METHOD FOR PRODUCING F-BPA AND AN INTERMEDIATE COMPOUND Russian patent published in 2022 - IPC C07C229/36 C07C249/02 C07C251/24 C07F5/02 C07B59/00

Abstract RU 2776178 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a method for producing ¹⁸F-BPA (2-fluoro-4-boron-L-phenylalanine) with the following structure:

The method includes the interaction of an intermediate compound I-2 with an ¹⁸F ion, resulting in an ¹⁸F-substituted compound

I-2

removal of protection from the ¹⁸F-substituted compound, resulting in ¹⁸F-BPA

wherein R₁₀ and R₂₀ constitute OH or, taken together with the boron atom whereto they are attached, constitute a substituent hydrolysable to a boric acid group, R₃ or R₄ independently constitute hydrogen, an amino-protective group, or -NR₃R₄ constitutes and R₅ constitutes a carboxyl-protective group. Also proposed are an intermediate compound I and an application thereof for producing ¹⁸F-BPA.

EFFECT: proposed method is a simple and effective way for producing ¹⁸F-BPA, with mild reaction conditions and high output, and it satisfies the clinical needs.

12 cl, 3 dwg, 7 ex

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RU 2 776 178 C1

Authors

Li Shi-Hong

He Jing

Cai Fei

Yan Heng

Dates

2022-07-14—Published

2019-08-15—Filed