METHOD OF 4-BORONOPHENYLALANINE PRODUCTION

METHOD OF 4-BORONOPHENYLALANINE PRODUCTION

The present invention relates to a method of production of 4-boronophenylalanine (BPA) from 4-iodophenylalanine, in which all the functional groups of the amino acid are protected by benzyl protection method, and which uses isopropyl magnesium halogenide stabilized by a complexation base, and subseq...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: STURC, ANTONIN, MALINAK, JIRI, ZAHRADNIK, PETR, KOCI, JAN
Format: Patent
Sprache:eng ; pol
Schlagworte:
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:The present invention relates to a method of production of 4-boronophenylalanine (BPA) from 4-iodophenylalanine, in which all the functional groups of the amino acid are protected by benzyl protection method, and which uses isopropyl magnesium halogenide stabilized by a complexation base, and subsequent condensation of the resulting Grignard reagent with a boric acid ester. The final reaction step, catalytic hydrogenolysis or transfer hydrogenolysis of protecting groups on the amino acid, occurs after hydrolysis of the boronate ester groups.