1-t-Butyl- and 1-(4-methylbenzyl)-3-bromo-3-methylazetidines were prepared from the corresponding N-(2,3-dibromo-2-methylpropylidene)alkylamines and their propensity to undergo nucleophilic substitution at the 3-position by different nucleophiles was assessed, providing a convenient access to novel 3-alkoxy-, 3-aryloxy-, 3-hydroxy-, 3-cyano-, 3-carboxy-, 3-(aminomethyl)- and 3-(hydroxymethyl)azetidines. (C) 2011 Elsevier Ltd. All rights reserved.
Synthesis and reactivity of non-activated 2-(chloromethyl)aziridines
作者:Sonja Stanković、Matthias D’hooghe、Jo Dewulf、Piet Bogaert、Robrecht Jolie、Norbert De Kimpe
DOI:10.1016/j.tetlet.2011.06.062
日期:2011.8
efficient synthesis of non-activated 2-(chloromethyl)aziridines and 2-chloromethyl-2-methylaziridines as new representatives of the class of 2-(halomethyl)aziridines was developed. Furthermore, the reactivity of these azaheterocycles was assessed and compared to that of their brominated counterparts, pointing to a similar profile for 2-(chloromethyl)aziridines and 2-(bromomethyl)aziridines on the one
The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula I-I all have the meaning as defined herein.
The invention provides novel compounds having the general formula:
and tautomers and pharmaceutically acceptable salts thereof, wherein A
1
, A
2
, A
3
, A
4
, R
1
, R
4
, R
5
, R
6
, R
7
and R
8
are as defined herein, compositions including the compounds and methods of using the compounds.
BENZOFURAN ANALOGUE AS NS4B INHIBITOR
申请人:CHANGZHOU YINSHENG PHARMACEUTICAL CO., LTD.
公开号:US20170240519A1
公开(公告)日:2017-08-24
Provided is a benzofuran analogue having a structure represented by formula (I) and used as an NS4B inhibitor, or a pharmaceutically acceptable salt of the benzofuran analogue. The benzofuran analogue has anti-hepatitis C virus activity.
BIHETEROARYL COMPOUNDS AND USES THEREOF
申请人:Genentech, Inc.
公开号:US20200188397A1
公开(公告)日:2020-06-18
The present invention provides for compounds of Formula I-I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R
1
, R
2
, R
3
, X
1
, X
2
, A and Cy variable in Formula I-I all have the meaning as defined herein.