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Synthesis of (5‐methyl‐2‐oxo‐1,3‐dioxol‐4‐YL)methyl 7‐[D‐O‐(L‐alanyl)[β‐ 14 C]mandelamido]‐3‐[[(5‐methyl‐1,3,4‐thiadiazol‐2‐YL)thio]methyl]‐3‐cephem‐4‐carboxylate and its active compound
Author(s) -
Nishizawa Susumu,
Matsui Hiroshi,
Ohkubo Akio,
Kakeya Nobuharu,
Kiritani Reiko
Publication year - 1988
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580250505
Subject(s) - chemistry , mandelic acid , thio , medicinal chemistry , organic chemistry
(5‐Methyl‐2‐oxo‐1,3‐dioxol‐4‐yl)methyl 7‐[D‐O‐(L‐alanyl)[β‐ 14 C]‐mandelamido]‐3‐[[(5‐methyl‐1,3,4‐thiadiazol‐2‐yl)thio]methyl]‐3‐cephem‐4‐carboxylate ( 14 C‐KY‐109) and its parent drug ( 14 C‐KY‐087) were synthesized from D‐(‐)‐mandelic‐β‐ 14 C acid prepared by optical resolution of DL‐(±)‐ mandelic‐β‐ 14 C acid. The overall radiochemical yields were 16.2% for 14 C‐KY‐087 and 49.6% for 14 C‐KY‐109, based on D‐(‐)‐mandelic‐β‐ 14 C acid. Both the products had radiochemical purities greater than 97% as measured by TLC.