350255-25-3Relevant academic research and scientific papers
Total synthesis and radiolabelling of an efficient rt-PA inhibitor: [11C] (Z,Z)-BABCH. A first route to [11C] labelled amidines
Simeon,Sobrio,Gourand,Barre
, p. 690 - 694 (2001)
A rapid route for the synthesis of radiolabelled t-PAstop 8, an efficient serine protease inhibitor, is described. (E,E)-2,7-Bis(4-iodobenzylidene)cycloheptan-1-one 2a was obtained in high yields (>90%) from cycloheptanone and 4-iodobenzaldehyde, with the unprecedented use of CsOH or by microwave irradiation using catalytic amounts (11CN] followed by palladium catalysis to give the labelled bisnitrile 7 was 80-90%. A series of experiments with various methods is reported and the first procedure for the preparation of [11C]amidines from the corresponding [11C]bisnitriles with N-acetylcysteine is presented; the radiochemical yield, based on analytical liquid chromatography was 80% for the radioamidination. [11C]t-PAstop was isolated in a radiochemical yield ranging from 50 to 60% in 55 min overall and with a radiochemical purity higher than 95%.
