Otsuka Pharmaceutical Company, Limited

Jiri Malinak

Yoshito Masuda

Antonin Sturc

Jan Koci

Jiri Prokop

Petr Zahradnik

Ivan Hlavacek

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.

Method of 4-boronophenylalanine production

The present invention generally relates to a process of preparing iosimenol and a process of preparing a crystal of iosimenol, as well as a crystal of iosimenol prepared by these processes.

Innovative preparation and crystallization of iosimenol

Growing community of inventors

Jesenice, Czechia

Jiri Malinak