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公开(公告)号：US08399684B2
公开(公告)日：2013-03-19
申请号：US12726212
申请日：2010-03-17
申请人： Rich Garrett Carter , Hua Yang
发明人： Rich Garrett Carter , Hua Yang
IPC分类号： C07D207/09 , C07D209/14 , C07C311/50
CPC分类号： B01J31/0237 , B01J31/0222 , B01J31/0247 , B01J31/0271 , B01J2231/32 , B01J2231/341 , B01J2231/346 , B01J2231/4283 , B01J2231/46
摘要： 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.
摘要翻译： 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环状化合物的分子内环化，例如具有一个或多个手性中心的5-或6-元环。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。
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公开(公告)号：US20100184986A1
公开(公告)日：2010-07-22
申请号：US12726212
申请日：2010-03-17
申请人： Rich Garrett Carter , Hua Yang
发明人： Rich Garrett Carter , Hua Yang
IPC分类号： C07D221/22 , C07C317/32 , C07D207/08 , C07D215/36 , C07C317/24 , C07C317/04 , C07C49/172 , C07C49/395 , C07C49/403 , C07C311/35 , C07D213/62 , C07D319/06
CPC分类号： B01J31/0237 , B01J31/0222 , B01J31/0247 , B01J31/0271 , B01J2231/32 , B01J2231/341 , B01J2231/346 , B01J2231/4283 , B01J2231/46
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US06958401B2
公开(公告)日：2005-10-25
申请号：US10352340
申请日：2003-01-27
IPC分类号： C07D277/20 , C07D417/06 , C07D277/22 , A61P35/00
CPC分类号： C07D277/20 , C07D417/06
摘要： A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B.
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公开(公告)号：US06596875B2
公开(公告)日：2003-07-22
申请号：US09846154
申请日：2001-04-30
IPC分类号： C07D49304
CPC分类号： C07D277/20 , C07D417/06
摘要： A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B.
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公开(公告)号：US07145018B2
公开(公告)日：2006-12-05
申请号：US11123530
申请日：2005-05-05
IPC分类号： C07D277/22
CPC分类号： C07D277/20 , C07D417/06
摘要： A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. One embodiment of the method was used to synthesize epothilone B by a convergent approach that entailed Wittig coupling of an ylide derived from phosphonium bromide with an aldehyde. The former was prepared from propargyl alcohol by a nine-step pathway which installed both trisubstituted double bonds with clean Z configuration. Macrolactonization of a resulting seco acid provided the following intermediate diene epothilone analog. Selective saturation of the 9,10-olefin and subsequent epoxidation provided epothilone B
摘要翻译： 描述了制备埃坡霉素和埃坡霉素类似物的方法，以及通过该方法制备的新型化合物。 该方法的一个实施方案用于通过收敛方法合成埃坡霉素B，其使得衍生自溴化鏻的内鎓盐与醛的Wittig偶联。 前者由炔丙醇通过九步路径制备，其安装了具有清洁Z构型的三取代双键。 得到的仲酸的大环内酯化得到以下的中间体二烯雌二醇类似物。 选择性饱和的9,10-烯烃和随后的环氧化提供埃坡霉素B
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公开(公告)号：US06906188B2
公开(公告)日：2005-06-14
申请号：US10354694
申请日：2003-01-29
IPC分类号： C07D277/20 , C07D417/06 , C07D225/02 , C07D321/00 , C07D327/02 , C07D411/06
CPC分类号： C07D277/20 , C07D417/06
摘要： A method for making epothilones and epothilone analogs is described, as are novel compounds made by the method. Exemplary novel compounds include those according to the formula: With respect the formula, G is selected from the group consisting of R2 substituents independently are selected from the group consisting of H and lower alkyl groups; Z is selected from the group consisting of the halogens and —CN; M is selected from the group consisting of O and NR3; R3 is selected from the group consisting of H, lower alkyl, R4CO, R4OCO, and R4SO2; R4 is selected from the group consisting of H, lower alkyl, and aryl; T is selected from the group consisting of CH2, CO, HCOH and protected derivatives thereof; W is H or OR; and X and Y independently are selected from the group consisting of O, NH, S, CO, and C. Embodiments of the method provide convenient access to analogs of the epothilones, such as those having alternate stereochemistry and those containing an ester, amide, thioester, or alkyne moieties in the macrocycle.
摘要翻译： 描述了制备埃坡霉素和埃坡霉素类似物的方法，以及通过该方法制备的新型化合物。 示例性的新化合物包括根据下式的化合物：关于式，G选自R 2 2取代基，独立地选自H和低级烷基; Z选自卤素和-CN; M选自O和NR 3; R 3选自H，低级烷基，R 4 CO，R 4 OCO和R 4， / SO 2 SO 2; R 4选自H，低级烷基和芳基; T选自CH 2 CO，HCOH及其被保护的衍生物; W为H或OR; X和Y独立地选自O，NH，S，CO和C.这些方法的实施方案提供方便地获得埃坡霉素的类似物，例如具有交替立体化学的那些类似物，以及含有酯，酰胺， 硫代酯或炔烃部分。
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