DOAJ Open Access 2022

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

Raúl M. Pérez-García Patrick J. Riss Patrick J. Riss Patrick J. Riss Patrick J. Riss

Abstrak

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 [18F]fluoride ion in radiochemical yields of up to 55% with and even without isolation of the boronate-intermediate.

Topik & Kata Kunci

Chemistry

Penulis (5)

Raúl M. Pérez-García

Patrick J. Riss

Format Sitasi

APA MLA BibTeX

Pérez-García, R.M., Riss, P.J., Riss, P.J., Riss, P.J., Riss, P.J. (2022). Mild, Organo-Catalysed Borono-Deamination as a Key to Late-Stage Pharmaceutical Precursors and 18F-Labelled Radiotracers. https://doi.org/10.3389/fchem.2022.884478

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Informasi Jurnal

Tahun Terbit: 2022
Sumber Database: DOAJ
DOI: 10.3389/fchem.2022.884478
Akses: Open Access ✓