Cyanation

Cyanation

The Modification of Histidine Residues

Published in Roger L. Lundblad, Chemical Reagents for Protein Modification, 2020

The cyanation of histidine residues (Figure 5) in myoglobin using an equimolar ratio of cyanogen bromide and protein at pH 7.0 has been reported.27,28 This derivative is somewhat unstable but has proved useful in spectral studies (NMR, IR, UV-VIS) of this protein.

Absorption, distribution, metabolism and excretion of darolutamide (a novel non-steroidal androgen receptor antagonist) in rats

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Journal Information

Published in Xenobiotica, 2020

Päivi Taavitsainen, Hille Gieschen, Timo Korjamo, Marja Kähkönen, Chira Malmström, Olaf Prien, Michael Niehues, Steffen Sandmann, Wiebke Janssen, Mikko Koskinen

Darolutamide is a 1:1 mixture of two diastereoisomers, (S,R)- and (S,S)-darolutamide. Labelling synthesis of [14C]darolutamide was performed using cuprous [14C]cyanide to introduce the cyano label into the phenyl moiety of darolutamide. Cyanation of a bromo precursor and subsequent reduction of the keto group produced [14C]darolutamide. The labelling site has been considered as metabolically stable. The radiochemical purity was checked before any use and was >98%; the specific radioactivity was 2.3–2.6 MBq/mg.

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The Modification of Histidine Residues

Absorption, distribution, metabolism and excretion of darolutamide (a novel non-steroidal androgen receptor antagonist) in rats