The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Aug. 24, 2021
Filed:
Feb. 19, 2019
Applicant:
Otsuka Pharmaceutical Co., Ltd., Tokyo, JP;
Inventors:
Petr Zahradnik, Chomutov, CZ;
Antonin Sturc, Prague, CZ;
Jiri Malinak, Jesenice, CZ;
Jan Koci, Prelouc, CZ;
Assignee:
OTSUKA PHARMACEUTICAL CO., LTD., Tokyo, JP;
Primary Examiner:
Int. Cl.
CPC ...
C07F 5/02 (2006.01);
U.S. Cl.
CPC ...
C07F 5/027 (2013.01);
Abstract
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.