PROCESS FOR PREPARING HEXITOLS CONTAINING FREE CARBOXYL GROUP

• Main Authors: KERPEL-FRONIUS,SANDOR,HU, ELEKES,ILONA,HU, SUGAR,JANOS,HU, INSTITORIS,LASZLO,HU, MEDZIHRADSZKY,KALMANNE,HU, HINDY,IVAN,HU, OETVOES,LASZLO,HU, SOMFAI-RELLE,ZSUZSA,HU, MEDZIHRADSZKY,KALMAN,HU, GLERIA,KATALIN,HU, ECKHARDT,SANDOR,HU
• Format: Patent
• Language: English
• Published: 28.12.1983
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Hexitols of the general formula (wherein the hexitol skeleton corresponds to dulcitol, mannitol or iditol, R@ represents a halogen atom, R represents a hydroxy group, or R and R together form an oxygen atom; R represents a free carboxy containing saturated or unsaturated alkylcarbonyl group with 4 to 10 carbon atoms, a free carboxy containing arylcarbonyl group with 8 to 12 carbon atoms or a free carboxy containing satiurated or unsaturated aralkylcarbonyl group with 9 to 11 carbon atoms) and Rs@ represents a hydrogen atom, a free carboxy containing saturated or unsaturated alkylcarbonyl group with 4 to 10 carbon atoms, a saturated or unsaturated C2-10 alkylcarbonyl group, an alkoxycarbonyl containing saturated or unsaturated alkylcarbonyl group with 4 to 10 carbon atoms, a saturated or unsaturated C8-10 aralkylcarbonyl group, a free carboxy containing arylcarbonyl group with 8 to 12 carbon atoms or a free carboxy containing saturated or unsaturated aralkylcarbonyl group with 9 to 11 carbon atoms) and salts thereof possess tumour inhibiting activity. The hexitols of the present invention are prepared by hydrogenation of a corresponding benzyloxycarbonyl containing 1,2-5,6-dianhydrohexitol, reaction of 1,2-5,6-dianhydrohexitol with a dicarboxylic acid anhydride and halogenation of a corresponding 1,2-5,6-dianhydrohexitol.