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The synthesis of several tritiated non‐nucleoside, HIV‐1 reverse transcriptase inhibitors
Author(s) -
Hamill Terence G.,
Brenner Nancy J.,
Eng Waisi,
Burns H. Donald
Publication year - 1998
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/(sici)1099-1344(199804)41:4<319::aid-jlcr84>3.0.co;2-s
Subject(s) - chemistry , tritiated water , reverse transcriptase , tritium , benzoxazole , chemical synthesis , thymidine , nucleoside , ring (chemistry) , nucleoside reverse transcriptase inhibitor , stereochemistry , radiochemistry , biochemistry , organic chemistry , rna , in vitro , physics , nuclear physics , gene
The synthesis of three tritiated reverse transcriptase inhibitors is described herein. These compounds contained the benzoxazole ring linked to a 2‐pyridinone ring by an aminomethylene group. The tritiated compounds were synthesized by hydrologenolysis of bromobenzoxazole precursors. The final tritiated compounds had specific activities ranging from 3–10 Ci/mmol. © 1998 John Wiley & Sons, Ltd.