CAS: 145238-45-5; (R)-1,3,3-Triphenyltetrahydro-1H,3H-Pyrrolo[1,2-C][1,3,2]Oxazaborole

该化合物是一个复杂的有机化合物,其特点是其独特的双环结构,在其框架中结合了和氮.该化合物的特点是一个烧灼环,它与一个氧化辛-波洛(oxazbolo)运动结合在一起,有助于其独特的化学特性.多个苯基团体的存在增强了其稳定性,并可能影响其溶解性和再活动.通常,这种性质的化合物表现出有趣的生物活动,使它们对医药化学和药物开发感兴趣.(3aR)的命名表明,原子的立体化学安排可以显著地影响化合物与生物目标的相互作用.此外,该结构中的原子可以参与各种协调和联动相互作用,有可能导致独特的催化或治疗应用.

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上下游产品

(R)-α,α-diphenylprolinol phenylboronic acid

合成工艺路线路线简述

    📜(R)-(+)-Alpha,Alpha-二苯基脯氨醇,苯硼酸 以 甲苯 用作溶剂,化学反应 12.0H,反应生成(R)-2-苯基-Cbs-恶唑硼烷
    参考文献:模块化,可扩展的a组链霉菌素抗生素的合成
    标题:模块化,可扩展的a组链霉菌素抗生素的合成
    摘要:链霉菌素抗生素在临床上用于治疗耐多药细菌感染,但其理化性质较差和活性谱较窄,限制了其实用性.化学修饰链霉菌素的新方法将使结构优化能够克服这些局限性,并对抗日益增长的对该类药物的抵抗力.在这里,我们报告了a组链霉菌素抗生素的模块化,可扩展合成方法,该过程可通过简单的化学构建单元以6-8个线性步骤进行.我们已经将路线应用到了该类别的四种天然产物的合成中,其中包括两种以前从未通过完全合成路线获得的天然产物.我们预计这项工作将导致发现克服该类别先前局限性的新型链霉素抗生素.
    Doi:10.1021/jacs.7B08577

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    专利信息


    专利号:US-2010010212-A1
    优先权日:2005-09-08
    标题 :Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe
    发明人:KANSAL VINOD KUMAR; AHMAD SUHAIL; TYAGI BHUPENDRA; GUPTA NITIN
    权利人:KANSAL VINOD KUMAR; AHMAD SUHAIL; TYAGI BHUPENDRA; GUPTA NITIN
    摘要:The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a) having an enantiomeric purity of at least about 97.5%. The invention also encompasses Compound 2a having a chemical purity of at least about 97%. The invention further encompasses processes for preparing Compound 2a from Compound 1 having the following formula: n n n n n n n n n n The invention also encompasses processes for preparing a compound having the following formula: n n n n n n n n n n from a compound having the following formula: n n n n n n n n n n wherein R is selected from the group consisting of: H or a hydroxyl protecting group. The invention also encompasses processes for preparing Compound 2a, preferably to form Compound 2a-Form 01. Also included are processes for preparing ezetimibe from Compound 2a-Form 01 or Compound 2a prepared according to the invention, compositions containing such ezetimibe, and methods for reducing cholesterol using such compositions

    专利号:US-2007259845-A1
    优先权日:2005-09-08
    标 题 :Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe

    专利号:US-5576442-A
    优先权日:1991-07-22
    标 题:Process and chiral intermediates for thiazole antidiabetics
    发明人:QUALLICH GEORGE J
    权利人:PFIZER
    摘要:Two novel optically pure intermediates, (R)-4-(2-bromo-1-hydroxyethyl)-2- trifluoro(-)methylthiazole and (S)-4-oxiranyl-2-trifluoromethylthiazole, which have utility in the synthesis of a potent class of antidiabetic agents. The invention also embraces an enantioselective reduction process for their preparation.

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    ✅ COA系统入驻 | 共享模式

    合成参考文献

    参考DOI号:10.1021/jacs.7b08577
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