US 11,655,261 B2
Method for preparing 18F-BPA and intermediate
Shi-hong Li, Jiangsu (CN); Jing He, Jiangsu (CN); Heng Yan, Jiangsu (CN); and Fei Cai, Jiangsu (CN)
Assigned to NEUBORON MEDTECH LTD., Jiangsu (CN)
Filed by NEUBORON MEDTECH LTD., Jiangsu (CN)
Filed on Feb. 9, 2021, as Appl. No. 17/171,224.
Application 17/171,224 is a continuation of application No. PCT/CN2019/100678, filed on Aug. 15, 2019.
Claims priority of application No. 201810940708.3 (CN), filed on Aug. 17, 2018; application No. 201811478614.5 (CN), filed on Dec. 5, 2018; and application No. 201811478615.X (CN), filed on Dec. 5, 2018.
Prior Publication US 2021/0230192 A1, Jul. 29, 2021
Int. Cl. C07F 5/02 (2006.01); C07B 59/00 (2006.01); C07C 229/34 (2006.01); C07C 249/02 (2006.01)
CPC C07F 5/027 (2013.01) [C07B 59/004 (2013.01); C07C 229/34 (2013.01); C07C 249/02 (2013.01)] 8 Claims
1. A method for preparing 18F-BPA with the structure:

OG Complex Work Unit Chemistry
reacting intermediate I-2 with a 18F ion to obtain a 18F-substituted compound

OG Complex Work Unit Chemistry
deprotecting the 18F-substituted compound to obtain the 18F-BPA

OG Complex Work Unit Chemistry
wherein R10 and R20 are OH, or taken together with a boron atom to which they are attached, represent a substituent that is hydrolyzable to —B(OH)2 group;
R3 or R4 independently represents hydrogen, an amino-protecting group, or an imino group combined with an amino group for protecting the amino group; and
R5 represents hydrogen or a carboxyl-protecting group.