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.

Date of Patent:
Aug. 09, 2016

Filed:

Oct. 08, 2013
Applicants:

Osaka Prefecture University Public Corporation, Sakai-Shi, Osaka, JP;

Stella Pharma Corporation, Chuo-ku, Osaka-Shi, Osaka, JP;

Inventors:

Hiroshi Takenaka, Osaka, JP;

Yoichiro Ohta, Osaka, JP;

Yusuke Taguchi, Osaka, JP;

Sayuri Ueda, Osaka, JP;

Yuko Ishino, Osaka, JP;

Hideki Nakashima, Osaka, JP;

Kohki Uehara, Osaka, JP;

Mitsunori Kirihata, Sakai, JP;

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07F 5/02 (2006.01); C07C 229/08 (2006.01); C07F 5/04 (2006.01); C07C 229/36 (2006.01); C07B 59/00 (2006.01); C07C 271/22 (2006.01); C07C 251/24 (2006.01);
U.S. Cl.
CPC ...
C07F 5/025 (2013.01); C07B 59/001 (2013.01); C07C 229/08 (2013.01); C07C 229/36 (2013.01); C07C 251/24 (2013.01); C07C 271/22 (2013.01); C07F 5/027 (2013.01); C07F 5/04 (2013.01); Y02P 20/55 (2015.11);
Abstract

Provided are: a novel chiral 4-boronophenylalanine (BPA) derivative; a method for producing the derivative; and a method for producingF-2-fluoro-4-borono-L-phenylalanine (F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BRR, BXor BXM(wherein X represents a halogen atom, and Mrepresents a monovalent monoatomic cation, a polyatomic cation or a complex cation); Rrepresents a hydrogen atom or a protecting group PG1; Rrepresents a hydrogen atom or a protecting group PG2; Rand Rindependently represent OH, or R, Rand B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO, NH, Sn(R), N═N—NRR, OSOR, NRR, a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepareF-labeled BPA.


Find Patent Forward Citations

Loading…