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1. 发明授权

US06630577B2 1,2-Phenylenediboronic acid reagents and complexes 失效
标题翻译： 1,2-苯基二硼酸试剂和络合物
公开(公告)号：US06630577B2
公开(公告)日：2003-10-07
申请号：US09874633
申请日：2001-06-04
申请人： Mark L. Stolowitz , Guisheng Li , Jean P. Wiley
发明人： Mark L. Stolowitz , Guisheng Li , Jean P. Wiley
IPC分类号： C07F502
CPC分类号： C07J1/00 , C07C229/38 , C07C233/49 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/025 , G01N33/531 , G01N33/54353 , Y10S530/81 , Y10S530/816
摘要： A reagent having the general formula of General Formula I: wherein group Z comprises a spacer selected from an aliphatic chain up to about 6 carbon equivalents in length, an unbranched aliphatic chain of from about 6 to 18 carbon equivalents in length with at least one of an intermediate amide and a disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; wherein group R is an electrophilic or nucleophilic moiety suitable for reaction of the reagent with a biologically active species; and wherein group Q is one of nothing at all, an amide, a methyl amide, a methylene, an ether, a thioether, a methyl ether, and a methyl thioether moiety. Also, a conjugate, a bioconjugate and a method of conjugating.
摘要翻译：具有通式I的通式的试剂：其中基团Z包括选自长度为约6碳当量长度的脂肪族链的间隔基，长度为约6至18个碳当量长度的无支链脂族链，其中至少一个为中间体酰胺和二硫化物部分，和长度为约3至12个碳当量的聚乙二醇链; 其中基团R是适于试剂与生物活性物质的反应的亲电或亲核部分; 并且其中基团Q是任何一个，酰胺，甲基酰胺，亚甲基，醚，硫醚，甲基醚和甲基硫醚部分。另外，缀合物，生物缀合物和缀合方法。

2. 发明授权

US06590100B2 Process for preparing a polyaromatic compound 失效
标题翻译：制备多芳族化合物的方法
公开(公告)号：US06590100B2
公开(公告)日：2003-07-08
申请号：US10146263
申请日：2002-05-15
申请人： Jean-Christophe Galland , Monique Savignac , Jean-Pierre Genet
发明人： Jean-Christophe Galland , Monique Savignac , Jean-Pierre Genet
IPC分类号： C07F502
CPC分类号： C07C17/263 , C07C1/321 , C07C45/68 , C07C213/08 , C07C221/00 , C07D333/06 , C07C15/00 , C07C225/22
摘要： The present invention provides a process for preparing a polyaromatic compound comprising at least one sequence of two aromatic rings. The process of the invention, which consists in reacting an aromatic compound bearing a leaving group and an arylboronic acid and/or its derivatives in the presence of a base and an effective amount of a nickel catalyst, is characterized in that the reaction is conducted in a reaction solvent which is water optionally in a mixture with an organic solvent and in the presence of an effective amount of a catalyst based on nickel with at least one water-soluble phosphine ligand.
摘要翻译：本发明提供了一种制备包含至少一个两个芳香环序列的多芳族化合物的方法。本发明的方法包括使带有离去基团的芳族化合物与芳基硼酸和/或其衍生物在存在下反应的碱和有效量的镍催化剂的特征在于反应在反应溶剂中进行，反应溶剂是任选与有机溶剂的混合物的水，并且在有效量的基于镍的催化剂存在下，至少一种水溶性膦配体。

3. 发明授权

US06576789B1 Process for the preparation of substituted phenylboronic acids 失效
标题翻译：制备取代苯基硼酸的方法
公开(公告)号：US06576789B1
公开(公告)日：2003-06-10
申请号：US09553036
申请日：2000-04-20
申请人： Steffen Haber , Andreas Meudt , Stefan Scherer , Frank Vollmueller
发明人： Steffen Haber , Andreas Meudt , Stefan Scherer , Frank Vollmueller
IPC分类号： C07F502
CPC分类号： C07F5/025 , C07F3/02 , Y02P20/55
摘要： Compounds of the formula (I) in which Q1 and Q2 are each OH or form a trimeric boric anhydride, Z is CHO, CH2Y, X or a protected aldehyde group, and X is CN, COOH, COCl, CONH2 or C(OR)3, and Y is OH or NH2, and Z is in the o-, m- or p-position to the boronic acid radical, are prepared by a) reacting a compound of the formula (II) with Mg in the presence of an anthracene compound and, if desired, a transition-metal halide and, if desired, an Mg halide or in the presence of a transition-metal halide and, if desired, an Mg halide, to give the corresponding arylmagnesium chloride, b) reacting the latter with a borate of the formula B(OR′)3 and hydrolyzing the product, with removal of the aldehyde protecting group, c) and, if desired, oxidizing or reducing the free aldehyde group.
摘要翻译：式（I）化合物，其中Q 1和Q 2各自为OH或形成三聚硼酸酐，Z为CHO，CH 2 Y，X或保护的醛基，X为CN，COOH，COCl，CONH 2或C（OR）3 ，并且Y是OH或NH 2，并且Z与硼酸根在o-，m-或p-位，是通过以下方法制备的：a）在蒽化合物存在下使式（II）化合物与Mg反应制备如果需要，可以使用过渡金属卤化物，如果需要，还可以在过渡金属卤化物存在下，或者如果需要的话使用卤化镁，得到相应的芳基氯化镁，b）使后者与式B（OR'）3的硼酸盐，并水解产物，除去醛保护基，c），如果需要，氧化或还原游离醛基。

4. 发明授权

US06410764B1 Method for preparation of boratabenzene derivatives 失效
标题翻译：硼代苯衍生物的制备方法
公开(公告)号：US06410764B1
公开(公告)日：2002-06-25
申请号：US09764722
申请日：2001-01-18
申请人： Leonard V. Cribbs , Bradley P. Etherton
发明人： Leonard V. Cribbs , Bradley P. Etherton
IPC分类号： C07F502
CPC分类号： C07F17/00 , C07F5/027
摘要： A process for preparing boratabenzene derivatives is provided. The process includes the hydrogenation of a compound containing a boranaphthalene functional group to form a boratabenzene-containing compound. Depending on the compound containing a boranaphthalene functional group, the resulting boratabenzene compound may be converted into a catalyst suitable for olefin polymerization. A process for forming a boratabenzene derivative from a halo-dioxaborolane is also provided. In this process, a halo-dioxaborolane is reacted with a piperylide salt for form a pentadienyl dioxaborolane. The pentadienyl-dioxaborolane is reacted with a strong base to form an intermediate boratacyclohexanediene salt. The intermediate boratacyclohexanediene salt is then reacted with a trialkylaluminum compound to form an alkylboratabenzene salt.
摘要翻译：提供了一种制备硼代苯衍生物的方法。该方法包括含有硼烷官能团的化合物的氢化以形成含硼代苯的化合物。根据含有硼烷官能团的化合物，所得的硼代苯化合物可以转化为适用于烯烃聚合的催化剂。还提供了由卤代二氧硼烷制备硼代苯衍生物的方法。在该方法中，将卤代二氧杂硼杂环戊烷与哌啶子盐反应形成戊二烯基二氧杂硼杂环戊烷。将戊二烯基二氧杂硼杂环戊烷与强碱反应形成中间体硼烷环己烷二盐。然后将中间体硼烷环己二烯盐与三烷基铝化合物反应以形成烷基硼代苯盐。

5. 发明授权

US06388138B1 Process for producing a magnesium di[tetrakis(Faryl)borate] and products therefrom 有权
标题翻译：二[四（氟芳基）硼酸镁]及其制品的制备方法
公开(公告)号：US06388138B1
公开(公告)日：2002-05-14
申请号：US09724647
申请日：2000-11-28
申请人： John Y. Lee
发明人： John Y. Lee
IPC分类号： C07F502
CPC分类号： C07F5/027
摘要： A solution comprising a halomagnesium tetrakis(Faryl)borate in a liquid organic medium, wherein the liquid organic medium is comprised of one or more liquid dihydrocarbyl ethers, one or more liquid hydrocarbons, one or more liquid halogenated hydrocarbons, or mixtures thereof, is contacted with water. This produces magnesium di[tetrakis(Faryl)borate] in the organic phase of a two-phase water/liquid organic medium. The magnesium di[tetrakis(Faryl)borate] can be, but need not be, isolated. A protic ammonium salt, an onium salt, or a triarylmethyl salt can be reacted with the magnesium di[tetrakis(Faryl)borate] to produce the corresponding protic ammonium, onium, or triarylmethyl tetrakis(Faryl)borate. The magnesium di[tetrakis(Faryl)borate] can instead be reacted with a metal salt to form a metal tetrakis(Faryl)borate. The produced metal tetrakis(Faryl)borate can be further reacted with a protic ammonium salt, an onium salt, or a triarylmethyl salt to yield a protic ammonium, onium, or triarylmethyl tetrakis(Faryl)borate. Certain of these tetrakis(Faryl)borates can be conveniently purified via the formation of a liquid clathrate at ambient temperatures.
摘要翻译：一种在液体有机介质中包含四（氟芳基）硼酸镁的溶液，其中所述液体有机介质由一种或多种液态二烃基醚，一种或多种液态烃，一种或多种液态卤代烃或其混合物组成，与水。这在二相水/液体有机介质的有机相中产生二[四（氟芳基）硼酸镁]镁。二[四（氟芳基）硼酸镁]可以是但不必是孤立的。可以将质子铵盐，鎓盐或三芳基甲基盐与二[四（氟芳基）硼酸镁]反应以产生相应的质子铵，鎓或三芳基甲基四（氟芳基）硼酸盐。二[四（氟芳基）硼酸镁]可以代替与金属盐反应形成四（氟芳基）硼酸金属。所制备的四（氟芳基）硼酸金属盐可以进一步与质子铵盐，鎓盐或三芳基甲基盐反应，得到质子铵，鎓或三芳基甲基四（氟芳基）硼酸盐。这些四（Faryl）硼酸盐中的某些可以通过在环境温度下形成液体包合物来方便地纯化。

6. 发明授权

US06833470B2 Method for producing formylphenylboronic acids 有权
公开(公告)号：US06833470B2
公开(公告)日：2004-12-21
申请号：US10433827
申请日：2003-06-05
申请人： Andreas Meudt , Stefan Scherer , Frank Vollmueller , Michael Erbes
发明人： Andreas Meudt , Stefan Scherer , Frank Vollmueller , Michael Erbes
IPC分类号： C07F502
CPC分类号： C07F5/025
摘要： A process for preparing formylphenylboronic acids of the formula (I) by reaction of protected chlorobenzaldehydes of the formula (II) with lithium in an inert solvent to form compounds of the formula (III) and subsequent reaction with a boron compound of the formula BY3 to give compounds of the formula (I).

7. 发明授权

US06706925B2 Process for preparing bisallylboranes and nonaromatic boronic acids 失效
标题翻译：制备双烯丙基硼烷和非芳族硼酸的方法
公开(公告)号：US06706925B2
公开(公告)日：2004-03-16
申请号：US10236749
申请日：2002-09-06
申请人： Stefan Scherer , Alexei Kalinin , Victor Snieckus
发明人： Stefan Scherer , Alexei Kalinin , Victor Snieckus
IPC分类号： C07F502
CPC分类号： C07F5/027
摘要： A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents R1 to R6 having the following meanings: R1-R6 are H, aryl or substituted or unsubstituted C1-C4-alkyl or two radicals R may be closed to form a cyclic system. As oxidant, it is possible to use, for example, alkyl halides or dialkyl sulfates. In a particularly preferred embodiment, the diene used is 2,5-dimethylhexa-2,4-diene (R1, R2, R5, R6=methyl, R3, R4=H).
摘要翻译：在惰性溶剂中在氧化剂存在下使二烯与硼氢化钠反应制备式（I）的双烯丙基硼烷的方法，其中原位产生的硼烷与二烯选择性地反应形成式（I）的双（烯丙基）硼烷，（I）和具有以下含义的取代基R 1至R 6具有以下含义：R 1 -R 6是H，芳基或取代或未取代的C 1 -C 4 - 烷基或两个基团R可以被封闭形成环状体系。作为氧化剂，可以使用例如烷基卤化物或二烷基硫酸盐。在一个特别优选的实施方案中，所用的二烯是2,5-二甲基己-1,4-二烯（R 1，R 2，R 5，R 6 =甲基，R 3，R 4）= H）。

8. 发明授权

US06600066B1 Method for producing mono-organoboranes or di-organoboranes 失效
标题翻译：制备单有机硼烷或二有机硼烷的方法
公开(公告)号：US06600066B1
公开(公告)日：2003-07-29
申请号：US09868074
申请日：2001-06-14
申请人： Jörg Schottek , Patricia Becker , Iris Küllmer
发明人： Jörg Schottek , Patricia Becker , Iris Küllmer
IPC分类号： C07F502
CPC分类号： C07F5/02 , C07F5/025 , C07F5/066
摘要： A novel process for preparing perhalogenated monoorganoboranes or diorganoboranes which makes it possible to obtain these compounds under conditions which can readily be implemented in the industry is described.
摘要翻译：描述了一种制备全卤代单有机硼烷或二有机硼烷的新方法，其使得可以在可容易地在工业中实施的条件下获得这些化合物成为可能。

9. 发明授权

US06462179B1 Phenyldiboronic acid reagents and complexes 失效
标题翻译：苯二硼酸试剂和络合物
公开(公告)号：US06462179B1
公开(公告)日：2002-10-08
申请号：US09625231
申请日：2000-07-25
申请人： Mark L. Stolowitz , Edward A. Kesicki , Kevin P. Lund , Karin A. Hughes
发明人： Mark L. Stolowitz , Edward A. Kesicki , Kevin P. Lund , Karin A. Hughes
IPC分类号： C07F502
CPC分类号： C07C233/49 , C07C229/38 , C07C233/51 , C07C237/12 , C07C237/22 , C07C255/13 , C07C259/10 , C07C271/22 , C07C281/02 , C07D207/452 , C07D207/46 , C07D213/71 , C07F5/025 , C07K5/0207 , G01N33/531 , G01N33/54353 , Y10S530/81 , Y10S530/816
摘要： Reagents suitable for the modification of a bioactive species for the purpose of incorporating one or more phenyldiboronic acid (PDBA) moieties for subsequent conjugation to a different (or the same) bioactive species having one or more pendant boronic compound complexing moieties of the general formula of General Formula I, wherein group R is a reactive electrophilic or nucleophilic moiety suitable for reaction of the PDBA reagent with a bioactive species. Group Z is a spacer selected from a saturated or unsaturated chain up to about 0 to 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moiety, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length. Group Q is a linkage that includes one of amide, ether and thioether moieties. Group R is preferably selected from, but not limited to, one of acrylamide, bromo, bromoacetamide, chloro, chloroacetamide, dithiopyridyl, hydrazide, N-hydroxysuccinimidyl ester, N-hydroxysulfo-succinimidyl ester, imidate ester, imidazolide, iodo, iodoacetamide, maleimide, amino and thiol moieties. Group Z is preferably an unbranched alkyl chain of the general formula (CH2)n, wherein n=1 to 6. Group Q is preferably selected from one of NHCO, CONH, NHCOCH2, CONHCH2, O, OCH2, S, and SCH2 moieties.
摘要翻译：适于修饰生物活性物质的试剂，用于引入一种或多种苯基二硼酸（PDBA）部分以用于随后与不同（或相同）生物活性物质缀合的具有一个或多个通式的侧链化合物络合部分的生物活性物质通式I，其中基团R是适于PDBA试剂与生物活性物质反应的反应性亲电或亲核部分。 Z组是选自饱和或不饱和链长度至多约0至6当量长度的间隔基，长度为约6至18当量长度的至少一个中间体酰胺或二硫化物部分的无支链饱和或不饱和链，以及长度为约3至12碳当量的聚乙二醇链。 Q组是包括酰胺，醚和硫醚部分之一的连接。基团R优选选自但不限于丙烯酰胺，溴代，溴乙酰胺，氯代，氯乙酰胺，二硫代吡啶基，酰肼，N-羟基琥珀酰亚胺酯，N-羟基磺基琥珀酰亚胺酯，亚氨酸酯，咪唑啉，碘，碘乙酰胺，马来酰亚胺，氨基和硫醇部分。组Z优选为通式（CH 2）n的无支链烷基链，其中n = 1-6。组Q优选选自NHCO，CONH，NHCOCH2，CONHCH2，O，OCH2，S和SCH2部分之一。

10. 发明授权

US06444846B1 Process for preparing tetrafluoroborate salt and intermediates thereof 失效
标题翻译：制备四氟硼酸盐的方法及其中间体
公开(公告)号：US06444846B1
公开(公告)日：2002-09-03
申请号：US09838479
申请日：2001-04-19
申请人： W. Novis Smith , Joel McCloskey
发明人： W. Novis Smith , Joel McCloskey
IPC分类号： C07F502
CPC分类号： C07C209/12 , C07C211/63
摘要： There is provided a process for preparing tetraalkyl ammonium halide utilizing a catalytic amount of acetonitrile in a reaction under pressure and at an elevated temperature of an alkyl halide and a trialkyl halide and in which tetrafluoroborate can be subsequently prepared.
摘要翻译：在烷基卤化物和三烷基卤化物的加压和升高的温度下，提供了使用催化量的乙腈制备四烷基卤化铵的方法，其中随后可以制备四氟硼酸盐。

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