Process for synthesis of azetidine and novel intermediates therefor
摘要
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.
申请公布号
US4966979(A)
申请公布日期
1990.10.30
申请号
US19890341994
申请日期
1989.04.24
申请人
A. H. ROBINS COMPANY, INCORPORATED
发明人
LO, YOUNG S.;SHAMBLEE, DWIGHT A.;CAUSEY, DAVID H.;MAYS, RICHARD P.