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Journal of Medicinal Chemistry
for Schizophrenia; John Wiley & Sons, Inc.: Hoboken, NJ, USA, 2012;
pp 273-294.
added sequentially. The vial was sealed and the mixture was
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stirred vigorously at room temperature for 2 – 3 h. The organic
phase was isolated and the aqueous phase was reextracted with
toluene (2 x 2 mL). The organic phases were combined, washed
with brine (2 mL), dried over MgSO4, filtered, concentrated in
vacuo and purified by flash chromatography to yield a clear oil.
The oil was dissolved in Et2O (1.5 mL) and MeOH (1.5 mL)
before 2M HCl in Et2O (1.5 mL) was added. The mixture was
stirred at room temperature for 24 h under argon. The mixture
was concentrated in vacuo, dissolved in water (8 mL), added 2M
NaOH (2 mL) and EtOAc (10 mL). After thorough mixing the
mixture was filtered, the organic phase isolated and the aqueous
phase reextracted with EtOAc (10 mL). The combined organic
phases was washed with brine (10 mL), dried over MgSO4,
filtered and concentrated in vacuo.
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ASSOCIATED CONTENT
Supporting information
Experimental procedures and full characterization of all new
compounds including 1H NMR and 13C NMR spectre and
pharmacological methods. This material is available free of
AUTHOR INFORMATION
†Authors have contributed equally to this article.
Corresponding Author
Notes
The Authors declare no competing financial interest
ACKNOWLEDGEMENT
The chemistry described was conducted at H. Lundbeck A/S. We
gratefully acknowledge the research facilities and materials provid-
ed by H. Lundbeck A/S and Department of Drug Design and
Pharmacology, The Faculty of Health and Medical Sciences, The
University of Copenhagen. Niels Krogsgaard-Larsen was supported
by a DRA PhD scholarship provided by the Faculty of Health and
Medical Sciences, The University of Copenhagen in collaboration
with H. Lundbeck A/S. Anders A. Jensen was supported by the
Novo Nordisk Foundation and the Aase and Ejnar Danielsen
Foundation. The cDNA of the human 5-HT2C receptor was a kind
gift from Drs. Alan Saltzman and Stuart Sealfon.
ABBREVIATIONS
PD: Parkinson’s disease; SZ: Schizophrenia; AD: Alzheimers
disease; CNS: Central nervous system.
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