A facile method for direct Pd(OAc)2-catalyzed oxidative cross-coupling of unactivated imidazo[1,2-a]pyridine with simplearenes has been developed. The reaction shows good reaction efficiency, high regioselectivity, and good functional-group compatibility. This approach provides a useful protocol for the preparation of imidazo[1,2-a]pyridine–arene structure of interest in biological and pharmaceutical
已开发了一种简便的方法,用于未活化的咪唑并[1,2- a ]吡啶与简单的芳烃的直接Pd(OAc)2催化的氧化交叉偶联。该反应显示出良好的反应效率,高的区域选择性和良好的官能团相容性。该方法为生物和药物材料中感兴趣的咪唑并[1,2 - a ]吡啶-芳烃结构的制备提供了有用的方案。
[EN] METHODS AND INTERMEDIATES FOR THE PREPARATION OF MACROLACTAMS<br/>[FR] PROCÉDÉS ET INTERMÉDIAIRES POUR LA PRÉPARATION DE MACROLACTAMES
申请人:MERCK SHARP & DOHME
公开号:WO2015095430A1
公开(公告)日:2015-06-25
The present invention relates to synthetic processes useful in the preparation of macrolactams that inhibit hepatitis C virus (HCV), specifically macrolactam compounds that inhibit the HCV NS3 protease activity and have application in the treatment of conditions caused by HCV. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
[EN] NEW BIS-AMIDO PYRIDINES<br/>[FR] NOUVEAUX BIS-AMIDO PYRIDINES
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2015025018A1
公开(公告)日:2015-02-26
This invention relates to bis-amidopyridinesof general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.
Regioselective copper-catalyzed thiolation of imidazo[1,2-a]pyridines.
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AMIDE COMPOUND
申请人:Setoh Masaki
公开号:US20100041891A1
公开(公告)日:2010-02-18
A compound having GPR52 agonist activity or a salt thereof is provided.
The compound can be provided as a preventive/therapeutic agent for schizophrenia or the like. The compound is represented by the following formula:
wherein
A represents —CONR
a
— or —NR
a
CO—,
R
a
represents a hydrogen atom or the like,
B represents a hydrogen atom or the like,
a ring Cy1 represents a six-membered aromatic ring which may have one or more substituents in addition to a group represented by -A-B,
a ring Cy2 represents a six-membered ring which may be substituted with a halogen atom or the like,
a ring Cy3 represents a five- or six-membered ring which may have one or more substituents;
X represents C
1-2
alkylene or the like,
m represents an integer of 0 to 2, and
a ring Cy4 represents a six-membered aromatic ring which may have one or more substituents.