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AssigneeBristol-Myers Squibb Company
InventorsDaniel A. Benigni, Kenton L. Shultis, Henry S. L. Wong
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7-(Diphenylmethyl)oxy-9a-methoxymitosane is a novel intermediate for conversion into 7-amino and 7-oxy-9a-methoxymitosanes and is also useful for inhibiting mammalian tumor growth. The compound is prepared by reacting 7-hydroxy-9a-methoxymitosane with diazodiphenylmethane. In a preferred reaction, the compound is prepared from mitomycin C via 7-hydroxy-9a-methoxymitosane without drying (water removal). The intermediate is advantageously converted to the very effective anti-tumor agent 7-[2-(4-nitrophenyldithio) ethylamino]-9a-methoxymitosane in unexpectedly high yields using a two step process where the first step constitutes conversion to 7-[2-(2-pyridyldithio) ethylamino]-9a-methoxymitosane. or 7-[2-(3-nitro-2-pyridyldithio)ethylamino]-9a-methoxymitosane.
Process for the preparation of 7-(diphenylmethyl)oxy-9a-methoxymitosane comprising the step of reacting 7-hydroxy-9a-methoxymitosane with diazodiphenylmethane to produce 7-(diphenylmethyl)oxy-9a-methoxymitosane.
Process for the preparation of 7-(diphenylmethyl)oxy-9a-methoxymitosane, said process comprising the steps of
Process for the preparation of 7-(diphenylmethyl)oxy-9a-methoxymitosane, said process comprising the steps of:
Dependencies are inferred from the claim text.