7-(DIPHENYLMETHYL)OXY-9A-METHOXYMITOSANE AND MAKING AND USE THEREOF

摘要

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-vitro-2-pyridyldithio)ethylamino]- 9a-methoxymitosane.