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-18 Method for Synthesis of [18F]Fluoromethyl-substituted Radiopharmaceuticals by Using Selective Azidation and Precursor Scavenging
专利权人:
주식회사 비아이케이테라퓨틱스
发明人:
이병철,육영청,조병민
申请号:
KR1020180113473
公开号:
KR1021370010000B1
申请日:
2018.09.21
申请国别(地区):
KR
年份:
2020
代理人:
摘要:
The present invention through the 18 O (p, n) 18 F reaction from a cyclotron [18 F] a first step of obtaining a fluoride, wherein the [18 F] fluoride for the acetonitrile 2.2.2 K and K 2 CO 3 is dissolved the separation using the nitrile reaction solution [18 F] F - / H 2 18 O step 2 to obtain a solution, wherein the [18 F] F - / H 2 O solution is heated to 18 K 2.2.2 / K 18 F a The third step of obtaining, by adding the K 2.2.2 /K 18 F and the bistosiloxymethane compound together in a reaction vessel, and reacting by adding a reaction solvent to obtain a first precursor solution, the first precursor by cooling the solution was added to the azide reagent perform azide substitution reaction, [18 F] a fifth step of obtaining a methyl tosylate compounds fluoro, said [18 F] bioactive molecular precursor of methyl tosylate compound fluorophenyl Fluoro-18-labeled fluoromethyl by removing the unreacted precursor by adding a precursor scavenger to the sixth step of obtaining a second precursor solution and adding the precursor scavenger to the second precursor solution by adding the It relates to a method for producing a fluorine-18-labeled fluoromethyl-substituted radiopharmaceutical using a selective azide substitution reaction comprising a seventh step of preparing a substituted radiopharmaceutical without an HPLC separation process. According to the present invention, in the process of synthesizing radiopharmaceuticals, an excess of bistosiloxymethane compound present in the reaction mixture is deactivated through a selective azide substitution reaction, and the next step of bioactive molecular precursor and [ 18 F]fluoromethyltosyl Fluoro-18-substituted fluoromethyl-substituted radiopharmaceuticals with high radiochemical purity can be synthesized even when the separation and purification process of HPLC is omitted while significantly improving the alkylation yield between the rate compounds, and the manufacturing time and Manufacturing cost can be reduced.본 발명은 사이클로트론
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