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公开(公告)号：US5466798A
公开(公告)日：1995-11-14
申请号：US138612
申请日：1993-10-15
IPC分类号： C07C213/00 , C07C215/08 , C07D295/084 , C07D295/088 , C07D295/096 , C07D223/02 , C07D207/00 , C07F5/02
CPC分类号： C07D295/096 , C07C213/00 , C07C215/08 , C07D295/084 , C07D295/088 , C07D295/092
摘要： The present invention relates to novel, powerful reducing agents, lithium aminoborohydrides which are prepared by addition of BH.sub.3 .cndot.THF to the corresponding dialkylamine at 25.degree. C. to give the intermediate amineborane complex. Subsequent deprotonation by strong base, e.g. n-BuLi, yields the aminoborohydride quantitatively. Lithium aminoborohydrides are powerful reducing agents, comparable in strength to lithium aluminum hydride. The activity is determined by the dialkylamine. Lithium pyrrolidinoborohydride has unique activity and selectivity in its reducing properties. Esters, lactones and anhydrides are reduced cleanly at 25.degree. C. to give the corresponding alcohols, while carboxylic acids are not reduced. Test reductions show that lithium pyrrolidinoborohydride is also capable of reducing a wide range of functional groups including amides, epoxides, oximes, nitriles and halides.
摘要翻译： 本发明涉及通过在25℃下向相应的二烷基胺中加入BH3.THF而制得的新的强大的还原剂氨基硼酸锂，得到中间体胺硼烷络合物。 随后通过强碱去质子化，例如 n-BuLi，定量产生氨基硼氢化钠。 氨基硼氢化锂是强大的还原剂，其强度与氢化铝锂相当。 活性由二烷基胺决定。 吡咯烷基硼氢化锂在还原性能方面具有独特的活性和选择性。 酯，内酯和酸酐在25℃下干净地还原，得到相应的醇，而羧酸不被还原。 测试减少表明，吡咯烷基硼氢化锂还能够减少宽范围的官能团，包括酰胺，环氧化物，肟，腈和卤化物。
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2.发明授权Asymmetric synthesis of .beta.-amino alcohols from chiral or achiral enamines 失效手性或非手性烯胺对β-氨基醇的不对称合成
公开(公告)号：US5367073A
公开(公告)日：1994-11-22
申请号：US138613
申请日：1993-10-15
IPC分类号： C07C213/00 , C07C215/08 , C07D295/084 , C07D295/088 , C07D295/096 , C07D207/12 , C07D295/08 , C07C213/38
CPC分类号： C07D295/096 , C07C213/00 , C07C215/08 , C07D295/084 , C07D295/088 , C07D295/092
摘要： The present invention relates to a process for the synthesis of chiral enantiomerically pure .beta.-amino alcohols which are extraordinarily important as therapeutic agents for the treatment of a variety of human disorders and as chiral auxiliaries in organic synthesis. The hydroboration of enamines is a versatile and convenient method for the synthesis of both racemic and enantiomerically pure .beta.-amino alcohols in high yields. This methodology enables the synthesis of virtually any .beta.-amino alcohol. Hydroboration of these enamines with chiral organic borohydrides, e.g. either mono- or diisopinocampheylborane, followed by oxidation with aqueous or solid NaOH/30% H.sub.2 O.sub.2 or Me.sub.3 NO, gives the corresponding chiral .beta.-amino alcohol. Enantiomeric excesses ranged from 60% for reactions run at 25.degree. C. to greater than 99% for reactions run at -25.degree. C.
摘要翻译： 本发明涉及合成手性对映异构纯的β-氨基醇的方法，其作为用于治疗多种人类疾病的治疗剂非常重要，并且作为有机合成中的手性助剂。 烯胺的硼氢化合物是以高产率合成外消旋和对映异构纯的β-氨基醇的通用和方便的方法。 该方法使得几乎可以合成任何β-氨基醇。 这些烯胺与手性有机硼氢化物的水解，例如 单或二蒎烷基硼烷，然后用水或固体NaOH / 30％H 2 O 2或Me 3 NO 3氧化，得到相应的手性β-氨基醇。 在25℃下进行的反应，对映异构体的过量范围为60％，对于在-25℃下进行的反应为大于99％
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公开(公告)号：US06362373B1
公开(公告)日：2002-03-26
申请号：US09661421
申请日：2000-09-13
IPC分类号： C07C20922
CPC分类号： C07D295/096 , C07B2200/07 , C07C213/04 , C07C215/44 , C07C2601/14 , C07C2603/74 , C07D209/44 , C07D211/14 , C07D211/62 , C07D217/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/205
摘要： The disclosed invention comprises a compound having the formula: in which R1 and R2 independently represent a hydrogen or an alkyl group of 4 carbon atoms or greater. Further disclosed is a process for the preparation of the disclosed chiral amino alcohols from a starting amine compound and a limonene oxide.
摘要翻译： 所公开的发明包括具有下式的化合物：其中R 1和R 2独立地表示氢或4个或更多个碳原子的烷基。 进一步公开的是从起始胺化合物和柠檬烯氧化物制备公开的手性氨基醇的方法。
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公开(公告)号：US4895996A
公开(公告)日：1990-01-23
申请号：US258744
申请日：1988-10-17
IPC分类号： C07C1/32 , C07C11/02 , C07D211/70 , C07D213/06 , C07D213/127 , C07D213/16 , C07D309/18 , C07D317/72 , C07D333/08 , C07D335/02
CPC分类号： C07D213/06 , C07C1/323 , C07C11/02 , C07D211/70 , C07D213/16 , C07D309/18 , C07D317/72 , C07D333/08 , C07D335/02
摘要： Alkenes are prepared by the hydroboration of enamines followed by an elimination reaction to form the alkene. This process has wide applicability and is useful for the stereospecific synthesis of [Z] isomers. It is preferred to use 9-borabicyclo[3.3.1 nonane as the hydroborating agent and to use methanol to catalyze the elimination reaction.
摘要翻译： 烯烃通过烯胺的氢化制备，然后进行消除反应以形成烯烃。 该方法具有广泛的适用性，可用于[Z]异构体的立体有择合成。 优选使用9-硼双环[3.3.1壬烷作为加氢硼化剂，并使用甲醇催化消除反应。
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5.发明授权
公开(公告)号：US4886924A
公开(公告)日：1989-12-12
申请号：US258743
申请日：1988-10-17
IPC分类号： C07D333/08
CPC分类号： C07D333/08
摘要： A process for the stereospecific synthesis of [E] alkenes from enamines comprising the steps of hydroborating the enamine; esterifying the organoborane so formed and oxidizing the boronic ester in the presence of hydrogen peroxide and in the absence of added base under conditions sufficient to form the [E] alkene in high yield.
摘要翻译： 从烯胺立体特异性合成[E]烯烃的方法，包括加氢烯胺的步骤; 酯化如此形成的有机硼烷，并在过氧化氢存在下和在不加入碱的情况下将硼酸酯氧化成足以以高产率形成[E]烯烃的条件。
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公开(公告)号：US20090149656A1
公开(公告)日：2009-06-11
申请号：US12189089
申请日：2008-08-08
IPC分类号： C07D401/00 , C07C69/52
CPC分类号： A61K49/0019 , B82Y5/00 , B82Y10/00 , B82Y15/00 , B82Y30/00 , C07D213/82 , C07F5/025 , C09K9/02 , C09K2211/1007 , C09K2211/1011 , C09K2211/1029 , G01N33/542 , G01N33/543 , G01N33/582 , G01N33/66 , Y10T436/144444
摘要： The present invention concerns an improved optical method and optical sensing device for determining the levels of polyhydroxyl-substituted organic molecules in vitro and/or in vivo in aqueous media. The range of detection is between about 400 and 800 nm. In particular, a sensory devise is implemented in a mammal to determine sugar levels. Specifically, a dye is combined with a conjugated nitrogen-containing heterocyclic aromatic boronic acid-substituted bis-onium compound in the presence of a sugar, such as fructose or glucose. The viologens are preferred as the aromatic conjugated nitrogen-containing boronic acid substituted compounds. The method is useful to determine sugar levels in a human being.
摘要翻译： 本发明涉及一种改进的光学方法和光学感测装置，用于确定水性介质中体外和/或体内多羟基取代的有机分子的水平。 检测范围在约400和800nm之间。 特别地，在哺乳动物中实施感官设计以确定糖水平。 具体地说，在糖如果糖或葡萄糖的存在下，将染料与共轭含氮杂环芳族硼酸取代的双鎓化合物组合。 紫罗兰是优选的芳族共轭含氮硼酸取代的化合物。 该方法对于测定人的糖含量是有用的。
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公开(公告)号：US06465193B2
公开(公告)日：2002-10-15
申请号：US09466994
申请日：1999-12-10
申请人： Mark Akeson , David W. Deamer , Wenonah Vercoutere , Hugh E. Olsen , Rebecca Braslau , Bakthan Singaram , Derek Steiner , Frank Cappuccio
发明人： Mark Akeson , David W. Deamer , Wenonah Vercoutere , Hugh E. Olsen , Rebecca Braslau , Bakthan Singaram , Derek Steiner , Frank Cappuccio
IPC分类号： G01N3353
CPC分类号： G01N33/5438 , C12Q1/6823 , G01N33/48721 , G01N33/532 , G01N33/54386 , C12Q2565/607 , C12Q2563/179 , C12Q2523/319
摘要： Targeted molecular bar codes and methods for using the same are provided. The subject targeted molecular bar codes include a molecular bar code and a member of a specific binding pair, where the specific binding pair member is generally bonded to the bar code through a linking group. The subject molecular bar code may be read during translocation through a single nano-meter scale pore. The subject targeted molecular bar codes find use in a variety of different applications involving analyte detection, such as screening and diagnostic applications.
摘要翻译： 提供了目标分子条形码及其使用方法。 受试者靶向分子条形码包括分子条形码和特异性结合对的成员，其中特异性结合对成员通常通过连接基团键合到条形码。 在通过单个纳米尺度孔隙的易位期间可以读取主题分子条形码。 主题分子条形码可用于涉及分析物检测的各种不同应用，如筛选和诊断应用。
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公开(公告)号：US20150119580A1
公开(公告)日：2015-04-30
申请号：US14234382
申请日：2012-07-20
申请人： Jacob W. Clary , Bakthan Singaram
发明人： Jacob W. Clary , Bakthan Singaram
摘要： Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg0. When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
摘要翻译： 通过Grignard试剂与含硼底物的反应，在环境温度下在醚溶剂中合成硼酸酯和硼酸。 含硼底物可以是硼酸酯，例如频哪醇硼烷，新戊基乙二醇硼烷，或二异丙基氨基硼烷等二烷基氨基硼烷化合物。 格氏试剂可以由烷基，烯基，芳基，芳基烷基，杂芳基，乙烯基或烯丙基卤化合物和MgO预先形成或生成。 当含硼底物是硼酸酯时，反应通常在室温下进行，而不在约1至3小时内加入碱以形成硼酸酯化合物。 当含硼底物是二烷基氨基硼烷化合物时，反应通常在0℃下在约1小时内完成以形成硼酸化合物。
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公开(公告)号：US07968714B2
公开(公告)日：2011-06-28
申请号：US12189089
申请日：2008-08-08
IPC分类号： C07F5/02 , C07D401/04
CPC分类号： A61K49/0019 , B82Y5/00 , B82Y10/00 , B82Y15/00 , B82Y30/00 , C07D213/82 , C07F5/025 , C09K9/02 , C09K2211/1007 , C09K2211/1011 , C09K2211/1029 , G01N33/542 , G01N33/543 , G01N33/582 , G01N33/66 , Y10T436/144444
摘要： The present invention concerns an improved optical method and optical sensing device for determining the levels of polyhydroxyl-substituted organic molecules in vitro and/or in vivo in aqueous media. The range of detection is between about 400 and 800 nm. In particular, a sensory devise is implemented in a mammal to determine sugar levels. Specifically, a dye is combined with a conjugated nitrogen-containing heterocyclic aromatic boronic acid-substituted bis-onium compound in the presence of a sugar, such as fructose or glucose. The viologens are preferred as the aromatic conjugated nitrogen-containing boronic acid substituted compounds. The method is useful to determine sugar levels in a human being.
摘要翻译： 本发明涉及一种改进的光学方法和光学感测装置，用于确定水性介质中体外和/或体内多羟基取代的有机分子的水平。 检测范围在约400和800nm之间。 特别地，在哺乳动物中实施感官设计以确定糖水平。 具体地说，在糖如果糖或葡萄糖的存在下，将染料与共轭含氮杂环芳族硼酸取代的双鎓化合物组合。 紫罗兰是优选的芳族共轭含氮硼酸取代的化合物。 该方法对于测定人的糖含量是有用的。
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公开(公告)号：US09243004B2
公开(公告)日：2016-01-26
申请号：US14234382
申请日：2012-07-20
申请人： Jacob W. Clary , Bakthan Singaram
发明人： Jacob W. Clary , Bakthan Singaram
摘要： Boronic esters and boronic acids are synthesized at ambient temperature in an ethereal solvent by the reaction of Grignard reagents with a boron-containing substrate. The boron-containing substrate may be a boronic ester such as pinacolborane, neopentylglycolborane, or a dialkylaminoborane compound such as diisopropylaminoborane. The Grignard reagents may be pre-formed or generated from an alkyl, alkenyl, aryl, arylalkyl, heteroaryl, vinyl, or allyl halide compound and Mg0. When the boron-containing substrate is a boronic ester, the reactions generally proceed at room temperature without added base in about 1 to 3 hours to form a boronic ester compound. When the boron-containing substrate is a dialkylaminoborane compound, the reactions generally proceed to completion at 0° C. in about 1 hour to form a boronic acid compound.
摘要翻译： 通过Grignard试剂与含硼底物的反应，在环境温度下在醚溶剂中合成硼酸酯和硼酸。 含硼底物可以是硼酸酯，例如频哪醇硼烷，新戊基乙二醇硼烷，或二异丙基氨基硼烷等二烷基氨基硼烷化合物。 格氏试剂可以由烷基，烯基，芳基，芳基烷基，杂芳基，乙烯基或烯丙基卤化合物和MgO预先形成或生成。 当含硼底物是硼酸酯时，反应通常在室温下进行，而不在约1至3小时内加入碱以形成硼酸酯化合物。 当含硼底物是二烷基氨基硼烷化合物时，反应通常在0℃下在约1小时内完成以形成硼酸化合物。
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