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    Two step synthesis of D- and L- .alpha.-amino acids and D- and L- .alpha.-amino-aldehydes
    1.
    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。

    Two step synthesis of D- and L- &agr;-amino acids and D- and L- &agr;-amino aldehydes
    3.
    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。

    Catalytic asymmetric aminohydroxylation of olefins with sulfonamides
    4.
    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。

    Catalytic asymmetric aminohydroxylation of olefins with carbamates
    6.
    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。

    CHIRAL 2-ARYLPROPYL-2-SULFINAMIDE AND CHIRAL N-2-ARYLPROPYL-2-SULFINYLIMINES AND SYNTHESIS THEREOF
    7.
    发明申请
    CHIRAL 2-ARYLPROPYL-2-SULFINAMIDE AND CHIRAL N-2-ARYLPROPYL-2-SULFINYLIMINES AND SYNTHESIS THEREOF 审中-公开

    公开(公告)号：US20140275582A1

    公开(公告)日：2014-09-18

    申请号：US14207390

    申请日：2014-03-12

    申请人： Guigen LI

    发明人： Guigen LI

    IPC分类号： C07D307/52 ,  C07C313/02 ,  C07C313/06

    CPC分类号： C07D307/52 ,  C07B2200/07 ,  C07C313/06 ,  C07C2601/14

    摘要： Provided herein are novel chiral sulfinamide and imine compounds. Also provided herein are methods of synthesizing novel chiral sulfinamide and imine compounds comprising simplified purification methods when compared to prior methods. The novel chiral sulfinamide and imine compounds are useful, for example, in the synthesis of complex natural products and pharmaceutical important compounds.

    摘要翻译： 本文提供了新型手性亚磺酰胺和亚胺化合物。 本文还提供了与现有技术相比较，合成新型手性亚磺酰胺和亚胺化合物的方法，其包括简化的纯化方法。 新型手性亚磺酰胺和亚胺化合物可用于例如复合天然产物和药物重要化合物的合成。

    STRECKER REAGENTS, THEIR DERIVATIVES, METHODS FOR FORMING THE SAME AND IMPROVED STRECKER REACTION
    8.
    发明申请
    STRECKER REAGENTS, THEIR DERIVATIVES, METHODS FOR FORMING THE SAME AND IMPROVED STRECKER REACTION 审中-公开
    STRECKER试剂，它们的衍生物，形成它们的方法和改进的STRECKER反应

    公开(公告)号：US20130137889A1

    公开(公告)日：2013-05-30

    申请号：US13702060

    申请日：2010-03-26

    申请人： Guigen Li ,  Xiangzhen Sun ,  Huabing Chen

    发明人： Guigen Li ,  Xiangzhen Sun ,  Huabing Chen

    IPC分类号： C07F9/6584 ,  C07F5/06 ,  C07F9/6574

    CPC分类号： C07F9/65848 ,  C07F5/066 ,  C07F5/068 ,  C07F5/069 ,  C07F9/657154 ,  C07F9/65742

    摘要： Strecker reagents, their derivatives and methods for forming the same and improved Strecker reaction are provided. The electrophiles for asymmetric Strecker reaction include achiral N-phosphorazides, N-phosphoramides, N-phosphonyl imines and their derivatives. The nucleophiles for asymmetric Strecker reaction include chiral BINOL-derived azides, amides, imines and their derivatives, the chiral and achiral diol-based cyanides and their derivatives, the chiral and achiral diamine-based cyanides and their derivatives, the chiral and achiral amino alcohol-based cyanides and their derivatives, the Strecker nucleophiles that are derived from chiral and achiral hydroxyl carboxylic acids and amino acids. Methods of forming the electrophile for asymmetric Strecker reaction comprise the reactions with steps of: a) synthesizing phosphoryl chloride from achiral diamine; b) synthesizing phosphorous azide; c) synthesizing phosphoramide; d) synthesizing the corresponding achiral N-phosphonyl imines. The asymmetric catalytic Strecker reaction of new achiral N-phosphonyl imines has been developed to give excellent enantioselectivity (up to >99% ee) and yields (up to >97%).

    摘要翻译： 提供了Strecker试剂，其衍生物和形成相同和改进的Strecker反应的方法。 用于不对称Strecker反应的亲电子试剂包括非手性N-磷酰肼，N-磷酰胺，N-膦酰基亚胺及其衍生物。 用于不对称Strecker反应的亲核试剂包括手性BINOL衍生的叠氮化物，酰胺，亚胺及其衍生物，手性和非手性二醇基氰化物及其衍生物，手性和非手性二胺基氰化物及其衍生物，手性和非手性氨基醇 的氰化物及其衍生物，衍生自手性和非手性羟基羧酸和氨基酸的Strecker亲核体。 形成不对称Strecker反应的亲电子试剂的方法包括以下步骤的反应：a）从非手性二胺合成磷酰氯; b）合成磷叠氮化物; c）合成磷酰胺; d）合成相应的非手性N-膦酰基亚胺。 已经开发了新的非手性N-膦酰亚胺的不对称催化Strecker反应，以提供优异的对映选择性（高达> 99％ee）和产率（高达> 97％）。