Metal-free C–N bond-forming reaction: straightforward synthesis of anilines, through cleavage of aryl C–O bond and amide C–N bond
摘要:
An efficient metal-free C-N bond forming reaction through cleavage of aryl C-O bond and amide C-N bond has been developed. This process represents a practical method for the facile construction of anilines with a broad substrate scope and wide functional group tolerance in moderate to excellent yields. (C) 2013 Elsevier Ltd. All rights reserved.
Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including cardiovascular diseases, pharmaceutical compositions comprising such compounds, methods for using such compounds and processes for making such compounds.
[EN] PYRROLOPYRAZINE KINASE INHIBITORS<br/>[FR] INHIBITEURS DE PYRROLOPYRAZINE KINASE
申请人:HOFFMANN LA ROCHE
公开号:WO2013030138A1
公开(公告)日:2013-03-07
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
Novel cyclohexylmethyl compounds corresponding to formula I
wherein R
1
, R
2
, R
3
, R
4
and R
5
, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.
[EN] FUNGICIDAL 4-SUBSTITUTED-3-{PHENYL[(HETEROCYCLYLMETHOXY)IMINO]METHYL}-1,2,4-OXADIZOL-5(4H)-ONE DERIVATIVES<br/>[FR] DÉRIVÉS DE 3-{PHÉNYL[(HÉTÉROCYCLYLMÉTHOXY)IMINO]MÉTHYL}-1,2,4-OXADIZOL-5(4H)-ONE 4-SUBSTITUÉE FONGICIDES
申请人:BAYER IP GMBH
公开号:WO2013037717A1
公开(公告)日:2013-03-21
The present invention provides fungicidal 4-substituted-3-phenyl[(heterocyclylmethoxy)imino]methyl}-1,2,4-oxadiazol-5(4H)-one derivatives of formula (I) wherein A represents a pyridyl or thiazole group and X1, Y1 to Y5 represent independently different substituents.
[EN] FUNGICIDAL 3-[(PYRIDIN-2-YLMETHOXYIMINO)(PHENYL)METHYL]-2-SUBSTITUTED-1,2,4-OXADIAZOL-5(2H)-ONE DERIVATIVES<br/>[FR] DÉRIVÉS FONGICIDES DE 3-[(PYRIDIN-2-YLMÉTHOXYIMINO)(PHÉNYL)MÉTHYL]-2-SUBSTITUÉ-1,2,4-OXADIAZOL-5(2H)-ONE
申请人:BAYER IP GMBH
公开号:WO2013098147A1
公开(公告)日:2013-07-04
The present invention relates to 3-[(pyridin-2-ylmethoxyimino)(phenyl)methyl]-2-substituted-1,2,4-oxadiazol-5(2H)-one derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.