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Studies towards the synthesis of stable isotope labeled PNU‐95666, a CNS agent currently under development for the treatment of Parkinson's disease, is described. The synthesis of non‐labeled PNU‐95666 starts using a large excess of methylamine. While the non‐labeled methylamine is inexpensive and in plentiful supply, the stable isotope labeled form is expensive and limited availability. Different synthetic routes and conditions, including the use of different aminating agents and various amounts of methylamine were explored and new synthetic conditions were established. Copyright © 2004 John Wiley & Sons, Ltd.
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