Simultaneous dehalogenation and hydrogenation reduction of halogen-heteroaromatic aldehydes
摘要:
Treatment of halogen-heteroaromatic aldehydes with catalytic amount of PdCl2 under atmosphere pressure of hydrogen in base medium (sodium acetate) leads to the corresponding dehalogenated primary alcohols. The reaction system was especially effective for the heteroaromatic compounds bearing aldehyde groups and halides (bromo- or chloro-functions). Crown Copyright (C) 2012 Published by Elsevier Ltd. All rights reserved.
The present invention provides a process for preparing a heterocyclic aldehyde by oxidizing a heterocyclic alcohol with high selectivity and high yield. Specifically, the heterocyclic aldehyde is prepared by reacting a heterocyclic compound having at least one hydroxymethyl group bonded to a carbon atom of a heterocyclic ring with a hypohalogenous acid salt in the presence of a base to oxidize the hydroxymethyl group, wherein reaction is conducted in the co-presence of a 2,2,6,6-tetramethylpiperidine-1-oxyl derivative having at least two 2,2,6,6-tetramethylpiperidine-1-oxyl-4-yl groups.
Imidazonaphthyridine ring systems substituted with an aryl substituent, pharmaceutical compositions containing the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
The present invention relates to new compounds of general formula (I), wherein the groups R
1
to R
3
, X
1
, X
2
, X
3
and L
1
are defined as in claim
1
, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.
ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
申请人:Vertex Pharmaceuticals Incorporated
公开号:US20140038936A1
公开(公告)日:2014-02-06
The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Isoindolinone inhibitors of phosphatidylinositol 3-kinase
申请人:Vertex Pharmaceuticals Incorporated
公开号:US10183933B2
公开(公告)日:2019-01-22
The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.