	US 12,421,179 B2
	Production method for radiolabeled aryl compound
Yoshifumi Shirakami, Suita (JP); Hayato Ikeda, Suita (JP); Yasukazu Kanai, Suita (JP); Eku Shimosegawa, Suita (JP); Jun Hatazawa, Suita (JP); Tadashi Watabe, Suita (JP); and Kazuko Kaneda, Suita (JP)
Assigned to OSAKA UNIVERSITY, Suita (JP)
Filed by OSAKA UNIVERSITY, Suita (JP)
Filed on Jun. 20, 2023, as Appl. No. 18/337,623.
Application 18/337,623 is a continuation of application No. 16/636,236, granted, now 11,731,917, previously published as PCT/JP2018/030006, filed on Aug. 3, 2018.
Claims priority of application No. 2017-151632 (JP), filed on Aug. 4, 2017.
Prior Publication US 2023/0331640 A1, Oct. 19, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. C07B 59/00 (2006.01); C07F 5/02 (2006.01); C07F 13/00 (2006.01)

CPC C07B 59/001 (2013.01) [C07B 59/004 (2013.01); C07F 5/025 (2013.01); C07F 13/00 (2013.01); C07F 13/005 (2013.01); C07B 2200/05 (2013.01)]

8 Claims

1. A method of producing a radiolabeled aryl drug compound represented by formula (I):

Ar—X (I)

wherein

Ar is a C_6-14aryl group optionally having substituent(s), and

X is ¹²³I, ¹²⁴I, ¹²⁵I or ¹³¹I,

or a salt thereof, which comprises reacting an aryl boronic acid compound represented by formula (II):

Ar—Y (II)

wherein

Ar is as defined above, and

Y is a borono group (—B(OH)₂) or an ester group thereof,

or a salt thereof, with a radionuclide selected from the group consisting of ¹²³I, ¹²⁴I, ¹²⁵I and ¹³¹I, in the presence of an oxidizing agent selected from the group consisting of N-bromosuccinimide and N-chlorosuccinimide, in water, in an organic solvent-free system.