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Synthesis of 14 C‐labelled 2‐aminothiazole, 2‐amino‐5‐nitrothiazole, 2‐chloro‐5 nitrothiazole, and 1‐(5‐nitro‐2‐thiazolyl)‐2‐imidazolidinone (active substance of ambilhar®)
Author(s) -
Faigle J. W.,
Keberle H.
Publication year - 1969
Publication title -
journal of labelled compounds
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0022-2135
DOI - 10.1002/jlcr.2590050211
Subject(s) - nitro , thiazole , chemistry , ring (chemistry) , stereochemistry , organic chemistry , alkyl
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 14 C 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 14 C‐thiazole which have not hitherto been described were obtained, i.e. 2‐aminothiazole‐2‐ 14 C, 2‐amino‐5‐nitrothiazole‐2‐ 14 C, and 2‐chloro‐5‐nitrothiazole‐2‐ 14 C.