A method for the preparation of folates labeled with 18F

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专利权人:

MERCK & CIE

发明人:

AMETAMEY, SIMON MENSAH,MOSER, RUDOLF,ROSS, TOBIAS LUDWIG,LAM, PHOEBE,GROEHN, VIOLA

申请号：

ES08736117

公开号：

ES2449774T3

申请日:

2008.04.11

申请国别(地区):

ES

年份:

2014

代理人:

摘要：

A direct radiolabeling method of the glutamate moiety of a folate compound with 18F, comprising the stage of reacting a compound of formula VII or VIIa with 18F, wherein X1 to X5 are N, X6, X7 are, independently of each other, O or N, R1, R2 are, independently of each other, H, Hal, -OR ', -NHR', C1-C12 alkyl, C1-C12 alkoxy, C1-C12 alkanoyl, C2-C12 alkenyl, C2-C12 alkynyl , (C1-C12 alkoxy) carbonyl or (C1-C12-amino) carbonyl alkyl, where R 'is H or C1-C6 alkyl, R3, R4 are, independently of each other, H, formyl, iminomethyl, nitrous, C1 alkyl -C12, C1-C12 alkoxy, C1-C12 alkanoyl, halo substituted C1-C12 alkanoyl, R5 is H, CN, Hal, NO2, C1-C12 alkyl, C1-C12 alkoxy, C1-C12 alkanoyl, C2-C12 alkenyl , C2-C12 alkynyl, (C1-C12 alkoxy) carbonyl, (C1-C12-amino) carbonyl alkyl, R6, R7 are, independently of one another, H or C1-C12 straight or branched chain alkyl, which is substituted or is substituted with at least one CN, Hal or NO2, S2 e s C1-C12 straight or branched chain alkyl, which is not substituted or substituted with at least one CN, Hal or NO2, and wherein one or more of the non-adjacent CH2 groups can be independently replaced by -O-； or a five or six membered aromatic ring having 0, 1 or 2 heteroatoms, which is not substituted or substituted with CN, Hal, NO2, COR 'or COOR', wherein R'representa H or C1-C6 alkyl, or a combination thereof, m is 1, p is 0, 1 or 2, q has a value of 1 to 7, Z is a labile group, and wherein 18F is activated by phase transfer catalysts such as tetrabutylammonium carbonate or aminopolyethers (eg Kryptofix © 2.2.2) combined with carbonate or potassium oxalate.Un método de radiomarcaje directo del resto glutamato de un compuesto de folato con 18F, que comprende laetapa de hacer reaccionar un compuesto de fórmula VII o VIIa con 18F, en donde X1 a X5 son N, X6, X7 son, independientemente uno de otro, O o N, R1, R2 son, independientemente uno de otro, H, Hal, -OR', -NHR', alquilo C1-C12, alcoxi C1-C12, alcanoílo C1-C12, alquenilo C2-C12, al

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