An improved one-pot procedure for the preparation of [¹¹C-carbonyl]-WAY100635

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• 作者：Hwang1 ; Dah-Ren ; Simpson ; Norman R. ; Montoya ; Julie ; Mann2 ; J. John ; Laruelle2 ; Marc
• 关键词：5HT1A receptor ; WAY100635 ; Carbon-11 ; Antagonist ; PET
• 刊名：Nuclear Medicine and Biology
• 出版年：1999
• 出版时间：October, 1999
• 年：1999
• 卷：26
• 期：7
• 页码：815-819
• 全文大小：288 K

文摘

A simple one-pot procedure for the preparation of [¹¹C-carbonyl]-WAY100635, a potent 5HT1A receptor antagonist, was developed. The procedure involves the trapping of ¹¹CO₂ in a tetrahydrofuran (THF) solution of cyclohexylmagnesium chloride, elimination of excess Grignard reagents with anhydrous HCl, reaction with SOCl₂, and the reaction of the resulting acid chloride with WAY100634 (2 mg) and triethylamine (20 μL) in THF. The total synthesis time is 45 min. Starting from 1326 ± 173 mCi of ¹¹CO₂, the average amount of [¹¹C-carbonyl]-WAY100635 ( n