Process for synthesis of azetidine and novel intermediates therefor
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United States of America Patent
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Oct 30, 1990
Issued Date -
N/A
app pub date -
Apr 24, 1989
filing date -
Jan 28, 1987
priority date (Note) -
Expired
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Abstract
A novel process is described for preparing azetidine and 2 or 3 methyl and ethyl azetidine free bases by reacting primary arylmethylamine having suitable bulk providing substituents attached to the methyl carbon and an appropriate propane derivative having leaving groups in the one and three position in hot organic solvent containing a non-nucleophilic base and an amount of water sufficient to promote azetidine ring formation to give N-protected-azetidines and deprotecting by hydrogenolysis under acidic conditions to give an acid salt of the azetidines and thereafter flashing off vaporized azetidine from a hot, agitated strong base solution or slurry and condensing to give the liquid azetidine free bases.
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