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RU2007126814A - Способ получения фторорганических соединений в спиртовых растворителях - Google Patents

Способ получения фторорганических соединений в спиртовых растворителях Download PDF

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RU2007126814A
RU2007126814A RU2007126814/04A RU2007126814A RU2007126814A RU 2007126814 A RU2007126814 A RU 2007126814A RU 2007126814/04 A RU2007126814/04 A RU 2007126814/04A RU 2007126814 A RU2007126814 A RU 2007126814A RU 2007126814 A RU2007126814 A RU 2007126814A
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fluoride
formula
butanol
alkyl
alcohol
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Дае Хиук МООН (KR)
Дае Хиук МООН
Дае Йоон ТИ (KR)
Дае Йоон ТИ
Донг Воок КИМ (KR)
Донг Воок КИМ
Сеунг Дзун ОХ (KR)
Сеунг Дзун ОХ
Дзин-соок РИУ (KR)
Дзин-соок РИУ
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Фьючеркем Ко., Лтд. (Kr)
Фьючеркем Ко., Лтд.
Дзе Эйшн Фаундейшн (Kr)
Дзе Эйшн Фаундейшн
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Claims (22)

1. Способ получения фторорганических соединений взаимодействием фторида с алкилгалогенидом или алкилсульфонатом в присутствии спирта формулы 1 в качестве растворителя
Формула 1
Figure 00000001
в которой R1, R2 и R3 представляют атом водорода или С1-С18 алкил.
2. Способ по п. 1, в котором фторид содержит фтор-18 или фтор-19.
3. Способ по п. 1, в котором R1 представляет атом водорода или С1-С18 алкил; R2 является атомом водорода или С1-С18 алкилом; и R3 представляет атом водорода или С1-С18 алкил.
4. Способ по п. 1, в котором R1 представляет метил или этил; R2 представляет метил или этил; и R3 является метилом или этилом.
5. Способ по п. 1, в котором спирт формулы 1 выбран из группы, состоящей из первичных спиртов, таких как метанол, этанол, н-пропанол, н-бутанол, амиловый спирт, н-гексиловый спирт, н-гептанол или н-октанол; вторичных спиртов, таких как изопропанол, изобутанол, изоамиловый спирт и 3-пентанол; и третичных спиртов, таких как трет-бутанол, трет-амиловый спирт, 2,3-диметил-2-бутанол, 2-(трифторметил)-2-пропанол, 3-метил-3-пентанол, 3-этил-3-пентанол, 2-метил-2-пентанол, 2,3-диметил-3-пентанол, 2,4-диметил-2-пентанол, 2-метил-2-гексанол, 2-циклопропил-2-пропанол, 2-циклопропил-2-бутанол, 2-циклопропил-3-метил-2-бутанол, 1-метилциклопентанол, 1-этилциклопентанол, 1-пропилциклопентанол, 1-метилциклогексанол, 1-этилциклогексанол и 1-метилциклогептанол.
6. Способ по п.1, в котором спирт формулы 1 выбран из группы, состоящей из трет-бутанола, трет-амилового спирта, 2,3-диметил-2-бутанола и 2-(трифторметил)-2-пропанола.
7. Способ по п.1 или 2, в котором фторид представляет фторид цезия или фторид тетраалкиламмония, и спирт выбран из группы, состоящей из трет-бутанола, трет-амилового спирта, 2,3-диметил-2-бутанола и 2-(трифторметил)-2-пропанола.
8. Способ по пп.1 и 2, в котором фторид предпочтительно выбран из группы, состоящей из фторидов щелочных металлов, включающих щелочные металлы, выбранные из группы, состоящей из лития, натрия, калия, рубидия и цезия; фторидов щелочно-земельных металлов, включающих щелочно-земельные металлы, выбранные из группы, состоящей из магния, кальция, стронция и бария; и фторида аммония.
9. Способ по п.8, в котором фторид аммония предпочтительно выбран из группы, состоящей из фторидов четвертичного аммония, включая фторид тетрабутиламмония и фторид бензилтриметиламмония; фторидов третичного аммония, включая фторид триэтиламмония и фторид трибутиламмония; фторидов вторичного аммония, включая фторид дибутиламмония и фторид дигексиламмония; и фторидов первичного аммония, включая фторид бутиламмония и фторид гексиламмония.
10. Способ по пп.1 и 2, в котором фторид представляет фторид цезия или фторид тетраалкиламмония.
11. Способ по п.10, в котором фторид цезия или фторид тетраалкиламмония адсорбирован на подложках, выбранных из группы, состоящей из целита, молекулярного сита, оксида алюминия и силикагеля.
12. Способ по пп.1 и 2, в котором количество фторида составляет 1,0-10 экв к алкилгалогениду или алкилсульфонату в случае фтора-19, и количество фторида является следовым количеством [18F]фторида к алкилгалогениду или алкилсульфонату в случае фтора-18.
13. Способ по п.12, в котором используют 1 пкг-100 нг [18F]фторида на 1 мг алкилгалогенида или алкилсульфоната соли фторида в случае фтора-18.
14. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фтордезоксиглюкозу формулы 2
Формула 2
Figure 00000002
15. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фтормизонидазол формулы 3.
Формула 3
Figure 00000003
16. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фторэстрадиол формулы 4
Формула 4
Figure 00000004
17. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фторпропилкарбометокситропан формулы 5
Формула 5
Figure 00000005
18. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фторDDNP формулы 6
Формула 6
Figure 00000006
19. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фтортимидин формулы 7
Формула 7
Figure 00000007
20. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фторхолин формулы 8
Формула 8
Figure 00000008
21. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фторэтилхолин формулы 9
Формула 9
Figure 00000009
22. Способ по пп.1 и 2, в котором фторорганическое соединение представляет [18F]фторпропилхолин формулы 10
Формула 10
Figure 00000010
RU2007126814/04A 2004-12-15 2005-12-09 Способ получения [18f]фторорганических соединений в спиртовых растворителях RU2357947C2 (ru)

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EP2017359A3 (en) 2007-06-11 2009-08-05 Trasis S.A. Method for the elution of 18F fluoride trapped on an anion-exchange resin in a form suitable for efficient radiolabeling without any evaporation step
KR101009712B1 (ko) * 2007-02-22 2011-01-19 재단법인 아산사회복지재단 양성자성 용매와 이에 녹는 염들을 이용한 음이온 교환고분자 지지체로부터의 플루오린-18 플루오라이드 용리와이를 이용한 플루오린-18의 표지방법
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