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Synthesis of tritium-labelled BIBN4096, an experimental h-CGRP-antagonist

✍ Scribed by V. P. Shevchenko; I. Yu. Nagaev; N. F. Myasoedov; A. B. Susan; K.-H. Switek; H. Braunger

Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
140 KB
Volume
49
Category
Article
ISSN
0022-2135

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✦ Synopsis

Synthesis of tritium labelled BIBN 4096 -1-piperidine-

antagonist for the treatment of migraine is described. Selective tritiation of a heterocyclic aromatic fragment in the presence of aromatic ring in a precursor of BIBN4096 was successfully carried out using the solid state catalytic exchange method. Subsequent completion of the synthesis sequence gave the final [ 3 H]BIBN4096 with a specific activity of >170 Ci/mmol.

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