Synthesis of 1-Oxo-1-(3-pyridazinyl) Derivatives - Potent Inhibitors of Fatty Acid Amide Hydrolase (FAAH): An Improved and Optimized Procedure

Goffredo Rosini; Daniele G. Andreotti; Primiano D’Ambrosio; Emanuela Marotta; Alessandro Tinarelli; Paolo Righi

doi:10.1055/s-2007-990774

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Synthesis of 1-Oxo-1-(3-pyridazinyl) Derivatives - Potent Inhibitors of Fatty Acid Amide Hydrolase (FAAH): An Improved and Optimized Procedure

Goffredo Rosini*^a, Daniele G. Andreotti^b, Primiano D’Ambrosio^a, Emanuela Marotta^a, Alessandro Tinarelli^a, Paolo Righi^a
^a Dipartimento di Chimica Organica ‘A. Mangini’ - Alma Mater Studiorum, Università di Bologna, Viale del Risorgimento 4, 40136 Bologna, Italy
Fax: +39(051)2093654; e-Mail: goffredo.rosini@unibo.it;
^b GlaxoSmithKline, Medicine Research Centre, Via A. Fleming 4, 37135 Verona, Italy

Abstract

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Abstract

A greatly improved procedure for the preparation of long-chain α-ketopyridazines, a class of potent inhibitors of fatty acid amide hydrolase (FAAH), is described. This optimization study shows a great dependence of the yields of desired products on the pyrididazinyl lithium/Weinreb amide ratio and offers a general approach to this kind of compound.

Key words

3-acylpyridazines - regioselective acylations - FAAH inhibitors - Weinreb amides - lithiation - drugs

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References

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