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    Catalytic asymmetric aminohydroxylation of olefins with sulfonamides
    1.
    发明授权
    Catalytic asymmetric aminohydroxylation of olefins with sulfonamides 失效
    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。

    Two step synthesis of D- and L- &agr;-amino acids and D- and L- &agr;-amino aldehydes
    2.
    发明授权
    Two step synthesis of D- and L- &agr;-amino acids and D- and L- &agr;-amino aldehydes 有权
    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。

    Two step synthesis of D- and L- .alpha.-amino acids and D- and L- .alpha.-amino-aldehydes
    3.
    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

    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。

    Catalytic asymmetric aminohydroxylation of olefins with carbamates
    4.
    发明授权
    Catalytic asymmetric aminohydroxylation of olefins with carbamates 失效
    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。

    Synthesis of aryl serines
    8.
    发明授权
    Synthesis of aryl serines 失效
    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。

    Optically active enantiomers of substituted glyceraldehydes or glycidaldehydes formed as subtituted 1,5- dihydro-3H-2,4-benzodioxepines
    10.
    发明授权
    Optically active enantiomers of substituted glyceraldehydes or glycidaldehydes formed as subtituted 1,5- dihydro-3H-2,4-benzodioxepines 失效
    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。