Pharmachemie B.v.

Dirk De Vos

Johan W Scheeren

Joannes F De Bie

Marcel Gielen

Rudolph Willem

Joannes F Martinus De Bie

Abdelaziz El Khloufi

Mohammad Boualam

The invention relates to anti-tumor compositions containing as an active ingredient one or more compounds of the formula

Organo-tin compounds having anti-tumour activity and anti-tumour

This invention provides novel anti-tumour compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or together form an alkyl-, alkoxy- or OH-substituted aromatic group, which optionally contains an N atom as a hetero-atom; R is --COCH.sub.3 or --C.tbd.C--R.sub.4 and R.sub.4 is H or trimethylsilyl; and R.sub.3 is H or --COCF.sub.3 ; and acid addition salts thereof; as well as compositions containing these compounds.

Anthracycline compounds and intermediates

The invention provides novel cyclic triketone compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R* is a group of the formule ##STR2## wherein R.sup.1 is methyl and R.sub.2 is an alkyl group containing at least 2 carbon atoms or R.sup.1 is an alkyl group having 1-4 carbon atoms and R.sup.2 is an aryl group, a hetero aryl group, a --CH.sub.2 OR' group, a --CH.sub.2 N&lt;group, a --CH.sub.2 SR' group or a --CH.sub.2 CH.dbd.CH.sub.2 group, wherein R' and R' are alkyl groups having 1-4 carbon atoms. These compounds can be used for preparing daunomycinone and derivatives thereof. Daunomycinone is used for preparing daunomycin and adriamycin. By introducing chirality at C-1 of ring A in the preparation of said novel compounds by using a novel diene of formula (1) in a Diels-Alder reaction for said preparation, the chirality of C-3 is established in the subsequent reaction with LiC.tbd.CSi(CH.sub.3).sub.3 in the synthesis of daunomycinone and deriviatives thereof. ##STR3## This last reaction leads to the desired compound wherein OH at C-3 and OR at C-1 are in the cis-position with respect to each other.

Cyclic triketone compounds and trimethylsilyoxy butadiene compounds and

The invention relates to novel compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R is a good leaving group, and to the preparation of these compounds in a stereospecific manner to obtain a configuration wherein OH at C-3 and OR at C-1 are in the cis-position, which compounds can be used for the synthesis of daunomycinone and derivatives thereof. Daunomycinone can be used for the preparation of daunomycin and adriamycin.

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Oegstgeest, Netherlands

Dirk De Vos