📜1-二苯甲基-3-甲烷磺酸氮杂环丁烷置于sodium Tetrahydroborate体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 3.0H,以81%的收率获得1-二苯甲基氮杂环丁烷 参考文献:Synthesis Of Azetidine From 1-Substituted Azetidin-3-Ols 标题:Synthesis Of Azetidine From 1-Substituted Azetidin-3-Ols 摘要: Doi:10.3987/r-1986-09-2467
专利信息
专利号:US-4870189-A 优先权日:1987-01-28 标 题:Process for synthesis of azetidine and novel intermediates therefor 发明人:LO YOUNG S; SHAMBLEE DWIGHT A; CAUSEY DAVID H; MAYS RICHARD P 权利人:ROBINS CO INC A H 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.
专利号:US-4966979-A 优先权日:1987-01-28 标题 :Process for synthesis of azetidine and novel intermediates therefor 发明人:LO YOUNG S; SHAMBLEE DWIGHT A; CAUSEY DAVID H; MAYS RICHARD P 权利人:ROBINS CO INC A H 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.