Journal
SYNLETT
Volume 27, Issue 12, Pages 1798-1802Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0035-1562116
Keywords
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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