Synthesis of substituted Calix[6] arene and 18F labeling reaction as catalyst in preparation of 18F-FET

The phase transfer catalyst Substituted Calix[6] arene was prepared and it was used as catalyst to prepare the tumor diagnostic drug 18F-FET. The results showed that para-sulfonated-calix[6] arene not only catalyzes 19F substitution reaction, but also catalyzes 18F labelling reaction with radiochemical yield of 11%. However, para-tert-butyl-calix[6] arene has no catalytic activity for the 19F substitution reaction nor the 18F labelling reaction of the precursor of FET. The catalyzing of para-sulfonated-calix[6]arene may be related to it's sulfonate groups, which participated in the coordination reaction and increased the polarity of calyx[6] arene and so on. Although radiochemical yield of the para-sulfonated-calix[6] arene catalyzed 18F labeling of the precursor of FET was much lower than that obtained by Kryptofix 2. 2. 2, this study still has significant meaning for us to find better substituted Calix[6] arene catalysts by optimizing the reaction conditions. (authors)