4-苯胺类阿片苷衍生物对μ-阿片受体的体内成像

IF 1 4区化学 Q4 CHEMISTRY, ORGANIC

Letters in Organic Chemistry Pub Date : 2020-03-31 DOI:10.2174/1570178616666190905144136

J. Marton, Attila Sipos, S. Berényi, Brita Glaenzel, G. Henriksen

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引用次数: 1

摘要

以4-苯基氨基-1-苄基-4-哌啶羧酸为原料，建立了2-氟丙酰基卡芬太尼的克级制备方法。合成了2-氟丙酰基-卡芬太尼羧酸和2-氯丙酰基-卡芬太尼作为前体，通过两种不同的反应途径辐射合成11Can和/或18F标记的2-氟丙酰-卡芬太尼衍生物。采用计算方法对2-氟丙酰基卡芬太尼的构象进行了分析。给出了计算的1H和13C-NMR位移。

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4-Anilidopiperidine Derivatives for in vivo Imaging of μ-Opioid Receptors

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.

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来源期刊

Letters in Organic Chemistry 化学-有机化学

CiteScore

1.30

自引率

12.50%

发文量

135

审稿时长

7 months

期刊介绍： Aims & Scope Letters in Organic Chemistry publishes original letters (short articles), research articles, mini-reviews and thematic issues based on mini-reviews and short articles, in all areas of organic chemistry including synthesis, bioorganic, medicinal, natural products, organometallic, supramolecular, molecular recognition and physical organic chemistry. The emphasis is to publish quality papers rapidly by taking full advantage of latest technology for both submission and review of the manuscripts. The journal is an essential reading for all organic chemists belonging to both academia and industry.