Asymmetric Synthesis of Spirocyclic 2-Benzopyrans for Positron Emission Tomography of σ1 Receptors in the Brain

Asymmetric Synthesis of Spirocyclic 2-Benzopyrans for Positron Emission Tomography of σ1 Receptors in the Brain

Sharpless asymmetric dihydroxylation of styrene derivative 6 afforded chiral triols (R)-7 and (S)-7, which were cyclized with tosyl chloride in the presence of Bu2SnO to provide 2-benzopyrans (R)-4 and (S)-4 with high regioselectivity. The additional hydroxy moiety in the 4-position was exploited fo...

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Bibliographic Details
Main Authors: Katharina Holl, Dirk Schepmann, Steffen Fischer, Friedrich-Alexander Ludwig, Achim Hiller, Cornelius K. Donat, Winnie Deuther-Conrad, Peter Brust, Bernhard Wünsch
Format: Article
Language:English
Published: MDPI AG 2014-01-01
Series:Pharmaceuticals
Subjects:
2-benzopyrans
Sharpless Asymmetric Dihydroxylation
spirocycles
σ affinity
radiochemistry
positron emission tomography
autoradiography
organ distribution
Online Access:http://www.mdpi.com/1424-8247/7/1/78

Internet

http://www.mdpi.com/1424-8247/7/1/78

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