Synthesis of 14C‐labelled 2‐aminothiazole, 2‐amino‐5‐nitrothiazole, 2‐chloro‐5 nitrothiazole, and 1‐(5‐nitro‐2‐thiazolyl)‐2‐imidazolidinone (active substance of ambilhar®)
- 1 April 1969
- journal article
- Published by Wiley in Journal of Labelled Compounds and Radiopharmaceuticals
- Vol. 5 (2) , 173-180
- https://doi.org/10.1002/jlcr.2590050211
Abstract
A description is given of the preparation of 1‐(5‐nitro‐2‐thiazolyl)‐2‐imidazolidinone (active substance of the antiparasitic drug AMBILHAR®) in labelled form. By introducing 14C into the molecule, at position 4 of the imidazolidinone ring in one case and at position 2 of the thiazole ring in the other case, two differently labelled preparations were produced. The specific aetivities were 2.5 mCi/mmole and 0.33 mCi/mmole respectively. As intermediate products and by‐products of the syntheses, three further derivatives of 14C‐thiazole which have not hitherto been described were obtained, i.e. 2‐aminothiazole‐2‐14C, 2‐amino‐5‐nitrothiazole‐2‐14C, and 2‐chloro‐5‐nitrothiazole‐2‐14C.Keywords
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