Collect. Czech. Chem. Commun. 1981, 46, 2116-2122

1-Substitution derivatives of 4-aryl-2,3-dibromo-1-naphthol

Jiří Křepelka, Jiří Roubík and Jiří Holubek

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3


Alkylation of 7-ethyl-4-(4-ethylphenyl)-2,3-dibromo-1-naphthol (I) with ethyl esters of ω-bromoalkanoic acids XX-XXIII in a non-aqueous medium gave the 1-substitution derivatives II, IV, VI and VIII which were hydrolyzed to the acids III, V, VII and IX. The acid III was used for syntheses of the esters X-XIII and amides XIV-XVIII. Compounds II-XVIII exhibited moderate antineoplastic effects in animals with transplanted tumours; best results were observed with the compound II.