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Synthesis of [ 3 H]‐1‐[1‐(3‐isothiocyanatophenyl) cyclohexyl]piperidine (METAPHIT), an acylating agent for phencyclidine receptors
Author(s) -
De Costa Brian R.,
Lessor Ralph A.,
Thurkauf Andrew,
Highet Robert J.,
Jacobson Arthur E.,
Rice Kenner C.
Publication year - 1989
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.2580270906
Subject(s) - piperidine , chemistry , phencyclidine , electrophile , acylation , yield (engineering) , stereochemistry , chemical synthesis , medicinal chemistry , receptor , organic chemistry , biochemistry , in vitro , nmda receptor , materials science , metallurgy , catalysis
The preparation of [ 3 H]‐labelled 1‐[1‐(3‐isothiocyanatophenyl) cyclohexyl]piperidine (METAPHIT), an electrophilic acylating agent for the phencyclidine (PCP) site is described. Synthesis of [ 3 H]METAPHIT was accomplished in three steps starting from 1‐[1‐(3‐nitrophenyl)cyclohexyl]piperidine. Introduction of the tritium‐label in 20.6% radiochemical yield was achieved in the penultimate step.