COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES;COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES
发明人:
BARRE, Louisa,MARCHAND, Patrice
申请号：
ES08869353
公开号：
ES2654528T3
申请日:
2008.12.23
申请国别(地区):
ES
年份:
2018
代理人:
摘要：
Process for preparing a 2-fluoro-purine derivative labeled with radioisotope 18F of formula ** Formula ** in which R2 represents H, an optionally substituted alkyl group, an optionally substituted aryl group, an optionally substituted furanose group or a optionally substituted pyranous group, R3 represents H, an optionally substituted alkyl group, an optionally substituted aryl group, a halogen, a -OR8 group or a -SR8 group, representing R8 H, an optionally substituted alkyl group or an optionally substituted aryl group, said process comprising the following successive steps consisting in: a) reacting a protected 2-nitro-purine derivative of formula (Ic) ** Formula ** in which R and R 'are protective groups, identical or different, chosen of an optionally substituted alkyl group, an optionally substituted acyl group, an optionally substituted aryl group, an optionally substituted benzyl group, a group optionally substituted benzoyl, an electroatractor group, an optionally substituted sulfinyl group, an optionally substituted sulfonyl group, a trityl group, a silyl group, a tert-butoxycarbonyl group (BOC), a fluorenylmethoxycarbonyl group (FMOC) and an imide derivative or a imine derivative, and R2 and R3 are as defined above, with a source of fluoride ions labeled with [18F] in a solvent that is acetonitrile, at a temperature of 55 to 60 ° C and for a period between 1 and 30 min, to obtain a protected 2- [18F] fluoro-purine derivative and possibly a partially unprotected 2- [18F] fluoro-purine derivative, said 2- [18F] fluoro-purine protected derivative of formula (Id ) ** Formula ** being R2, R3, R and R 'as defined above, said derivative of 2- [18F] being partially unprotected fluoro-purine of formula (Ie) ** Formula ** being R2, R3 and R as defined above, b) check out dich or derivative of 2- [18F] protected fluoro-purine and said partially unprotected 2- [18F] fluoro-purine derivative possibly obtained to obtain the 2- [18F] fluoro-purine derivative by reacting
