New Series of N‐Substituted Phenyl Ketone Oxime Ethers: Synthesis and Bovine β₃‐Adrenergic Agonistic Activities.

Abstract

Ketone derivatives Ketone derivatives Q 0370New Series of N-Substituted Phenyl Ketone Oxime Ethers: Synthesis and Bovine β 3 -Adrenergic Agonistic Activities. -Title ethers (V) are prepared via the intermediate epoxides as the key compounds. The crude epoxides are employed without purification for the subsequent reactions with alkyl, arylalkyl and aryl amines like (IV). The bovine β 3 -adrenoceptor and adenylyl cyclase activation properties of the ethers are evaluated. Benzodioxole dicarboxylate derivative (Ve) shows the highest agonistic affinity and potency as well as the highest intrinsic activity. The antagonists (Va), (Vb), and (Vd) are of interest as a tool for further conclusive functional identification of β 3 -adrenoceptors. Ketone oxime ethers are considered as an alternative to the arylethanolamine or aryloxypropanol amine structure in the search for specific β 3 -adrenergic ligands. -(EL HADRI, A.; NICOLLE*, E.; LECLERC, G.; PIETRI-ROUXEL, F.; STROSBERG, A. D.; ARCHIMBAULT, P.; Pharmazie 58 (2003) 1, 13-17; Lab. Chim. Org., Groupe Pharmacochim. Mol., Fac. Pharm., Univ. Joseph Fourier, F-38240 Meylan, Fr.; Eng.) -H. Hoennerscheid 20-097

Trifluoroacetic Acid-Mediated Oxidative Self-Condensation of Acetophenones in the Presence of SeO2: A Serendipitous Approach for the Synthesis of Fused [1,3]Dioxolo[4,5-d][1,3]dioxoles

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