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    Copper-catalysed ligation of azides and acetylenes
    31.
    发明申请
    Copper-catalysed ligation of azides and acetylenes 有权
    铜催化的叠氮化物和乙炔的连接

    公开(公告)号：US20080214831A1

    公开(公告)日：2008-09-04

    申请号：US12152031

    申请日：2008-05-09

    Applicant: K. Barry Sharpless ,  Valery Fokin ,  Vsevold A. Rostovtsev ,  Luke Green ,  Fahmi Himo

    Inventor： K. Barry Sharpless ,  Valery Fokin ,  Vsevold A. Rostovtsev ,  Luke Green ,  Fahmi Himo

    IPC: C07D249/04

    CPC classification number: C07D249/04 ,  B01J31/1805 ,  B01J2231/327 ,  B01J2531/16 ,  B01J2531/96 ,  C07D249/06 ,  C07D403/06

    Abstract: A copper catalyzed click chemistry ligation process is employed to bind azides and terminal acetylenes to provide 1,4-disubstituted 1,2,3-triazole triazoles. The process comprises contacting an organic azide and a terminal alkyne with a source of reactive Cu(I) ion for a time sufficient to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole. The source of reactive Cu(I) ion can be, for example, a Cu(I) salt or copper metal. The process is preferably carried out in a solvent, such as an aqueous alcohol. Optionally, the process can be performed in a solvent that comprises a ligand for Cu(I) and an amine.

    Abstract translation: 使用铜催化的点击化学连接方法结合叠氮化物和末端炔烃以提供1,4-二取代的1,2,3-三唑三唑。 该方法包括使有机叠氮化物和末端炔与活性Cu（I）离子源接触一段时间，足以通过环加成1,4-二取代的1,2,3-三唑形成。 反应性Cu（I）离子的来源可以是例如Cu（I）盐或铜金属。 该方法优选在溶剂如乙醇中进行。 任选地，该方法可以在包含Cu（I）和胺的配体的溶剂中进行。

    Synthesis of &agr;,&bgr;-substituted amino amides, esters, and acids
    33.
    发明授权
    Synthesis of &agr;,&bgr;-substituted amino amides, esters, and acids 有权
    α，β-取代氨基酰胺，酯和酸的合成

    公开(公告)号：US06573387B1

    公开(公告)日：2003-06-03

    申请号：US09381407

    申请日：2000-01-31

    Applicant: K. Barry Sharpless ,  A. Erik Rubin

    Inventor： K. Barry Sharpless ,  A. Erik Rubin

    IPC: C07D20304

    CPC classification number: C07D203/22 ,  C07C231/12 ,  C07C231/16 ,  C07C303/40 ,  C40B40/04 ,  C40B50/08 ,  C07C311/19

    Abstract: &agr;,&bgr;-Unsaturated amides and esters are converted to &agr;,&bgr;-substituted amino amides, esters, and acids. An &agr;,&bgr;unsaturated amide or ester is first converted to an &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The &agr;,&bgr;-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a &agr;,&bgr;-N-sulfonyl- or the &agr;,&bgr;-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(&agr;,&bgr;-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.

    Abstract translation: α，β-不饱和酰胺和酯转化为α，β-取代的氨基酰胺，酯和酸。 首先使用锇催化的氨基羟基化将α，β-不饱和酰胺或酯转化为α，β-羟基磺酰胺或羟基氨基甲酸酯酰胺或酯。 然后将α，β-羟基磺酰胺或羟基氨基甲酸酯酰胺或酯环化脱水以产生α，β-N-磺酰基或α，β-N-氨基甲酰基氮丙啶酰胺或酯。 然后将氮丙啶中间体环以区域选择性方式用各种亲核试剂进行亲核打开，得到$ g（α，β-取代的氨基酰胺或酯）。优选的亲核试剂包括硫，氧，碳和氮亲核试剂。

    Aminohydroxylation of Olefins
    34.
    发明授权
    Aminohydroxylation of Olefins 失效
    烯烃的氨基羟基化

    公开(公告)号：US06350905B1

    公开(公告)日：2002-02-26

    申请号：US09378516

    申请日：1999-08-20

    Applicant: K. Barry Sharpless ,  Valery Fokin

    Inventor： K. Barry Sharpless ,  Valery Fokin

    IPC: C07C29904

    CPC classification number: C07D295/13 ,  C07C227/06 ,  C07C303/40 ,  C07C2601/14 ,  C07F9/3808 ,  C07C229/22 ,  C07C229/36 ,  C07C229/48 ,  C07C311/19

    Abstract: Osmium-catalyzed aminohydroxylation reactions are accelerated and expanded in scope by the use of olefinic substrates having ionic groups, either anionic or cationic. The use of ionic groups on olefinic substrates also extends the aminohydroxylatable positions of unsaturations to include &agr;,&bgr;, &bgr;,&ggr;, and &ggr;,&dgr; positions, with respect to such ionic groups. A mechanism for the disclosed acceleration and extension is provided.

    Abstract translation: 通过使用具有阴离子或阳离子的离子基团的烯属底物，锇催化的氨基羟化反应在范围上得到加速和扩展。 在烯烃底物上使用离子基团也延伸了不饱和基团的氨基可羟化位置，包括相对于这些离子基团的α，β，β，γ和γ，δ位置。 提供了用于所公开的加速和扩展的机构。

    Two step synthesis of D- and L- .alpha.-amino acids and D- and L- .alpha.-amino-aldehydes
    35.
    发明授权
    Two step synthesis of D- and L- .alpha.-amino acids and D- and L- .alpha.-amino-aldehydes 失效
    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

    Applicant: K. Barry Sharpless ,  Guigen Li

    Inventor： K. Barry Sharpless ,  Guigen Li

    IPC: C07C213/08 ,  C07C227/32 ,  C07C269/04 ,  C07C269/06 ,  C07C303/40 ,  C07C311/21 ,  C07F9/40 ,  C07C229/04

    CPC classification number: C07F9/4056 ,  C07C213/08 ,  C07C227/32 ,  C07C269/04 ,  C07C269/06 ,  C07C303/40 ,  C07F9/4006 ,  C07B2200/07

    Abstract: 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.

    Abstract translation: 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。

    Ruthenium-catalyzed production of cyclic sulfates
    37.
    发明授权
    Ruthenium-catalyzed production of cyclic sulfates 失效
    钌催化的环状硫酸盐生产

    公开(公告)号：US5321143A

    公开(公告)日：1994-06-14

    申请号：US712199

    申请日：1991-06-07

    Applicant: K. Barry Sharpless ,  Yun Gao

    Inventor： K. Barry Sharpless ,  Yun Gao

    IPC: C07C213/02 ,  C07C215/20 ,  C07C227/32 ,  C07C247/12 ,  C07C331/14 ,  C07D203/08 ,  C07D317/28 ,  C07D327/10 ,  C07D411/14 ,  C07D89/08

    CPC classification number: C07D203/08 ,  C07C213/02 ,  C07C215/20 ,  C07C227/32 ,  C07C247/12 ,  C07C331/14 ,  C07D317/28 ,  C07D327/10 ,  C07D411/14 ,  C07C2101/14

    Abstract: A ruthenium catalyzed method to synthesize cyclic sulfate compounds from the corresponding cyclic sulfites, and the cyclic sulfate reaction products obtained by this method. These cyclic sulfates further react with selected nucleophiles to give various substituted products. The method is an efficient means for the synthesis of chiral building blocks from tartaric acid enantiomers in high yields using an overall two-stage, one-pot reaction procedure. The chiral compounds can be transformed by nucleophilic reactions into chiral building blocks useful for the synthesis of natural biologically active products, such as antibiotics and pheromones.

    Abstract translation: 从相应的环状亚硫酸盐合成环状硫酸盐化合物的钌催化方法和通过该方法得到的环状硫酸盐反应产物。 这些环状硫酸盐与选择的亲核试剂进一步反应，得到各种取代的产物。 该方法是使用总体两步一锅反应方法以高产率从酒石酸对映异构体合成手性结构单元的有效手段。 手性化合物可以通过亲核反应转化成用于合成天然生物活性产物（如抗生素和信息素）的手性结构单元。

    Ligand-accelerated catalytic asymmetric dihydroxylation using dihydroquinidine and dihydroquinidine esters as ligands
    38.
    发明授权
    Ligand-accelerated catalytic asymmetric dihydroxylation using dihydroquinidine and dihydroquinidine esters as ligands 失效
    使用二氢奎尼酮和二氢奎尼丁酯作为配体的配体加速催化不对称二羟基化

    公开(公告)号：US4871855A

    公开(公告)日：1989-10-03

    申请号：US159068

    申请日：1988-02-23

    Applicant: Istvan E. Marko ,  K. Barry Sharpless

    Inventor： Istvan E. Marko ,  K. Barry Sharpless

    IPC: C07C29/48

    CPC classification number: C07C29/48 ,  C07B2200/07 ,  C07C2101/14 ,  C07C2101/18

    Abstract: An osmium-catalyzed method of addition to an olefin. In the method of asymmetric dihydroxylation of the present invention, an olefin, a chiral ligand, an organic solvent, water, and aamine oxide and an osmium-containing compound are combined. In the method of asymmetric oxyamination of the present invention, an olefin, a chiral ligand, an organic solvent, water, an amine derivative and an osmium-containing compound are combined. In the method of asymmetric diamination of the present invention, an olefin, a chiral ligand, an organic solvent, a metallo-chloramine derivative or an amine derivative and an osmium-containing compound are combined. In one embodiment, an olefin, a chiral ligand which is a dihydroquinidine derivative or a dihydroquinine derivative, acetone, water, N-methyl morpholine N-oxide and osmium tetroxide are combined to effect asymmetric dihydroxylation of the olefin.

    Abstract translation: 一种加入烯烃的锇催化方法。 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，水和氧化胺和含锇化合物。 在本发明的不对称氧化法的方法中，合并烯烃，手性配体，有机溶剂，水，胺衍生物和含锇化合物。 在本发明的不对称二氨基化方法中，合并烯烃，手性配体，有机溶剂，金属氯胺衍生物或胺衍生物和含锇化合物。 在一个实施方案中，将烯烃，二氢奎尼丁衍生物或二氢喹啉衍生物的手性配体，丙酮，水，N-甲基吗啉N-氧化物和四氧化锇组合以实现烯烃的不对称二羟基化。

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