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Preparation of N.C.A. [17-18F]-fluoroheptadecanoic acid in high yields via aminopolyether supported, nucleophilic fluorination

✍ Scribed by Heinrich Hubert Coenen; Manfred Schüller; Gerhard Stöcklin; Bernd Klatte; Arndt Knöchel

Publisher
John Wiley and Sons
Year
1986
Tongue
French
Weight
445 KB
Volume
23
Category
Article
ISSN
0022-2135

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✦ Synopsis

A macrocyclic aminopolyether (Kryptofix 2.2.2.) supported labelling method for the preparation of n.c.a. [17-FIfluoroheptadecanoic acid is described. The equimolar complex of potassium carbonate and the aminopolyether

is used to provide nucleophilicity in a homogeneous solution of acetonitrile. Nucleophilic "F-for-Br substitution in the methylester of 17-bromoheptadecanoic acid is accomplished with radiochemical yields of 9 4 + 3%. Subsequent quantitative ester hydrolysis with KOH leads to a simple "one pot" procedure. Minimization of reagent concentrations allows a direct isolation of the product from the reaction mixture by means of reverse phase HPLC. The corrected radiochemical yield of high activity level routine production is 82 + 2% after 90 minutes of synthesis time. The specific activity is > 10,000 Ci/mmol.

📜 SIMILAR VOLUMES

Preparation of N.C.A. [18F]-CH2BrF via a
Preparation of N.C.A. [18F]-CH2BrF via aminopolyether supported nucleophilic substitution
✍ Heinrich Hubert Coenen; Marcello Colosimo; Manfred Schüller; Gerhard Stöcklin 📂 Article 📅 1986 🏛 John Wiley and Sons 🌐 French ⚖ 295 KB

A complex of the macrocyclic aminopolyether Kryptof ix@ 2.2.2. and potassium carbonate was used to synthesize [ 18F] -CH2BrF from dibromomethane. At the no-carrier-added level the nucleophilic 18F-for-Br exchange gives rise to a corrected radiochemical yield up to 62%.