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СПОСОБ ПОЛУЧЕНИЯ F-18 МЕЧЕННЫХ ПРОИЗВОДНЫХ ГЛУТАМИНОВОЙ КИСЛОТЫ
专利权人:
БАЙЕР ФАРМА АКЦИЕНГЕЗЕЛЬШАФТ (DE)
发明人:
БЕРНДТ Матиас (DE),ШМИТТ-ВИЛЛИХ Херберт (DE),ФРИБЕ Маттиас (DE),ГРЭМ Кейт (DE),БРУМБИ Томас (DE),ХУЛЬЧ Кристина (DE),ВЕСТЕР Ханс-Юрген (DE),ВАГНЕР Франциска (DE)
申请号:
RU2012124810/04
公开号:
RU2012124810A
申请日:
2010.11.06
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
1. A process for preparing a compound of formula Ikotory comprises steps of: Step 1: Synthesis of radiolabeled compounds of formula III by reacting a compound of formula II with the F-18 fluorinating agent Step 2: Deprotection of compounds of formula III to obtain a compound of formula I, Step 3: Purification and preparation of compounds of formula I wherein: X is selected from the group vklyuchayuscheya) connection, b) branched or unbranched (C2-C10) alkyl, c) branched or unbranched (C2-C10) alkoxy, d) branched or unbranched (C3-C10) alkenyl, e) p zvetvlenny or unbranched (C3 -C10) alkynyl, f) [(CH) -O] - (CH), Id) O - [(CH) -O] - (CH) n = 2-6, preferably n = 2 or 3 m = 1-3, preferably m = 1 or 2 a = 2-6, preferably a = 2 or 3 R and R is carboxyl-protecting group and wherein the carboxyl-protecting group is independently selected IZA) branched or unbranched (C-C) alkyl, b) benzyl, and c) allyl r and independently from each other are selected from the group consisting of: a ) hydrogen, b) an amino-protecting group ilic) NRRpredstavlyaet group is 1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl (phthalimido) or azido group iohvatyvaya their individual isomers, tautomers, diastereomers, enantiomers, mixtures thereof and suitable soli.2. A method according to claim 1, wherein Step 3 includes a solid-phase extraction, preferably cation exchange fazu.3 solid. A method according to claims 1 and / or 2, wherein the reaction [F] fluorination as described in Step 1 is carried out at 0 ° C - 160 ° C.4. A method according to claim 1 or 2, wherein [F] the fluorinating agent used in Step 1, form of a base and [F] fluoride and the ratio of the base and the compound of formula II is greater than zero (> 0) and equal to or less than 1 (≤1) .5. The method Correspondingly1. Способ получения соединения формулы Iкоторый включает стадии:Стадия 1: Синтезирование радиоактивно меченного соединения формулы III путем взаимодействия соединения формулы II с F-18 фторирующим агентом,Стадия 2: Отщепление
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