Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek Tno

Nederlandse Centrale Organisatie Voor Toegepast-Natuurwetenschappelijk

Nederlandse Organisatie Voor Toegepast

Nederlandse Centrale Organisatie Voor Toegespastnatuurwetenschappeliukond

Jan Berg

Francois Verbeek

Antonius Kerkenaar

Diederik J Schmedding

Eric J Bulten

Eric J Bluten

A method for preparing thiol compounds, comprising: (1) reacting cysteine by a non-enzymatical addition reaction with a compound having the formula (R.sub.1)(R.sub.2)C.dbd.C(R.sub.3)--CO--R.sub.4 via an --S-- bridge to form a cysteine conjugate, wherein the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent hydrogen or an optionally saturated and/or heterogeneous hydrocarbon group or wherein a combination of two groups selected from the group consisting of R.sub.1, R.sub.3 and R.sub.4, together with the carbon atoms to which the groups are bonded, form an optionally saturated and/or heterogeneous hydrocarbon ring system of five or six members; and (2) reacting the cysteine conjugate so obtained in a concentration of &gt;1 mM conjugate with a microbial .beta.-lyase to form a thiol compound.

Method for preparing thiol compounds with bacterial .beta.-lyase

Method for preparing thiol compounds by coupling cysteine having the formula HS--CH.sub.2 --CH(NH.sub.2)COOH via and --S-- bridge to a hydrocarbon compound and subsequently reacting the cysteine conjugate obtained with .beta.-lyase to form the relevant thiol compounds. For instance it is possible to prepare the flavor p-mentha-8-thiol-3-one starting from pulegone as illustrated in the diagram below: ##STR1##

Method for preparing p-mentha-8-thiol-3-one

Platinum diamine complexes of the general formulae ##STR1## wherein R.sub.1 and R.sub.2 independently from each other are a hydrogen atom or a substituted or unsubstituted alkyl, cyclo-alkyl, aryl or aralkyl group, while R.sub.1 and R.sub.2 may be together a substituted or unsubstituted cyclo-alkyl group, R.sub.3 and R.sub.4 independently of each other are a hydrogen atom or a substituted or unsubstituted alkyl, aryl or aralkyl group and X is a chlorine, bromine or iodine atom, a sulphate radical, a substituted or unsubstituted carboxylate rest like an acetate or substituted acetate radical, an oxalate, malonate, hydroxymalonate or otherwise substituted malonate group or a carboxylate group, the group Y, independently from X is a chlorine, bromine or iodine atom, a hydroxyl group, a nitrate group of a carboxylate group have been found to exhibit antitumor activity together with little or none kidney toxicity and are thus of interest as a medicament. Processes for the preparation of the platinum complexes are described and exemplified.

Platinum-diamine complexes, a process for the preparation thereof, a

This invention relates to novel platinum-diamine complexes having the formula: ##STR1## wherein R.sub.1 and R.sub.2 independently of each other may be selected from the group consisting of hydrogen, an alkyl group having 1-20 carbon atoms, a cycloalkyl group having from 3-7 carbon atoms in the ring, an aralkyl group, and an aryl group having 1-20 carbon atoms, whereas R.sub.1 and R.sub.2 together may form a cycloalkyl group having 3-7 carbon atoms in the ring and having the formula: ##STR2## wherein N is 2 to 7 and wherein R.sub.3 and R.sub.4 independently of each other are selected from the group consisting of hydrogen, an alkyl group having 1-20 carbon atoms, an aryl group or an aralkyl group having 1-20 carbon atoms in the alkyl group and X is an anionic group, providing that when X is either chlorine or malonate, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are not each H; when X is chlorine and R.sub.1 and R.sub.2 are each H, R.sub.3 and R.sub.4 are not each methyl; when X is chlorine and R.sub.1 and R.sub.2 are each methyl, R.sub.3 and R.sub.4 are not each H, and when X is chlorine R.sub.1 is hydrogen and R.sub.2 is methyl and R.sub.3 and R.sub.4 are not each hydrogen.

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Nieuwegein, Netherlands

Jan Berg