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...

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Hauptverfasser: MALINAK, Jiri, ZAHRADNIK, Petr, STURC, Antonin, KOCI, Jan
Format: Patent
Sprache:eng ; fre ; ger
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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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creator MALINAK, Jiri
ZAHRADNIK, Petr
STURC, Antonin
KOCI, Jan
description 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.
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subjects 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
title METHOD OF 4-BORONOPHENYLALANINE PRODUCTION
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