Farmitalia Carlo Erba S.p.a.

Farmitalia Carlo Erba S.r.l.

Societa' Farmaceutici Italia S.p.a.

Ettore Lazzari

Federico Maria Arcamone

Sergio Penco

Nicola Mongelli

Giuseppe Mazzini

Maria A Verini

Piero Melloni

Arturo D Torre

Luigi Bernardi

Alessandro Rossi

Aurelio Di Marco

Lorenzo Pegrassi

Maria L Malnati

The present invention relates to a new process for the preparation of 3-substituted derivatives of 1-amino-2-hydroxy-propane in the form of single diastereoisomers, to certain of these diastereoisomers, and to compounds which are intermediates in the new process of the invention.

Process for the preparation of 3-substituted derivatives of

The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and --Het-- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds. The compounds of the invention can be useful antitumor and antiviral agents.

Site specific alkylating agents

The present invention relates to a new process for the preparation of 3-substituted derivatives of 1-amino-2- hydroxy-propane in the form of single diastereoisomers, to certain of these diastereoisomers, and to compounds which are intermediates in the new process of the invention.

Process for preparation of 3-substituted derivatives of

The invention relates to distamycin A analogs of the following formula ##STR1## wherein n is 2, 3 or 4; A is an optionally substituted divalent radical chosen from ##STR2## and -Het- wherein Het is a pentatomic or hexatomic heteromonocyclic ring, except pyrrole; and wherein either one of R.sub.1 and R.sub.2 is hydrogen and the other is an acylating moiety or R.sub.1 and R.sub.2 are both hydrogen or both alkyl groups optionally substituted, including the pharmaceutically acceptable salts of the said compounds. The compounds of the invention can be useful antitumor and antiviral agents.

There are provided compounds of formula 1: ##STR1## wherein R=halogen atom or CN, NH.sub.2 and NO.sub.2 group, and pharmaceutically acceptable salts thereof. The compounds are antipsycotic agents.

Antipsycotic benzoxazines

The antitumor efficacy of the known antibiotics daunomycin (daunorubicin) and adriamycin (doxorubicin) is synergized by the use of said antibiotics together with a daunosamine nucleoside. The latter compounds are prepared by condensing a reactive protected daunosamine with a reactive protected heterocyclic base.

Growing community of inventors

Milan, Italy

Ettore Lazzari