Tuned Classical Thermal Aromatization Furnishing an Estrogenic Benzoacridine

Dedicated to the memory of Prof. Tsutomu Katsuki for his enormous contribution to synthetic organic chemistry and encouragement to us.

Abstract

The diversity-oriented doubling strategy, which generates two 12-arylbenzoacridines from a single triarylmethanol precursor was developed to construct a library of drug candidates for the identification of biologically active compounds. Exploration of this 12-arylbenzoacridine library furnished a 4′-OH derivative as an estrogenic compound.

Key words

arenes - cyclization - heterocycles - medicinal chemistry - aminotriarylmethanol - 12-arylbenzoacridine - diversity-oriented doubling strategy - estrogenic activity

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