我们已经开发了一种新的催化方法,用于通过PdPt-Fe 3 O 4纳米颗粒(NP)催化剂通过芳基腈与硝基烷烃的还原胺化反应,实现不对称仲胺的一锅级联反应。与单金属Pd–Fe 3 O 4或Pt–Fe 3 O 4相比,双金属催化剂的使用提高了反应性和选择性。NP催化剂。使用这种双金属催化体系,我们成功地在温和条件下合成了各种不对称仲胺。然而,含有给电子取代基的芳基腈相当耐还原胺化,当使用六氟异丙醇(HFIP)作为助溶剂时,不对称仲胺的反应选择性和收率大大提高。使用催化剂体系,可以由2-硝基苯基乙腈一锅克级地合成吲哚。由于Fe 3 O 4载体的磁性,双金属催化剂可以容易地使用外部磁体至少循环四次。
[EN] RAS PROTEIN DEGRADERS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC APPLICATIONS<br/>[FR] AGENTS DE DÉGRADATION DE LA PROTÉINE RAS, COMPOSITIONS PHARMACEUTIQUES DE CEUX-CI ET LEURS APPLICATIONS THÉRAPEUTIQUES
申请人:BIOTHERYX INC
公开号:WO2021051034A1
公开(公告)日:2021-03-18
Provided herein are RAS protein degraders, e.g., a compound of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RAS-mediated disorder, disease, or condition.
[EN] PDE4 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND THERAPEUTIC APPLICATIONS<br/>[FR] INHIBITEURS DE PDE4, COMPOSITIONS PHARMACEUTIQUES ET APPLICATIONS THÉRAPEUTIQUES
申请人:BIOTHERYX INC
公开号:WO2021119571A1
公开(公告)日:2021-06-17
Provided herein are phosphodiesterase 4 (PDE4) inhibitors, e.g., a compound of Formula (I) or (II), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a disease, disorder, or condition associated with PDE4 malfunction.
One-pot, chemoselective synthesis of secondary amines from aryl nitriles using a PdPt–Fe<sub>3</sub>O<sub>4</sub> nanoparticle catalyst
作者:Jin Hee Cho、Sangmoon Byun、Ahra Cho、B. Moon Kim
DOI:10.1039/d0cy00630k
日期:——
unsymmetrical secondary amines under mild conditions. However, aryl nitriles containing an electron-donating substituent were rather resistant to the reductive amination, and when hexafluoroisopropanol (HFIP) was used as a co-solvent, the reaction selectivity and yield for unsymmetrical secondary amines increased dramatically. Using the catalyst system, one-pot, gram-scale synthesis of indole was possible
我们已经开发了一种新的催化方法,用于通过PdPt-Fe 3 O 4纳米颗粒(NP)催化剂通过芳基腈与硝基烷烃的还原胺化反应,实现不对称仲胺的一锅级联反应。与单金属Pd–Fe 3 O 4或Pt–Fe 3 O 4相比,双金属催化剂的使用提高了反应性和选择性。NP催化剂。使用这种双金属催化体系,我们成功地在温和条件下合成了各种不对称仲胺。然而,含有给电子取代基的芳基腈相当耐还原胺化,当使用六氟异丙醇(HFIP)作为助溶剂时,不对称仲胺的反应选择性和收率大大提高。使用催化剂体系,可以由2-硝基苯基乙腈一锅克级地合成吲哚。由于Fe 3 O 4载体的磁性,双金属催化剂可以容易地使用外部磁体至少循环四次。