4.4 Article

A Straightforward Access to [14C]- and [13C]-Labeled 2-Aminobenzoxazoles and Benzothiazoles via a KCN Polarity Inversion Strategy

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SYNLETT
卷 27, 期 12, 页码 1798-1802

出版社

GEORG THIEME VERLAG KG
DOI: 10.1055/s-0035-1562116

关键词

2-aminobenzoxazoles; 2-aminobenzothiazoles; electrophilic cyanating agent; isotopic labeling; carbon; cyanide

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A convenient one-pot synthetic access to 2-aminobenzoxazoles and 2-aminobenzothiazoles has been developed. The protocol uses KCN as starting material and proceeds through an in situ polarity inversion step. This approach provides a new valuable and straightforward entry to carbon-14-radiolabeled pharmaceutically relevant heterocycles and substantially reduces as well the amount of radioactive wastes generated.

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