دورية أكاديمية

Mild, Organo-Catalysed Borono-Deamination as a Key to Late-Stage Pharmaceutical Precursors and 18 F-Labelled Radiotracers.

التفاصيل البيبلوغرافية
العنوان: Mild, Organo-Catalysed Borono-Deamination as a Key to Late-Stage Pharmaceutical Precursors and 18 F-Labelled Radiotracers.
المؤلفون: Pérez-García RM; Section of Organic Chemistry, Department of Chemistry, University of Oslo, Oslo, Norway., Riss PJ; Section of Organic Chemistry, Department of Chemistry, University of Oslo, Oslo, Norway.; Division of Clinical Neuroscience, Oslo University Hospitals HF, Oslo, Norway.; GIGA Cyclotron Research Centre, Department of Chemistry, Liège, Belgium.; Department of Chemistry, Johannes Gutenberg-University, Mainz, Germany.
المصدر: Frontiers in chemistry [Front Chem] 2022 Apr 26; Vol. 10, pp. 884478. Date of Electronic Publication: 2022 Apr 26 (Print Publication: 2022).
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: Frontiers Media S.A Country of Publication: Switzerland NLM ID: 101627988 Publication Model: eCollection Cited Medium: Print ISSN: 2296-2646 (Print) Linking ISSN: 22962646 NLM ISO Abbreviation: Front Chem Subsets: PubMed not MEDLINE
أسماء مطبوعة: Original Publication: Lausanne : Frontiers Media S.A., [2013]-
مستخلص: A tris(pentafluorophenyl)borane catalysed method for the synthesis of boronic acid esters from aromatic amines in yields of up to 93% was devised. Mild conditions, benign reagents, short reaction times, low temperatures and a wide substrate scope characterize the method. The reaction was found applicable to the synthesis of boronic acid ester derivatives of complex drug molecules in up to 86% isolated yield and high purity suitable for labelling. These boronates were subsequently labelled with [ 18 F]fluoride ion in radiochemical yields of up to 55% with and even without isolation of the boronate-intermediate.
Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.
(Copyright © 2022 Pérez-García and Riss.)
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فهرسة مساهمة: Keywords: aromatic amines; aryl boronates; boronato-deamination; drug molecules; lewis acid-catalysis; positron emission tomography; radiofluorination
تواريخ الأحداث: Date Created: 20220513 Latest Revision: 20220716
رمز التحديث: 20231215
مُعرف محوري في PubMed: PMC9089349
DOI: 10.3389/fchem.2022.884478
PMID: 35559222
قاعدة البيانات: MEDLINE
الوصف
تدمد:2296-2646
DOI:10.3389/fchem.2022.884478