Method for the asymmetric dihydroxylation of olefins, using osmium catalysts
    21.
    发明授权
    Method for the asymmetric dihydroxylation of olefins, using osmium catalysts 失效
    使用锇催化剂对烯烃的不对称二羟基化反应的方法

    公开(公告)号:US06472570B1

    公开(公告)日:2002-10-29

    申请号:US09980504

    申请日:2001-10-19

    IPC分类号: C07C3326

    CPC分类号: C07C29/50 C07C33/26

    摘要: This invention relates to process for asymmetric dihydroxylation of olefins using osmium catalysts to obtain monofunctional, bifunctional, and/or polyfunctional chiral 1,2-diols of the formula (I) R1R2C(OH)—C(OH)R3R4  (I) where R1 to R4 are defined herein, by reacting an olefin of the formula (II) R1R2C═CR3R4  (II) where R1 to R4 are defined as for formula (I), with molecular oxygen in the presence of an osmium compound and a chiral amine ligand in water or a water-containing solvent mixture at a pH of from 8.5 to 13.

    摘要翻译: 本发明涉及使用锇催化剂来获得烯烃不对称二羟基化的方法,以获得式(I)的单官能,双功能和/或多官能的手性1,2-二醇,其中R 1至R 4在本文中定义,通过使式 (II)其中R 1至R 4如式(I)所定义,分子氧在锇化合物和手性胺配体存在下在水或含水溶剂混合物中的pH为8.5至13。

    Base-catalyzed synthesis of 1-aryl-4-(aryl ethyl)piperazines from aromatic olefins and 1-arylpiperazines
    22.
    发明授权
    Base-catalyzed synthesis of 1-aryl-4-(aryl ethyl)piperazines from aromatic olefins and 1-arylpiperazines 失效
    芳基烯烃和1-芳基哌嗪的碱基催化合成1-芳基-4-(芳基乙基)哌嗪

    公开(公告)号:US06313297B1

    公开(公告)日:2001-11-06

    申请号:US09600274

    申请日:2000-07-13

    IPC分类号: C07D29502

    摘要: A process for preparing a 1-aryl-4-(arylethyl)piperazine of the formula (I) by reacting a 1-arylpiperazine of the formula (II) with an aromatic olefin of the formula (III) Ar′CR1═CHR2  (III) in an inert solvent in the presence of at least one basic catalyst, where in the formulae (I) to (III) Ar and Ar′ independently of one another are an aryl radical, selected from the group of the fused and unfused C6-C22-aromatics and the fused or unfused C5-C22-heteroaromatics which have at least one nitrogen, oxygen or sulfur atom in the ring; and R1 and R2 independently of one another are a hydrogen atom, a C1-C8-alkyl radical or an aryl radical Ar.

    摘要翻译: 在惰性溶剂中,使式(I)的1-芳基-4-(芳基乙基)哌嗪通过式(II)的1-芳基哌嗪与式(III)的芳族烯烃在惰性溶剂中反应来制备式 至少一种碱性催化剂,其中在式(I)至(III)中Ar和Ar'彼此独立地为芳基,其选自稠合和未融合的C6-C22-芳族化合物和稠合或未融合的 在环中具有至少一个氮,氧或硫原子的C5-C22-杂芳族化合物; 并且R 1和R 2彼此独立地是氢原子,C 1 -C 8 - 烷基或芳基Ar。

    Process for the preparation of imidazolidine-2, 4-diones
    23.
    发明授权
    Process for the preparation of imidazolidine-2, 4-diones 失效
    咪唑烷-2,4-二酮的制备方法

    公开(公告)号:US06235910B1

    公开(公告)日:2001-05-22

    申请号:US09400311

    申请日:1999-09-21

    IPC分类号: C07D23340

    CPC分类号: C07D233/74

    摘要: A process for the preparation of compounds of the general formula (I) by reacting an aldehyde compound of the general formula (II) with a urea compound of the general formula (III) in the presence of carbon monoxide and a catalytically active metal compound. Compounds of the general formula (I) are important intermediates for the synthesis of &agr;-amino acids.

    摘要翻译: 在一氧化碳和催化活性金属化合物的存在下使通式(II)的醛化合物与通式(III)的脲化合物反应制备通式(I)的化合物的方法。 通式(I)的化合物是合成α-氨基酸的重要中间体。

    Phosphanes, their method of production and use in metal complexes
    24.
    发明授权
    Phosphanes, their method of production and use in metal complexes 失效
    磷化物,它们的生产和使用方法在金属络合物中

    公开(公告)号:US06225504B1

    公开(公告)日:2001-05-01

    申请号:US09331826

    申请日:1999-06-23

    IPC分类号: C07F950

    摘要: A process for the preparation of the formula Ar13−xP[(Ar2(OZ)y]x  I wherein Ar1 and Ar2 are individually aromatic of 6 to 20 carbon atoms or heteroaromatic of 4 to 9 carbon atoms, each unsubstituted or substituted with at least one member of the group consisting of halogen, carboxyl, —OH, alkyl of 1 to 6 carbon atoms, phenyl and naphthyl, Ar1 has one valence and R2 has y+1 valences, x is an integer of 1, 2 or 3, y is 1 or 2, Z is carbohydrate with a glycosidic bond comprising reacting a hydrocarbon halide of the formula Z′—X  II when Z′ has the definition of Z with —OH protected and X is chlorine, bromine or fluorine with a phosphane of the formula Ar13−xP[(Ar2 (OH)y]x  III in a multi-phase reaction medium in the presence of a base and a phase transfer catalyst to form a phosphane of the formula Ar13−xP[(Ar2(OZ1)y]x  IV and removal of the protective groups to form a compound of Formula I, metal complexes thereof and various processes.

    摘要翻译: 制备糠醛的方法Ar1和Ar2分别为6至20个碳原子的芳族或4至9个碳原子的杂芳族化合物,每个未取代或被至少一个由卤素,羧基,-OH, 具有1至6个碳原子的烷基,苯基和萘基,Ar 1具有一个化合价,R 2具有y + 1价,x是1,2或3的整数,y是1或2,Z是具有糖苷键的碳水化合物, 在碱和相转移催化剂存在下形成多相反应介质的烃卤化物,以形成下式的膦并除去保护基以形成式I化合物,其金属络合物和各种方法。

    Catalyst and process for the production of aldehydes by hydroformylation of olefinically unsaturated compounds
    25.
    发明授权
    Catalyst and process for the production of aldehydes by hydroformylation of olefinically unsaturated compounds 失效
    通过烯属不饱和化合物的加氢甲酰化生产醛的催化剂和方法

    公开(公告)号:US06191063B1

    公开(公告)日:2001-02-20

    申请号:US09230576

    申请日:1999-07-01

    IPC分类号: B01J3128

    摘要: A catalyst comprising rhodium and a compound of the formula (I) in which m is a number from 1 to 1000; x is a number from 0 to 4; W is a group of the formulae —CH2—CH2—, —CH(CH3)CH2—or —CH2CH(CH3)—; R is hydrogen, a straight-chain or branched C1-C5— alkyl radical; or a group of the formulae where a, b, c, d and e independently of one another are a number from 0 to 1000, at least one of the numbers a, b, c, d and e being greater than 0; R5, R6, R7, R8 and R9 are identical or different and are hydrogen, C1-C5-alkyl or a group of the formula R1 and R2 are identical or different and are a straight-chain, branched or cyclic C1-C30-alkyl radical or C6-10-aryl radical, which is unsubstituted or substituted by from one to five C1-C3-alkyl radicals, and L is C1-C5-alkyl, C1-C5-alkoxy, NO2, NR3R4, where R3 and R4 independently of one another are hydrogen or C1-C4-alkyl, or L is Cl or OH, for hydroformylation reactions.

    摘要翻译: 一种催化剂,其包含铑和式(I)化合物,其中m为1至1000的数; x为0至4的数; W为式-CH 2 -CH 2 - , - CH(CH 3) CH2-或-CH2CH(CH3) - ; R是氢,直链或支链C1-C5-烷基; 或一组式,b,c,d和e彼此独立地为0至1000的数,数a,b,c,d和e中的至少一个大于0; R 5,R 6, R 7,R 8和R 9相同或不同,为氢,C 1 -C 5 - 烷基或式R 1和R 2的基团相同或不同,为直链,支链或环状C 1 -C 30 - 烷基或C 6-10 芳基,其是未取代的或被1至5个C 1 -C 3 - 烷基取代,且L是C 1 -C 5 - 烷基,C 1 -C 5 - 烷氧基,NO 2,NR 3 R 4,其中R 3和R 4彼此独立地是氢或 C1-C4烷基,或L是Cl或OH,用于加氢甲酰化反应。

    Halogenated cinnamic acids and esters thereof, processes for the
preparation thereof and halogenated aryldiazonium salts
    27.
    发明授权
    Halogenated cinnamic acids and esters thereof, processes for the preparation thereof and halogenated aryldiazonium salts 失效
    卤化肉桂酸​​及其酯,其制备方法和卤代芳基重氮盐

    公开(公告)号:US5516932A

    公开(公告)日:1996-05-14

    申请号:US178089

    申请日:1994-01-06

    摘要: The present invention relates to compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen or an alkyl radical having 1 to 18 carbon atoms and optionally containing oxygen, nitrogen or halogen, the radicals X, Y and Z are identical and are a fluorine, bromine or iodine atom or if two of the radicals X, Y or Z are identical or all of the radicals X, Y, Z are different from each other, X, Y and Z are a fluorine, chlorine, bromine or iodine atom. The invention further relates to a process for the preparation of the compounds, by reacting an aryldiazonium salt of the formula ##STR2## in which the radicals X, Y and Z are identical and are a fluorine, bromine or iodine atom or, if two of the radicals X, Y and Z are identical or all of the radicals X, Y, Z are different from each other, X, Y and Z are a fluorine, chlorine, bromine or iodine atom and A.sup.(-) is an anion of an acid having a pK.sub.a

    摘要翻译: 本发明涉及式(I)的化合物,其中R 1和R 2相同或不同并且是氢或具有1至18个碳原子并且任选地含有氧,氮或卤素的烷基,基团X, Y和Z相同并且是氟,溴或碘原子,或者如果基团X,Y或Z中的两个相同或基团X,Y,Z的全部彼此不同,则X,Y和Z是 氟,氯,溴或碘原子。 本发明还涉及通过使基团X,Y和Z相同且为氟,溴或碘原子的式(II)的芳基重氮盐与式 如果基团X,Y和Z中的两个相同或全部基团X,Y,Z彼此不同,X,Y和Z是氟,氯,溴或碘原子,并且A( - )是 具有pKa <7的酸的阴离子与式(III)的化合物反应,其中R 1和R 2相同或不同,并且是氢或具有1至18个碳原子的烷基,并且任选地含有氧,氮 或卤素,在含钯催化剂的存在下,如果合适,加入碱,和式(II)的芳基重氮盐。

    Process for preparing vinyl-substituted aromatic compounds from
arylamines
    28.
    发明授权
    Process for preparing vinyl-substituted aromatic compounds from arylamines 失效
    从芳基胺制备乙烯基取代的芳族化合物的方法

    公开(公告)号:US5475176A

    公开(公告)日:1995-12-12

    申请号:US222325

    申请日:1994-04-04

    CPC分类号: C07C41/30 C07B37/04 C07C2/86

    摘要: The present invention relates to a process for preparing vinyl-substituted aromatic compounds of the formula (I) Ar--CH.dbd.CH.sub.2, where Ar is a phenyl group that may bear 1 to 5 substituents, naphthyl or anthryl or a naphthyl radical bearing 1 to 7 substituents or an anthryl radical bearing 1 to 8 substituents, or a mononuclear five-, six- or seven-membered heterocyclic aromatic group which contains an oxygen atom and/or one or two nitrogen atoms in the ring and may bear 1 to 5 substituents, wherein an arylamine of the formula (II) Ar--NH.sub.2, where Ar has the aforementioned meaning, is reacted in an organic acid with an organic nitrite of the formula (III) R--ONO, where R is an alkyl group having 1 to 18 carbon atoms, a phenyl radical which may bear 1 to 3 alkyl groups each having 1 to 4 carbon atoms, or is an alkylcarbonyl group having 2 to 5 carbon atoms, and ethylene in an organic solvent in the presence of a palladium(0) of palladium(II) compound at temperatures of 0.degree. to 35.degree. C.

    摘要翻译: 本发明涉及制备式(I)所示的乙烯基取代的芳族化合物的方法Ar-CH = CH 2,其中Ar是可以带有1至5个取代基的苯基,含有1至5个取代基的萘基或蒽基或萘基 7个取代基或含有1至8个取代基的蒽基,或在环中含有氧原子和/或一个或两个氮原子的单核五,六或七元杂环芳族基团,并且可以具有1至5个取代基 其中式(II)Ar-NH 2的芳基胺(其中Ar具有上述含义)在有机酸与式(III)的有机亚硝酸酯R-ONO反应,其中R是具有1〜 18个碳原子,可具有1至3个具有1至4个碳原子的烷基或者是具有2至5个碳原子的烷基羰基的苯基,以及在有机溶剂中的钯(0)存在下的乙烯, 的钯(II)化合物在0℃至35℃的温度下进行。

    Ketophosphamide glycosides
    29.
    发明授权
    Ketophosphamide glycosides 失效
    扑热息痛糖尿病

    公开(公告)号:US5132416A

    公开(公告)日:1992-07-21

    申请号:US570191

    申请日:1990-08-20

    CPC分类号: C07H15/04

    摘要: Compounds of the formula (I) ##STR1## wherein R.sup.1 represents a pyranosyl radical and R.sup.4, R.sup.2, and R.sup.3 are as specified herein, compositions containing the compounds, methods of using the compounds to selectively kill tumor cells, and a process for the preparation of the compounds.

    摘要翻译: 式(I)的化合物其中R1表示吡喃糖基,R4,R2和R3如本文所述,含有该化合物的组合物,使用该化合物选择性杀死肿瘤细胞的方法和方法 用于制备化合物。