ASYMMETRIC-SYNTHESIS OF (2S) AND (2R)-4-(3-T-BUTYLAMINO-2-HYDROXYPROPOXY)-BENZIMIDAZOL-2-[C-11]-ONE ((S) AND (R)-[C-11]-CGP-12177) FROM OPTICALLY-ACTIVE PRECURSORS

被引:29
作者
HAMMADI, A
CROUZEL, C
机构
[1] Service Hospitalier Frédéric Joliot, C.E.A., Orsay, 91406, D.R.I.P.P.
关键词
ASYMMETRIC SYNTHESIS; CGP-12177; ENANTIOMERS; C-11; PET; BETA-RECEPTOR;
D O I
10.1002/jlcr.2580290609
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Enantiomers of CGP 12177 ((2S)-and (2R)-4-(3-t-butylamino-2-hydroxypropoxy)-benzimidazol-2-one), a potent adrenergic beta-receptor antagonist were synthesized and labelled with C-11 for Positron Emission Tomography studies of beta-receptors in heart. The synthesis was accomplished from (2S)-and (2R)-3-tosyloxy-1,2-propanediol acetonide. Enantiomeric excess was greater than 95% for each of the prepared enantiomers. (S)- and (R)-[C-11]-CGP 12177 were obtained with a specific radioactivity of 29.6-44.4 GBq/mu-mol.
引用
收藏
页码:681 / 690
页数:10
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