Асимметрический синтез предшественников для получения радиотрейсеров, используемых в позитронной эмиссионной томографии
Диссертация
Получены и охарактеризованы комплексы Ni" основания Шиффа (S)-0-бензофенона ((5)-ВРВ) и (1S, 2R)-, (УЯ^-Ьаминоциклопропан^Д-дикарбоновых кислот. Разложение комплексов с последующим выделением аминокислот — возможный путь получения (1S, 2R)-, (/5,25)-1-аминоциклопропан-1,2-дикарбоновых кислот, асимметрический синтез которых является не простой синтетической задачей. Я период полураспада изотопа F… Читать ещё >
Содержание
- 1. ЛИТЕРАТУРНЫЙ ОБЗОР
- 1. 1. КРАТКИЕ СВЕДЕНИЯ О МЕТОДЕ ПЭТ
- 1. 1. 1. Позитронная Эмиссионная Томография как метод диагностики. Основы метода
- 1. 1. 2. Изотопы, используемые в ПЭТ. Тенденция развития метода
- 1. 1. 3. Современные представления о механизме накопления меченных аминокислот в клетках
- 1. 1. 4. Некоторые перспективные [18Р]содержащие аналоги аминокислот для использования в ПЭТ
- 1. 2. МЕТОДЫ СЕЛЕКТИВНОГО ВВЕДЕНИЯ ИЗОТОПА 18F
- 1. 2. 1. Методы нуклеофильного фторирования
- 1. 2. 1. 1. Фторирование алифатических соединений
- 1. 2. 1. 2. Введение атома ,8 °F в алифатический фрагмент аминокислот
- 1. 2. 1. 3. Фторирование ароматических соединений
- 1. 2. 1. 4. Методы введения атома 18 °F в ароматический фрагмент аминокислот
- 1. 2. 2. Нуклеофильное замещение в ароматическом ядре, активированном лгкомплексообразованием с металлами
- 1. 2. 2. 1. Возможные механизмы активации ароматического нуклеофильного замещения атома галогена
- 1. 2. 2. 2. Каталитическое ароматическое нуклеофильное замещение атома галогена
- 1. 2. 2. 3. Нуклеофильное замещение галогена в стехиометрически активированном ароматическом ядре
- 1. 2. 1. Методы нуклеофильного фторирования
- 1. 1. КРАТКИЕ СВЕДЕНИЯ О МЕТОДЕ ПЭТ
- 3. 1. НОВЫЕ ПОДХОДЫ К ЗАМЕЩЕНИЮ РАЗЛИЧНЫХ УХОДЯЩИХ ГРУПП НА АТОМ ФТОРА
- 3. 1. 1. Каталитические методы замещения
- 3. 1. 2. Попытки нуклеофильного замещения в активированных аренхромтрикарбонильных комплексах переходных металлов
- 3. 2. НОВЫЙ МЕТОД СИНТЕЗА ИЗВЕСТНОГО РАДИОТРЕЙСЕРА
- 3. 2. 1. Синтез предшественников для получения
- 3. 3. РАЗРАБОТКА МЕТОДОВ СИНТЕЗА НОВОГО ПЕРСПЕКТИВНОГО РАДИОТРЕЙСЕРА И ЕГО ПРЕДШЕСТВЕННИКА
- 3. 3. 1. Синтез предшественника для получения (S)-4-[uF]
- 3. 3. 1. 1. Каталитический метод получения
- 3. 3. 1. 2. Стехиометрический метод синтеза
- 3. 3. 2. Асимметрический синтез 4-фторглутаминовой кислоты
- 3. 3. 2. 1. Краткие сведения о методах получения 4-фторглутаминовой кислоты
- 3. 3. 2. 2. Стехиометрический метод с использованием хиральных вспомогательных реагентов
- 3. 3. 3. Методика замещения атома брома на атом фтора в синтезированном ранее предшественнике
- 3. 3. 1. Синтез предшественника для получения (S)-4-[uF]
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