PROCESS FOR PRODUCTION OF NEW DERIVATIVES OF 9 AND 11 NITRO-APOVINCAMIN ACID

• Main Authors: PALOSI,EVA,HU, SZOMBATHELYI,ZSOLT,HU, KARPATI,EGON,HU, RIESZ,MIKLOS,HU, MOLDVAI,ISTVAN,HU, ZAJERNE BALAZS,MARIA,HU, VEDRES,ANDRAS,HU, SZPORNY,LASZLO,HU, KISS,BELA,HU, STEFKO,BELA,HU, GROO,DORA,HU, SZANTAY,CSABA,HU
• Format: Patent
• Language: English
• Published: 28.04.1987
• Edition: 4
• Subjects: 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

The invention relates to a new process for preparing novel racemic and optically active 9- or 11-nitroapovincaminic acid derivatives of the general formula (I) (I) wherein R stands for a -CO-X group, wherein X means a halogen atom; or for a -CO-OR1 group, wherein R1 means an optionally mono- or polysubstituted C1-10 aliphatic group, a C3-8 alicyclic group or an aromatic C6-14 hydrocarbyl group; or for a -CO-NR2R3 group, wherein R2 and R3 are the same or different and stand for a hydrogen atom or a C1-8 alkyl group optionally forming a saturated heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R3 may also represent an amino group when R2 stands for a hydrogen atom; or for a cyano group, as well as their salts and pharmaceutical preparations containing these compounds. Furthermore the invention relates to a process for preparing these compounds and preparations. The racemic and optically active substances of the general formula (I) as well as their pharmaceutically acceptable acid addition and quaternary salts have valuable therapeutic properties, namely vasodilating, spasmolytic, antihypoxic and anticonvulsive effects.