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Positron labeled phorbol ester: Synthesis method for “non-carrier added” phorbol 13-[1-11C] butyrate using ketene reaction

✍ Scribed by Yoshio Imahori; Ryou Fujii; Tatsuo Ido; Kimiyoshi Hirakawa; Hisamitsu Nakahashi


Publisher
John Wiley and Sons
Year
1989
Tongue
French
Weight
344 KB
Volume
27
Category
Article
ISSN
0022-2135

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✦ Synopsis


A new method was developed to s y n t h e s i z e positron labeled phorbol [ l -l k ] propyl ketene was produced b y t h e p y r o l y t i c e s t e r s for second messenger imaging based on a receptor binding to protein kinase C . decomposition of [ 1 -l l C b u t y r i c a c i d . This new method was made possible b y t h e reaction of [ l-llC]propyl ketene to t h e h y d r o x y l group of phorbol under the non-carrier added conditions. The p r e c u r s o r protected i n t h e 20-hydroxyl group of phorbol was acylated b [ 1-l l C Ipropyl ketene to t h e 13-hydroxyl group producing phorbol 13-[ C lbutyrate ( [ l1 C ] P13Bu) .

Total s y n t h e s i s time was about 60 minutes and t h e specific a c t i v i t y was greater than 67 G B q / p o l (1800 mCi/urnol).