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3 H‐labeling of prokinetic motilide ABT‐229 for biodistribution and metabolism studies
Author(s) -
Faghih Ramin,
BurnellCurty Cynthia,
Surber Bruce,
Shoghi Simin,
Borre Anthony,
Yao Ye,
Lartey Paul A.,
Nellans Hugh N.
Publication year - 1996
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(199607)38:7<687::aid-jlcr889>3.0.co;2-q
Subject(s) - chemistry , biodistribution , pharmacology , ketone , derivative (finance) , drug , stereochemistry , biochemistry , organic chemistry , in vitro , medicine , economics , financial economics
The prokinetic drug candidate, ABT‐229, has been successfully [ 3 H]‐labeled in the macrolactone ring. This was accomplished with [ 3 H]‐NaBH 4 reduction of the 11‐ketone analog in a four step synthetic sequence beginning with the drug candidate. The 3 H‐labeled drug was obtained with specific activity of 9.0 Ci/mmol and radiochemical purity >99%. This constitutes the first methodology for 3 H‐labeling of the macrolactone in an erythromycin derivative.