CAS: 107128-00-7; 1-Benzhydrylazetidine

该化合物是一种含氮的环环化合物,其特点是用二苯甲基组物替代了一种环,具有独特的消毒和电子特性,使其成为制药和农用化学合成中有价值的中间体.亚氮环具有相近性,加强了药物设计中的结合性,加强了药物设计中的粘合性,而二苯甲基组物则有助于亲脂性和代谢稳定性.其紧凑,紧凑的环系系统有利于生物活性分子的调制药理动力学特征.该化合物因其平衡的极地性和成份性,在开发CNS目标剂,酶抑制剂和受体调节器方面特别有用.该化合物具有较高的纯度,可用于研究应用,确保合成分子的再生性.

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欧盟法规

ECHA物质C&L通报

上下游产品

toluene-4-sulfonic acid 1-benzhydryl-azetidin-3-yl ester 1-benzhydryl-3-azetidinyl methanesulfonate 1.3-chlorobromopropane Benzhydrylamine azetidine N-γ-aminopropyltrimethyleneimine Diphenylmethane azetidine hydr°Chloride

合成工艺路线路线简述

    📜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.

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    ✅ COA系统入驻 | 共享模式

    合成参考文献


    摘要:Couty, F., Science of Synthesis, (2009) 40, 773.
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