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1. 发明授权

US5859281A Catalytic asymmetric aminohydroxylation of olefins with sulfonamides 失效
标题翻译：用磺酰胺催化烯烃的不对称氨基羟基化
公开(公告)号：US5859281A
公开(公告)日：1999-01-12
申请号：US651819
申请日：1996-05-21
申请人： K. Barry Sharpless , Guigen Li , Han-Ting Chang
发明人： K. Barry Sharpless , Guigen Li , Han-Ting Chang
IPC分类号： C07C213/00 , C07C303/40 , C07C311/04 , C07C311/06 , C07C311/07 , C07C311/17 , C07C311/19 , C07C311/20 , C07C311/29 , C07C311/42 , C07C303/00
CPC分类号： C07C303/40 , C07C213/00 , C07B2200/07 , C07C2101/14
摘要： .beta.-Hydroxyamines and .beta.-hydroxysulfonamides are synthesized from olefin substrates by means on a catalyzed asymmetric addition reaction. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. Sulfonamides are employed as an oxidant nitrogen source for the production of .beta.-hydroxysulfonamides. Excellent yields and enantiomeric efficiencies are achieved with co-solvents containing a 50/50 (v/v) mixtures of water and organic solvent. .beta.-Hydroxyamines are obtained by deprotecting the corresponding .beta.-hydroxysulfonamides.
摘要翻译：通过催化不对称加成反应由烯烃底物合成β-羟基胺和β-羟基磺酰胺。加成反应由锇催化并被手性配体共催化。除了与锇共助催化剂之外，手性配体还用于区域选择地和对映选择性地引导加成反应。二价配体优于一价配体，因为它们具有增强的区域和对映选择性。磺酰胺被用作生产β-羟基磺酰胺的氧化剂氮源。使用含有水和有机溶剂的50/50（v / v）混合物的共溶剂可获得优异的收率和对映体效率。通过脱保护相应的β-羟基磺酰胺得到β-羟基胺。

2. 发明授权

US06509506B1 Two step synthesis of D- and L- &agr;-amino acids and D- and L- &agr;-amino aldehydes 有权
标题翻译： D-和L-α-氨基酸和D-和L-α-氨基醛的两步合成
公开(公告)号：US06509506B1
公开(公告)日：2003-01-21
申请号：US09171538
申请日：1999-04-05
申请人： K. Barry Sharpless , Guigen Li
发明人： K. Barry Sharpless , Guigen Li
IPC分类号： C07C20500
CPC分类号： C07C221/00 , C07C223/02
摘要： D- and L- &agr;-amino acids and D- and L-&agr;-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively, divalent ligands are preferred over monovalent ligands because of their enhanced regio-and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant &bgr;-hydoxycarbamate is deprotected to yield the corresponding &bgr;-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant &bgr;-hydroxysulfonamide is deprotected to yield the corresponding &bgr;-hydroxyamine. The resultant &bgr;-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L- &agr;-amino acid or D- and L-&agr;-amino aldehyde.
摘要翻译： D-和L-α-氨基酸和D-和L--α-氨基醛在两个步骤中由烯烃底物合成。第一步是对烯烃底物的催化不对称氨基羟基化加成反应。加成反应由锇催化并被手性配体共催化。除了与锇共助催化剂之外，手性配体还用于区域选择性和对映选择性地引导加成反应，因为二价配体优于单价配体，因为它们具有增强的区域和对映选择性。作为加成反应的氧化剂氮源，可以使用氨基甲酸酯或磺酰胺。如果使用氨基甲酸酯作为氧化剂氮源，则将所得的β-羟基氨基甲酸酯脱保护，得到相应的β-羟基胺。如果使用磺酰胺作为氧化剂氮源，则将所得的β-羟基磺酰胺脱保护，得到相应的β-羟基胺。然后在第二合成步骤中选择性氧化得到的β-羟基胺，以产生所需的D-和L-α-氨基酸或D-和L--α-氨基醛。

3. 发明授权

US5994583A Two step synthesis of D- and L- .alpha.-amino acids and D- and L- .alpha.-amino-aldehydes 失效
标题翻译： D-和L-α-氨基酸和D-和L-α-氨基醛的两步合成
公开(公告)号：US5994583A
公开(公告)日：1999-11-30
申请号：US651228
申请日：1996-05-22
申请人： K. Barry Sharpless , Guigen Li
发明人： K. Barry Sharpless , Guigen Li
IPC分类号： C07C213/08 , C07C227/32 , C07C269/04 , C07C269/06 , C07C303/40 , C07C311/21 , C07F9/40 , C07C229/04
CPC分类号： C07F9/4056 , C07C213/08 , C07C227/32 , C07C269/04 , C07C269/06 , C07C303/40 , C07F9/4006 , C07B2200/07
摘要： D- and L-.alpha.-amino acids and D- and L-.alpha.-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant .beta.-hydroxycarbamate is deprotected to yield the corresponding .beta.-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant .beta.-hydroxysulfonamide is deprotected to yield the corresponding .beta.-hydroxyamine. The resultant .beta.-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L-.alpha.-amino acid or D- and L-.alpha.-amino aldehyde.
摘要翻译： D-和L-α-氨基酸和D-和L-α-氨基醛在两个步骤中由烯烃底物合成。第一步是对烯烃底物的催化不对称氨基羟基化加成反应。加成反应由锇催化并被手性配体共催化。除了与锇共助催化剂之外，手性配体还用于区域选择地和对映选择性地引导加成反应。二价配体优于一价配体，因为它们具有增强的区域和对映选择性。作为加成反应的氧化剂氮源，可以使用氨基甲酸酯或磺酰胺。如果使用氨基甲酸酯作为氧化剂氮源，则将得到的β-羟基氨基甲酸酯脱保护，得到相应的β-羟基胺。如果使用磺酰胺作为氧化剂氮源，则所得的β-羟基磺酰胺被去保护，得到相应的β-羟基胺。然后在第二合成步骤中选择性地氧化所得的β-羟基胺以产生所需的D-和L-α-氨基酸或D-和L-α-氨基醛。

4. 发明授权

US5767304A Catalytic asymmetric aminohydroxylation of olefins with carbamates 失效
标题翻译：烯烃与氨基甲酸酯的催化不对称氨基羟基化
公开(公告)号：US5767304A
公开(公告)日：1998-06-16
申请号：US651104
申请日：1996-05-21
申请人： K. Barry Sharpless , Guigen Li
发明人： K. Barry Sharpless , Guigen Li
IPC分类号： C07C227/20 , C07C229/34 , C07C269/00 , C07F9/40 , C07C271/16
CPC分类号： C07F9/4056 , C07C227/20 , C07C269/00 , C07F9/4006 , C07C2102/10
摘要： .beta.-Hydroxyamines and .beta.-hydroxycarbamates are synthesized from olefin substrates by means on a catalyzed asymmetric addition reaction. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. Carbamates are employed as an oxidant nitrogen source for the production of .beta.-hydroxysulfonamides. Excellent yields and enantiomeric efficiencies are achieved with co-solvents containing a 50/50 (v/v) mixtures of water and organic solvent. The performance of the reaction is further enhanced by omitting the addition silver or mercurial salts conventionally employed in asymmetric aminohydroxylation additions to olefins performed in neat or substantially neat solvents. .beta.-Hydroxyamines are then obtained by deprotecting the corresponding .beta.-hydroxycarbamate.
摘要翻译：通过催化不对称加成反应，通过烯烃底物合成β-羟基胺和β-羟基氨基甲酸酯。加成反应由锇催化并被手性配体共催化。除了与锇共助催化剂之外，手性配体还用于区域选择地和对映选择性地引导加成反应。二价配体优于一价配体，因为它们具有增强的区域和对映选择性。使用氨基甲酸酯作为生产β-羟基磺酰胺的氧化剂氮源。使用含有水和有机溶剂的50/50（v / v）混合物的共溶剂可获得优异的收率和对映体效率。通过省略常规用于在纯净或基本上纯的溶剂中进行的烯烃的不对称氨基羟基化添加中的加成银或汞盐进一步提高反应的性能。然后通过脱保护相应的β-羟基氨基甲酸酯得到β-羟基胺。

5. 发明授权

US08927736B2 Copper catalyzed cycloaddition of organic azides and 1-haloalkynes 有权
标题翻译：有机叠氮化物和1-卤代炔的铜催化环加成
公开(公告)号：US08927736B2
公开(公告)日：2015-01-06
申请号：US13389987
申请日：2010-08-11
申请人： Jason E. Hein , Jonathan C. Tripp , Larissa Krasnova , K. Barry Sharpless , Valery V. Fokin
发明人： Jason E. Hein , Jonathan C. Tripp , Larissa Krasnova , K. Barry Sharpless , Valery V. Fokin
IPC分类号： C07D403/02 , B01J31/18 , B01J23/72 , C07D249/06 , C07D311/12 , C07D405/04
CPC分类号： B01J31/1805 , B01J23/72 , B01J31/181 , B01J2531/16 , C07D249/06 , C07D311/12 , C07D405/04
摘要： This invention provides a method for preparing a 1,2,3-triazole compound comprising contacting an organic azide with a 2-substituted-1-haloalkyne, in the presence of a copper catalyst and a copper-coordinating ligand (preferably a tertiary amine) in a liquid reaction medium, thereby forming a 1,4,5-substituted-1,2,3-triazole compound including a halo substituent at the 5-position of the triazole, the organic portion of the organic azide at the 1-position of the triazole, and the substituent of the 1-iodoalkyne at the 4-position of the triazole. A method for preparing 1-iodoalkynes is also provided.
摘要翻译：本发明提供了一种制备1,2,3-三唑化合物的方法，包括在铜催化剂和铜配位配体（优选叔胺）的存在下使有机叠氮化物与2-取代-1-卤代炔相接触，在液体反应介质中，由此形成在三唑的5位上含有卤素取代基的1,4,5-取代-1,2,3-三唑化合物，有机叠氮化物在1位的有机部分的三唑，以及在三唑的4-位上的1-碘代炔的取代基。还提供了制备1-碘代炔的方法。

6. 发明申请

US20100286405A1 Ruthenium-Catalyzed Cycloaddition of Alkynes and Organic Azides 有权
标题翻译：钌催化的炔烃和有机叠氮化物的加成反应
公开(公告)号：US20100286405A1
公开(公告)日：2010-11-11
申请号：US11992696
申请日：2006-09-29
申请人： Valery Fokin , Guocheng Jia , K. Barry Sharpless
发明人： Valery Fokin , Guocheng Jia , K. Barry Sharpless
IPC分类号： C07D249/06
CPC分类号： C07D249/04 , C07F17/02
摘要： A convenient process for the regioselective synthesis of 1,5-disubstituted 1,2,3-triazoles and 1,4,5-trisubstituted 1,2,3-triazoles from organic azides and alkynes employs catalytic ruthenium.
摘要翻译：从有机叠氮化物和炔烃区域选择性合成1,5-二取代的1,2,3-三唑和1,4,5-三取代的1,2,3-三唑的方便的方法使用催化钌。

7. 发明申请

US20090069561A1 CLICK CHEMISTRY ROUTE TO TRIAZOLE DENDRIMERS 审中-公开
标题翻译：点击化学品路线到三唑树脂
公开(公告)号：US20090069561A1
公开(公告)日：2009-03-12
申请号：US11631081
申请日：2005-06-30
申请人： Valery Fokin , K. Barry Sharpless , Peng Wu , Alina Feldman
发明人： Valery Fokin , K. Barry Sharpless , Peng Wu , Alina Feldman
IPC分类号： C07D249/04 , C07C247/04 , C07D403/12 , C07C43/205 , C07C317/10 , C07C205/03 , C07D251/32 , C07C247/06
CPC分类号： C08G73/00 , C07C233/05 , C07C311/16 , C07D403/12 , C07D403/14 , C08G83/003
摘要： The high efficiency and fidelity of click chemistry permits a large number of diverse dendrimers encompassing a wide variety of functionalities at the chain ends, repeat units, and/or core to be prepared. Almost quantitative yields were obtained during the synthesis. In some cases, filtration or solvent extraction was the only method required for purification. These features represent a significant advancement in dendrimer chemistry and demonstrate an evolving synergy between organic chemistry and functional materials.
摘要翻译：点击化学的高效率和高保真性允许大量不同的树枝状聚合物，其包括在链末端，重复单元和/或待制备的核心上的各种功能。在合成过程中获得了几乎定量的产率。在某些情况下，过滤或溶剂萃取是纯化所需的唯一方法。这些特征代表着树枝状大分子化学的显着进步，并展示了有机化学与功能材料之间不断发展的协同作用。

8. 发明授权

US6057473A Synthesis of aryl serines 失效
标题翻译：芳基丝氨酸的合成
公开(公告)号：US6057473A
公开(公告)日：2000-05-02
申请号：US50222
申请日：1998-03-26
申请人： K. Barry Sharpless , Beata Tao , Gunther Schlingloff
发明人： K. Barry Sharpless , Beata Tao , Gunther Schlingloff
IPC分类号： C07C227/20 , C07C229/34 , C07C269/00 , C07F9/40 , C07C229/28
CPC分类号： C07F9/4056 , C07C227/20 , C07C269/00 , C07F9/4006 , C07C2102/10
摘要： Anthraquinone chiral ligands (AQN) are used in asymmetric aminohydroxylation addition reactions of cinnamate based olefins for synthesizing aryl serines. The anthraquinones impart a reverse regioselectivity as compared to the commonly employed phalazine chiral ligands (PHAL). Carbamates are employed as the oxidant nitrogen source. The yields and enantiomeric efficiencies are Excellent. .beta.-Hydroxyamines are obtained by deprotecting the corresponding .beta.-hydroxycarbamate.
摘要翻译：蒽醌手性配体（AQN）用于肉桂酸酯类烯烃合成芳基丝氨酸的不对称氨基羟基化反应。与常用的哒嗪手性配体（PHAL）相比，蒽醌赋予反向区域选择性。使用氨基甲酸酯作为氧化剂氮源。产率和对映体效率优异。通过脱保护相应的β-羟基氨基甲酸酯获得β-羟基胺。

9. 发明授权

US5260461A Ligands for ADH: cinchona alkaloids and moderately sized organic substituents linked through a planar aromatic spacer group 失效
标题翻译： ADH的配体：通过平面芳族间隔基团连接的cinchona生物碱和中等大小的有机取代基
公开(公告)号：US5260461A
公开(公告)日：1993-11-09
申请号：US775683
申请日：1991-10-10
申请人： Jens Hartung , K. Barry Sharpless
发明人： Jens Hartung , K. Barry Sharpless
IPC分类号： C07B53/00 , C07B61/00 , C07C29/04 , C07C29/48 , C07C31/00 , C07C33/26 , C07C67/31 , C07C69/675 , C07C69/732 , C07D453/02 , C07D453/04 , C07C215/34 , C07C31/20 , C07C33/02 , C07C69/734 , C07C69/735 , C07D67/313
CPC分类号： C07C67/31 , C07C29/48 , C07D453/02 , C07D453/04 , C07B2200/07 , C07C2101/14 , C07C2101/18
摘要： Osmium-catalyzed methods of addition to an olefin are discussed. In the method of asymmetric dihydroxylation of the present invention, an olefin, a chiral ligand, an organic solvent, an aqueous solution, a base, a ferricyanide salt and an osmium-containing compound are combined. The chiral ligand is an alkaloid or alkaloid derivative linked to an organic substituent of at least 300 daltons molecular weight through a planar aromatic spacer group. The organic substituent can be another alkaloid or alkaloid derivative. With the described chiral ligands, asymmetric dihydroxylation of olefins with high yields and enantiomeric excesses are achieved.
摘要翻译：讨论了添加到烯烃中的锇催化方法。在本发明的不对称二羟基化方法中，合并烯烃，手性配体，有机溶剂，水溶液，碱，铁氰化物盐和含锇化合物。手性配体是通过平面芳族间隔基团与至少300道尔顿分子量的有机取代基连接的生物碱或生物碱衍生物。有机取代基可以是另一种生物碱或生物碱衍生物。使用所述手性配体，可以实现高产率和对映异构体过量的烯烃的不对称二羟基化。

10. 发明授权

US5162554A Optically active enantiomers of substituted glyceraldehydes or glycidaldehydes formed as subtituted 1,5- dihydro-3H-2,4-benzodioxepines 失效
标题翻译：由取代的1,5-二氢-3H-2,4-苯并二氧杂环庚三烯形成的取代的甘油醛或缩水甘醛的光学活性对映异构体
公开(公告)号：US5162554A
公开(公告)日：1992-11-10
申请号：US716902
申请日：1991-06-18
申请人： K. Barry Sharpless , Ryu Oi
发明人： K. Barry Sharpless , Ryu Oi
IPC分类号： C07D321/10 , C07D407/04 , C07D411/04
CPC分类号： C07D407/04 , C07D321/10 , C07D411/04
摘要： Stable, optically active enantiomers of substituted glyceraldehydes or glycidaldehydes are synthesized by using osmium-catalyzed asymmetric dihydroxylation of an olefin which is a substituted 1,5-dihydro-3H-2,4-benzodioxepine. For example, the protected glyceraldehyde, 3-(1,2-dihydroxyethyl)-1,5-dihydro-3H-2,4-benzodioxepine and the protected glycidaldehyde, 3-(1,2-epoxyethyl)-1,5-dihydro-3H-2,4-benzodioxepine have been synthesized and the optical enantiomer has been recovered. In the synthetic and isolation methods, enantiomers with high enantiomeric excess are recovered from the mother liquor following a recrystallization step.
摘要翻译：通过使用锇催化的不对称二羟基化的烯烃（其是取代的1,5-二氢-3H-2,4-benzodioxepine）来合成取代的甘油醛或缩水甘醛的稳定的旋光活性对映异构体。例如，保护的甘油醛，3-（1,2-二羟乙基）-1,5-二氢-3H-2,4-苯并二氧杂环庚烯和被保护的缩二醛，3-（1,2-环氧乙基）-1,5-二氢 -3H-2,4-苯并二氧杂环庚烯，并回收了光学对映体。在合成和分离方法中，在重结晶步骤后从母液中回收具有高对映体过量的对映异构体。

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