We present a straightforward synthesis of 3-aryl-2,5-dihydrofurans by ring contraction of 4-aryl-3,6-dihydro-2H-pyrans with the repeated treatment of MCPBA and BF3-OEt2. The building block 3-aryltetrahydrofuran-3-carboxylic acid with potential biological activities was also prepared.
We present a straightforward synthesis of 3-aryl-2,5-dihydrofurans by ring contraction of 4-aryl-3,6-dihydro-2H-pyrans with the repeated treatment of MCPBA and BF3-OEt2. The building block 3-aryltetrahydrofuran-3-carboxylic acid with potential biological activities was also prepared.
Catalytic Friedel‐Crafts Reactions on Saturated Heterocycles and Small Rings for sp
<sup>3</sup>
‐sp
<sup>2</sup>
Coupling of Medicinally Relevant Fragments
作者:Rosemary A. Croft、Maryne A. J. Dubois、Alexander J. Boddy、Camille Denis、Anna Lazaridou、Anne Sophie Voisin‐Chiret、Ronan Bureau、Chulho Choi、James J. Mousseau、James A. Bull
DOI:10.1002/ejoc.201900498
日期:2019.9
A systematic comparison of Lewis acid catalysts [Ca(II), Li(I) and Fe(III)] is presented for catalytic Friedel–Crafts reactions using alcohols on 4‐, 5‐, and 6‐membered oxygen and nitrogen heterocycles and cyclobutanes, forming gem‐diaryl quaternary centers.
The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like.
The present invention is a compound represented by the formula (1):
wherein each symbol is as described in the specification, or a salt thereof.
are employed as electrophiles in the Pd-catalyzed cross-coupling with tosylhydrazones affording di-, tri-, and tetrasubstituted olefins. Fine tunning of the reaction conditions are required to accomplish the coupling successfully, including the addition of LiCl and the presence of small amounts of water. Under the optimized conditions, the reactions proceed with high yield and also high stereoselectivity
PREPARATION OF 4-ALKOXY-7-(TETRAHYDRO-PYRAN-4-YL)-BENZOTHIAZOL-2-YLAMINE DERIVATIVES
申请人:Spurr Paul
公开号:US20080108826A1
公开(公告)日:2008-05-08
Processes for the preparation of 4-alkoxytetrahydropyrane derivatives used in the preparation of 4-alkoxy-7-(tetrahydropyran-4-yl)-benzothiazol-2-ylamine and derivatives.
Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I):
wherein each symbol is as defined in the present specification,
or a salt thereof.