New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives

…, C Batzl, RW Hartman, A Mannschreck

Index: Bayer, Herbert; Batzl, Christine; Hartmann, Rolf W.; Mannschreck, Albrecht Journal of Medicinal Chemistry, 1991 , vol. 34, # 9 p. 2685 - 2691

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Citation Number: 53

Abstract

The (E)-2-(4-pyridylmethylene)-l-tetralones 1-7 (1, H; 2, 50CH3; 3, 6-OCH3; 4, 7-OCH3; 5, 50H 6, 6-0H 7, 7-0H) were obtained by aldol condensation of the corresponding 1-tetralones with 4-pyridinecarboxaldehyde, and in the case of the OH compounds 5 and 7 subsequent ether cleavage of the OCH8-substituted 2-(4-~ yridylmethylene)-l-tetralones. Catalytic hydrogenation of 1-4 gave the 2-(4pyridylmethyl)-l-tetralones 8-11 (8, H 9, 50CH~; 10, 6- ...