme and are useful in the treatment of FGFR-associated diseases such as cancer.