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Synthesis of a tritium labelled analog of the novel hematoregulatory agent SB 209978
Author(s) -
Heerding Dirk,
Saunders David
Publication year - 1997
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(199706)39:6<455::aid-jlcr997>3.0.co;2-4
Subject(s) - hydrogenolysis , chemistry , regioselectivity , diamine , tritium , palladium , catalysis , organic chemistry , combinatorial chemistry , physics , nuclear physics
[ 3 H]SB 209978 ( 10 ) was synthesized in 6 steps from phenylene diamine dihydrochloride. A key aspect was the regioselective synthesis of 6‐chloropicolinic acid ( 7 ). This was condensed with diamine 6 and the resulting product was deprotected to give 9 . Palladium catalyzed 3 H‐hydrogenolysis of the chloropyridine rings gave the final product 10 . © John Wiley & Sons, Ltd.