NEW MATERIAL:3-Nitro-2,4,6-trihydroxybenzoate of formula I (R is 1-15C straight chain alkyl or 1-3C phenylalkyl).
EXAMPLE: Methyl 0-nitro 2,4,6-hydroxybenzoate.
USE: Useful as an antineoplastic agent. The above mentioned compound can promote differentiation of a tissue in a precancerous condition to a normal tissue and can inhibit conversion of a precancer cell to a malignant cell. In addition thereto, an antineoplastic effect can be obtained by inhibition of carcinogenic promotion. Capable of oral administration.
PREPARATION: Phloroglucinolcarboxylic acid of formula II is nitrated to obtain a compound of formula III. The above-mentioned nitration is carried out by reacting 1-3 equivalent concentrated nitric acid therewith in a sulfuric acid having a suitable concentration, e.g. 60% (V/V). The resultant compound of formula III is then condensed with an alcohol of formula IV in the presence of a condensation agent as the second process, thus giving the objective compound of formula I.
TOKUDA HARUKUNI
NISHINO HOUYOKU
YOSHIDA SHIGEO
KOZUKA MUTSUO
