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A simple synthesis of 3 H‐labelled ubenimex
Author(s) -
Koyama Michinori,
Saino Tetsushi
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.2580251202
Subject(s) - chemistry , chromatography , deuterium , high performance liquid chromatography , thin layer chromatography , quantum mechanics , physics
3 H‐Labelled ubenimex, N‐ (2S,3R)‐3‐amino‐2‐hydroxy‐4‐( o ‐ 3 H)phenylbutyrl)‐S‐leucine with a specific radioactivity of 15 mCi/mg was synthesized by a one step catalytic tritiation of N‐ ((2S,3R)‐3‐benzyloxycarbonylamino‐2‐hydroxy‐4‐( o ‐bromo)phenylbutyryl)‐S‐leucine benzyl ester previously isolated from a mixture of four optical isomers using preparative high performance liquid chromatography. Chemical and radiochemical purities were over 99% as determined by thin layer chromatography and high performance liquid chromatography using radioisotope detection. By gas chromatography‐mass spectrometric analysis of deuterated ubenimex, the 3 H‐label was determined to be in the aromatic ring.