	US 12,274,760 B2
	Method for preparing fluorine-18-labeled fluoromethyl-substituted radiopharmaceuticals using selective azide substitution reaction and precursor scavenging
Byung Chul Lee, Hanam-si (KR); Ying Qing Lu, Guangdong (CN); and Byeong Min Jo, Seoul (KR)
Assigned to BIK THERAPEUTICS INC., Seoul (KR)
Filed by Byung Chul Lee, Hanam-si (KR)
Filed on Mar. 19, 2021, as Appl. No. 17/206,979.
Application 17/206,979 is a continuation of application No. PCT/KR2019/002862, filed on Mar. 13, 2019.
Claims priority of application No. 10-2018-0113473 (KR), filed on Sep. 21, 2018.
Prior Publication US 2021/0205482 A1, Jul. 8, 2021
Int. Cl. A61K 51/04 (2006.01)

CPC A61K 51/0402 (2013.01) [A61K 51/04 (2013.01)]

8 Claims

1. A method for preparing a [¹⁸F]fluoromethyl-substituted radiopharmaceutical using a selective azide substitution reaction, comprising:

(1) performing a fluorine-18 labeling reaction of bis(tosyloxy)methane and obtaining a first precursor solution containing [¹⁸F]fluoromethyltosylate;

(2) adding an azide reagent to the first precursor solution to cause an azide substitution reaction selectively on unlabeled bis(tosyloxy)methane compound present in the first precursor solution; and

(3) adding a bioactive molecule to the [¹⁸F]fluoromethyltosylate compound and obtaining a second precursor solution containing a [¹⁸F]fluoromethyl-substituted radiopharmaceutical.