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    • 40. 发明申请
    • SULFONAMIDE-BASED ORGANOCATALYSTS AND METHOD FOR THEIR USE
    • 基于磺酰胺的有机物及其使用方法
    • US20100184986A1
    • 2010-07-22
    • US12726212
    • 2010-03-17
    • Rich Garrett CarterHua Yang
    • Rich Garrett CarterHua Yang
    • C07D221/22C07C317/32C07D207/08C07D215/36C07C317/24C07C317/04C07C49/172C07C49/395C07C49/403C07C311/35C07D213/62C07D319/06
    • B01J31/0237B01J31/0222B01J31/0247B01J31/0271B01J2231/32B01J2231/341B01J2231/346B01J2231/4283B01J2231/46
    • Organocatalysts, particularly proline sulfonamide organocatalysts, having a first general formula as follows are disclosed. Embodiments of a method for using these organocatalysts also are disclosed. The method comprises providing a disclosed organocatalyst, and performing a reaction, often an enantioselective or diastereoselective reaction, using the organocatalyst. Solely by way of example, disclosed catalysts can be used to perform aldol reactions, conjugate additions, Michael additions, Robinson annulations, Mannich reactions, α-aminooxylations, α-hydroxyaminations, α-aminations and alkylation reactions. Certain of such reactions are intramolecular cyclizations used to form cyclic compounds, such as 5- or 6-membered rings, having one or more chiral centers. Disclosed organocatalysts generally are much more soluble in typical solvents used for organic synthesis than are known compounds. Moreover, the reaction yield is generally quite good with disclosed compounds, as is their enantioselective and diastereoselective effectiveness.
    • 公开了具有第一通式的有机催化剂,特别是脯氨酸磺酰胺有机催化剂。 还公开了使用这些有机催化剂的方法的实施方案。 该方法包括提供所公开的有机催化剂,并使用有机催化剂进行反应,通常是对映选择性或非对映选择性反应。 公开的催化剂可以用于进行醛醇反应,共轭加成,迈克尔加成,罗宾逊环,曼尼希反应,α-氨基氧化,α-羟基胺化,α-胺化和烷基化反应。 某些此类反应是用于形成具有一个或多个手性中心的环状化合物(例如5-或6-元环)的分子内环化。 公知的有机催化剂通常比已知化合物更易溶于用于有机合成的典型溶剂。 此外,所公开的化合物的反应产率通常是相当好的,以及它们的对映选择性和非对映选择性的有效性。