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Site ‐specific deuteration or tritiation of benzo [b] thiophene and 1‐ methylindole analogs of biologically active indole derivatives (1)
Author(s) -
Bosin T. R.,
Rogers R. B.
Publication year - 1973
Publication title -
journal of labelled compounds
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0022-2135
DOI - 10.1002/jlcr.2590090302
Subject(s) - indole test , chemistry , metalation , thiophene , biological activity , tritium , stereochemistry , deuterium , medicinal chemistry , organic chemistry , in vitro , biochemistry , physics , quantum mechanics , nuclear physics
The site‐specific deuteration and tritiation of 1‐methylindole and benzo [b] ‐thiopheme analogs of biologically active indole derivatives has been achieved by use of the facile metalation of these heterocycles with n‐butyllithium and subsequent reaction with 2 H 2 or 3 H 2 O. Metalation occurs at the 2‐position and site and extent of deuterium incorporation was determined by N. M. K. The use of similar procedures with 3 H 2 O led to ready incorporation of tritium into these heterocycles.