A method for gram scale preparation of 2-fluoropropionyl-carfentanil was established, starting from 4-phenylamino-1-benzyl-4-piperidinecarboxylic acid. 2-Fluoropropionyl-carfentanil carboxylic acid and 2-chloropropionyl-carfentanil as precursors were synthesized for the radiosynthesis of 11C and/or 18F labelled 2-fluoropropionyl-carfentanil derivatives via two separate reaction routes. Conformational analysis of 2-fluoropropionyl-carfentanil was performed using computational methods. Calculated 1H and 13C-NMR shifts are presented.

中文翻译：

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用于μ阿片受体的体内成像的4-Anilidopiperidine衍生物

从4-苯基氨基-1-苄基-4-哌啶羧酸开始，建立了一种克级制备2-氟丙酰基-芬太尼的方法。合成了2-氟丙酰基-芬太尼羧酸和2-氯丙酰基-芬太尼作为前体，通过两种独立的反应路线，放射性合成了11C和/或18F标记的2-氟丙酰基-芬太尼衍生物。使用计算方法对2-氟丙酰基-芬太尼进行构象分析。给出了计算的1H和13C-NMR位移。