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A facile method for the preparation of [11C]cyanide from [11C]methyl iodide
https://repo.qst.go.jp/records/76124
https://repo.qst.go.jp/records/76124cd525b8b-c41d-479d-b918-b63ae009b2f9
Item type | 会議発表用資料 / Presentation(1) | |||||
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公開日 | 2019-05-30 | |||||
タイトル | ||||||
タイトル | A facile method for the preparation of [11C]cyanide from [11C]methyl iodide | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_c94f | |||||
資源タイプ | conference object | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
著者 |
Kikuchi, Tatsuya
× Kikuchi, Tatsuya× Ming-Rong, Zhang× D.Gee, Antony× Kikuchi, Tatsuya× Ming-Rong, Zhang |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Objectives. [11C]Cyanide is a useful intermediate for labelling functional groups such as CN, COOH, CONH2 and CH2NH2 in organic compounds. Conventional method for the preparation of [11C]cyanide, however, requires dedicated infrastructure. [11C]Cyanide is generally prepared by heating [11C]CH4 under NH3 gas flow at more than 900°C over a platinum filled column. Furthermore, the starting material, [11C]CH4, is produced by the irradiation of N2/H2 gas or by heating [11C]CO2 under H2 gas flow over nickel. In the previous meeting (ISRS2017), we reported that [11C]cyanide was prepared by the dehydration of [11C]formaldoxime, though the radiochemical yield was insufficient (around 20% from [11C]CO2). Thus, we explored more efficient method to prepare [11C]cyanide without any special equipment and reagents. In this study, we investigated the applicability of hydroxylamine-O-sulfonic acid (HOSA) to [11C]cyanide preparation from [11C]CH3I which is widely used for 11C-labelling. HOSA has been used as a reagent for the conversion of aldehydes into nitriles. Methods. [11C]CH3I (300–400 MBq) was trapped in a 1 mL of trimethylammonium oxide (TMAO, 15 mg) solution in DMF or DMSO and heated for 2 min to prepare [11C]HCHO (at 70°C for DMF solution, at 100°C for DMSO solution). The [11C]HCHO solution (200 μL) was subsequently added to the HOSA solution in the corresponding solvents (200 μL). The reaction conditions are summarized in Table 1. Radiochemical yields from [11C]CH3I were determined by radio-HPLC analysis of the reaction solution. More than 87% of radioactivity in the injected solution was eluted during the HPLC analysis. Results. The results are summarized in Table 1. Higher reaction temperature enhanced the formation of [11C]cyanide. The use of DMSO showed better yield of [11C]cyanide compared with DMF. The use of more than 1 equivalent of HOSA based on the amount of TMAO was required to obtain good yields of [11C]cyanide. Consequently, [11C]cyanide was produced in 87% radiochemical yield after 3 min reaction time. Conclusions. [11C]Cyanide was efficiently prepared from [11C]CH3I in one-pot using conventional reagents and lab-ware. Further optimization of reaction conditions for the production of [11C]cyanide with an automated system is in progress. |
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会議概要(会議名, 開催地, 会期, 主催者等) | ||||||
内容記述タイプ | Other | |||||
内容記述 | ISRS2019 (The 23rd International Symposium on Radiopharmaceutical Sciences) | |||||
発表年月日 | ||||||
日付 | 2019-05-28 | |||||
日付タイプ | Issued |