Farmitalia Carlo Erba S.r.l.

Consiglio Nazionale Delle Ricerche

Brichima, S.p.a.

Enicham Synthesis

Silvia De Bernardinis

Walter Cabri

Franco Francalanci

Sergio Penco

Ilaria Candiani

Angelo Bedeschi

Marcello Marchi

Mario Varasi

Carlo Neri

Attilio Citterio

Francesco Minisci

Luciano Pallini

Elena Vismara

Mariano Correale

Tiziano Martinengo

4-substituted anthracyclinones and anthracycline glycosides and the

Process for the preparation of substituted benzofuran derivatives

A compound of formula (I) ##STR1## wherein R' is hydrogen or methyl, m is zero or 1 and the symbol  means that the azabicyclic rings may be in the .alpha. or the .beta. orientation, and the pharmaceutically acceptable salts thereof, are useful in treating CNS disorders, gut motility disorders, and/or emesis and/or pain in mammals, and/or migraine.

Dihydrobenzofuran carboxamides and process for their preparation

4-substituted anthracyclinones and their preparation

Process for preparing anthracyclinones

Phenols are oxidated to quinones with hydrogen peroxide in the presence of catalytic amounts of bromine, iodine, hydrogen bromide and hydrogen iodide.

Process for the preparation of quinones

4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyldaunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound, in an appropriate reducing environment, with a catalytic amount of a transition metal complex, preferably palladium or nickel with 1,3 diphenylphosphinopropane or 1,1'-bis (diphenylphosphino) ferrocene, and eliminating the 13-dioxolanyl group by treatment with trifluoroacetic acid.

Process for preparing 4-demethoxydaunomycinone

4-Demethoxy-daunomycinone I: ##STR1## the known aglycone of 4-demethoxy-daunorubicin, is prepared by protecting the 13-keto group of 4-demethyl-daunomycinone, sulfonylating the 4-hydroxy group, reacting the sulfonylated compound with an amine, removing the amino protecting group from the resultant 4-demethyl-4-(protected amino)-13-dioxolanyl-daunomycinone, diazotizing the thus-freed 4-amino group and reducing under mild conditions the resulting diazonium compound.

Process for the preparation of 4-demethoxydaunomycinone, the aglycone of

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Milan, Italy

Silvia De Bernardinis