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    Process for the preparation of optically pure tetrahydropterins and derivatives, and specifically of optically pure tetrahydrofolic acid and derivatives thereof, by stereospecific hydrogenation
    3.
    发明授权
    Process for the preparation of optically pure tetrahydropterins and derivatives, and specifically of optically pure tetrahydrofolic acid and derivatives thereof, by stereospecific hydrogenation 有权
    通过立体特异性氢化制备光学纯四氢叶酸和衍生物，特别是光学纯的四氢叶酸及其衍生物的方法

    公开(公告)号：US07816525B1

    公开(公告)日：2010-10-19

    申请号：US10030692

    申请日：2000-07-12

    申请人： Hans Rudolf Muller ,  Rudolf Moser ,  Viola Groehn ,  Benoit Pugin

    发明人： Hans Rudolf Muller ,  Rudolf Moser ,  Viola Groehn ,  Benoit Pugin

    IPC分类号： C07D475/04

    CPC分类号： C07D475/04

    摘要： Process for the preparation of tetrahydropterin and tetrahydropterin derivatives by hydrogenating pterin and pterin derivatives with hydrogen in the presence of a hydrogenating catalyst, in which the hydrogenation is carried out in a polar reaction medium and metal complexes that are soluble in the reaction medium are employed as the hydrogenation catalysts. The process is suited to the hydrogenation, particularly asymmetric hydrogenation, of folic acid, folic acid salts, folic acid esters, folic acid ester salts or dihydroforms thereof, with the proviso that in the event of using folic acid, carboxylic acid salts thereof or dihydroforms thereof the reaction medium is aqueous, and in the event of using folic acid esters, folic acid ester salts or dihydroforms thereof the reaction medium is an alcohol. The process opens up straightforward access to achiral and chiral pterin derivatives.

    摘要翻译： 通过在氢化催化剂存在下氢气化蝶呤和蝶呤衍生物，其中氢极化在极性反应介质中进行，可溶于反应介质的金属配合物用作四氢去甲蝶呤和四氢蝶呤衍生物的方法， 氢化催化剂。 该方法适用于叶酸，叶酸盐，叶酸酯，叶酸酯盐或其二氢形式的氢化，特别是不对称氢化，条件是在使用叶酸的情况下，其羧酸盐或二氢形式 其反应介质是水性的，并且在使用叶酸酯，叶酸酯盐或其二氢形式的情况下，反应介质是醇。 该方法可以直接获得手性和手性蝶呤衍生物。

    Diphosphine ligands
    4.
    发明申请
    Diphosphine ligands 审中-公开
    二膦配体

    公开(公告)号：US20100029967A1

    公开(公告)日：2010-02-04

    申请号：US12308941

    申请日：2007-06-29

    申请人： Benoit Pugin ,  Xiangdong Feng ,  Felix Spindler

    发明人： Benoit Pugin ,  Xiangdong Feng ,  Felix Spindler

    IPC分类号： C07F15/00

    CPC分类号： C07F17/00 ,  B01J31/2295 ,  B01J31/2409 ,  B01J31/2428 ,  B01J2231/643 ,  B01J2231/645 ,  B01J2531/16 ,  B01J2531/17 ,  B01J2531/18 ,  B01J2531/821 ,  B01J2531/822 ,  B01J2531/824 ,  B01J2531/825 ,  B01J2531/827 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  C07B53/00 ,  C07F17/02

    摘要： Compounds of the formulae I and Ia in the form of mixtures of diastereomers or pure diastereomers, (I), (Ia), where R1 is a hydrogen atom or C1-C4-alkyl and R′1 is C1-C4-alkyl; X1 and X2 are each, independently of one another, a sec-phosphino group; T is C6-C20-arylene or C4-C18-heteroarylene having heteroatoms selected from the group consisting of O, S, —N═ and N(C1-C4-alkyl); v is 0 or an integer from 1 to 4; X1 is bound in the ortho position relative to the T-C* bond; Q is vinyl, methyl, ethyl, —CH2—OR, —CH2—N(C1-C4-alkyl)2 or a C- or S-bonded chiral group which directs metals of metallation reagents into the ortho position; R is hydrogen, a silyl radical or an aliphatic, cycloaliphatic, aromatic or aromatic-aliphatic hydrocarbon radical which has from 1 to 18 carbon atoms and is unsubstituted or substituted by C1-C4-alkyl, C1-C4-alkoxy, F or CF3; are ligands for metal complexes as homogeneous catalyst in asymmetric syntheses.

    摘要翻译： 式（I），（Ia），其中R 1是氢原子或C 1 -C 4 - 烷基和R 11是C 1 -C 4 - 烷基的非对映异构体或纯非对映体混合物形式的式I和Ia化合物; X1和X2各自独立地为仲膦基; T是具有选自O，S，-N-和N（C 1 -C 4 - 烷基）的杂原子的C 6 -C 20亚芳基或C 4 -C 18亚杂芳基; v为0或1至4的整数; X1相对于T-C *键的邻位结合; Q是乙烯基，甲基，乙基，-CH 2 -OR，-CH 2 -N（C 1 -C 4烷基）2或C-或S-键合的手性基团，其将金属化试剂的金属引导到邻位; R是氢，具有1至18个碳原子且未被取代或被C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，F或CF 3取代的甲硅烷基或脂族，脂环族，芳族或芳族 - 脂族烃基; 是不对称合成中金属络合物作为均相催化剂的配体。

    Ferrocene-Diphosphine Ligands
    5.
    发明申请
    Ferrocene-Diphosphine Ligands 审中-公开
    二茂铁 - 二膦配体

    公开(公告)号：US20090156851A1

    公开(公告)日：2009-06-18

    申请号：US11990208

    申请日：2006-08-10

    申请人： Walter Weissensteiner ,  Yaping Wang ,  Felix Spindler ,  Benoit Pugin ,  Xiangdong Feng

    发明人： Walter Weissensteiner ,  Yaping Wang ,  Felix Spindler ,  Benoit Pugin ,  Xiangdong Feng

    IPC分类号： C07F9/02 ,  C07F15/02

    CPC分类号： C07F17/02

    摘要： Compounds of the formula (I) in the form of racemates, mixtures of stereoisomers or optically pure stereoisomers, formula (I), where X1 and X2 are each, independently of one another, a secondary phosphino group; R1 is a halogen atom or a—substituent bound via a C atom, N atom, S atom, Si atom, a P(O) group or a P(S) group to the cyclopentadienyl ring; R2 is C1-C4-alkyl or phenyl; m is from 1 to 3 and n is 0 or from 1 to 5, are ligands for complexes of transition metals as enantioselective and homogeneous catalysts. As a result of the substitution, the conversion, the stereoselectivity and/or the configuration of the adduct formed can be influenced and optimization of catalysts can be made possible in this way.

    摘要翻译： 式（I）化合物为外消旋体形式，立体异构体混合物或光学纯立体异构体式（I），其中X1和X2各自独立地为次膦基; R1是通过C原子，N原子，S原子，Si原子，P（O）基团或P（S）键连接到环戊二烯基环上的卤素原子或取代基; R2是C1-C4烷基或苯基; m为1至3，n为0或1至5为过渡金属络合物作为对映选择性和均相催化剂的配体。 作为取代的结果，可以影响形成的加合物的转化率，立体选择性和/或构型，并且可以以这种方式使催化剂的优化成为可能。

    Chiral Ligands Used in Transition Metal Catysts for Asymmetric Addition Reactions Especially Hydrogenation
    7.
    发明申请
    Chiral Ligands Used in Transition Metal Catysts for Asymmetric Addition Reactions Especially Hydrogenation 有权
    用于非对称加成反应的过渡金属催化剂中的手性配体特别是氢化

    公开(公告)号：US20090171114A1

    公开(公告)日：2009-07-02

    申请号：US12227574

    申请日：2007-05-23

    申请人： Andreas Pfaltz ,  Yann Ribourdouille ,  Xiangdong Feng ,  Balamurugan Ramalingam ,  Benoit Pugin ,  Felix Spindler

    发明人： Andreas Pfaltz ,  Yann Ribourdouille ,  Xiangdong Feng ,  Balamurugan Ramalingam ,  Benoit Pugin ,  Felix Spindler

    IPC分类号： C07C69/34 ,  C07F15/02 ,  C07F9/53 ,  B01J31/18

    CPC分类号： C07F9/5022 ,  B01J31/1875 ,  B01J31/2495 ,  B01J2231/643 ,  B01J2231/645 ,  B01J2531/821 ,  B01J2531/822 ,  B01J2531/827 ,  C07B2200/07 ,  C07C51/36 ,  C07C67/303 ,  C07C213/02 ,  C07C231/12 ,  C07F15/008 ,  C07F17/02 ,  C07C57/30 ,  C07C69/675 ,  C07C69/732 ,  C07C69/34 ,  C07C217/08 ,  C07C233/47

    摘要： Ligands of the formula (I) secondary phosphine-Q-P(═O)HR1 (I) in the form of mixtures of diastereomers or pure diastereomers, in which secondary phosphine is a secondary phosphine group with hydrocarbon radicals or heterohydrocarbon radicals as substituents; Q is a bivalent bisaryl or bisheteroaryl radical with an axial chiral centre to which the two phosphorus atoms are bonded in the ortho positions to the bisaryl or bisheteroaryl bridge bond, or Q is a bivalent ferrocenyl radical with a planar chiral centre or without a planar chiral centre, to which the phosphorus atom of the secondary phosphine is bonded directly or via a C1-C4-carbon chain to a cyclopentadienyl ring, the —P*(═O)HR1 group is bonded either on the same cyclopentadienyl ring in ortho position to the bonded secondary phosphine or on the other cyclopentadienyl ring; P* is a chiral phosphorus atom, and R1 is a hydrocarbon radical, a heterohydrocarbon radical or a ferrocenyl radical, where R1 is a ferrocenyl radical with a planar chiral centre when Q is a ferrocenyl radical without a planar chiral centre. Metal complexes of these ligands are homogeneous catalysts for asymmetric addition reactions, particularly hydrogenations.

    摘要翻译： 式（I）以非对映异构体或纯非对映异构体混合物形式的仲膦-Q-P（-O）HR1（I）的配体，其中次膦是具有烃基或杂烃基作为取代基的仲膦基; Q是具有轴向手性中心的二价双芳基或双杂芳基，其中两个磷原子与双芳基或双杂芳基桥键的邻位键合，或Q是具有平面手性中心或不具有平面手性的二价二茂铁基 中心，仲膦的磷原子直接或通过C1-C4-碳键连接到环戊二烯基环上，-P *（ - O）HR 1基团在邻位相邻的环戊二烯基环上键合到 键合的次膦或在另一个环戊二烯基环上; P *是手性磷原子，R1是烃基，杂烃基或二茂铁基，其中当Q是没有平面手性中心的二茂铁基时，R 1是具有平面手性中心的二茂铁基。 这些配体的金属络合物是用于不对称加成反应的均相催化剂，特别是氢化。

    Ferrocenediphosphines
    8.
    发明申请
    Ferrocenediphosphines 有权
    二茂铁

    公开(公告)号：US20090124812A1

    公开(公告)日：2009-05-14

    申请号：US12226213

    申请日：2007-04-11

    申请人： Weiping Chen ,  Felix Spindler ,  Benoit Pugin

    发明人： Weiping Chen ,  Felix Spindler ,  Benoit Pugin

    IPC分类号： C07F15/02

    CPC分类号： C07F17/02 ,  C07B53/00 ,  C07F9/52

    摘要： Compounds of the formula I in the form of enantiomerically pure diastereomers or a mixture of diastereomers, (I), where the radicals R1 are identical or different and are each C1-C4-alkyl; m is 0 or an integer from 1 to 3; n is 0 or an integer from 1 to 4; R2 is a hydrocarbon radical or a C-bonded heterohydrocarbon radical; Cp is unsubstituted or C1-C4-alkyl-substituted cyclopentadienyl; Y is a C-bonded chiral group which directs metals of metallation reagents into the ortho position; and Phos is a P-bonded P(III) substituent. The compounds are chiral ligands for complexes of transition metals which are used as homogeneous catalysts in asymmetric syntheses.

    摘要翻译： 式I化合物为对映体纯的非对映体形式或非对映异构体（I）的混合物，其中基团R 1相同或不同并且各自为C 1 -C 4 - 烷基; m为0或1〜3的整数; n为0或1至4的整数; R2是烃基或C键合的杂烃基; Cp是未取代的或C 1 -C 4烷基取代的环戊二烯基; Y是将金属化试剂的金属引导到邻位的C-键合手性基团; Phos是P键合的P（III）取代基。 这些化合物是用于不对称合成中的均相催化剂的过渡金属络合物的手性配体。

    Tetradentate Ferrocene Ligands And Their Use
    9.
    发明申请
    Tetradentate Ferrocene Ligands And Their Use 审中-公开

    公开(公告)号：US20080076937A1

    公开(公告)日：2008-03-27

    申请号：US11631687

    申请日：2005-07-04

    申请人： Benoit Pugin ,  Xaing Dong Feng ,  Marc Thommen

    发明人： Benoit Pugin ,  Xaing Dong Feng ,  Marc Thommen

    IPC分类号： C07F17/02

    CPC分类号： C07F17/02

    摘要： Compounds of the formula (I) in the form of racemates, mixtures of diastereomers or pure diastereomers, where RO and Roo are each, independently of one another, hydrogen, C1-C20-alkyl, C3-C8-cycloalkyl, C6-C14-aryl or C3-C12-heteroaryl having heteroatoms selected from the group consisting of O, S and N, which are unsubstituted or substituted by C1-C6-alkyl, C1-C6-alkoxy, C5-C8-cycloalkyl, C5-C8-cycloalkoxy, phenyl, C1-C6-alkylphenyl, C1-C6-alkoxyphenyl, C3-C8-heteroaryl, F or trifluoromethyl; the radicals R1 are each, independently of one another, a hydrogen atom, a halogen atom or a substituent bound to the cyclopentadienyl rings via a C atom, S atom, Si atom, a P(O) or P(S) group; R2 and R02 are each, independently of one another, a hydrogen atom, C1-C20-alkyl, C3-C8-cycloalkyl, C6-C14-aryl or C3-C12-heteroaryl having heteroatoms selected from the group consisting of O, S and N, which are unsubstituted or substituted by C1-C6-alkyl, C1-C6-alkoxy, C5-C8-cycloalkyl, C5-C8-cycloalkoxy, phenyl, C1-C6-alkylphenyl, C1-C6-alkoxyphenyl, C3-C8-heteroaryl, F or trifluoromethyl; the two indices m are each, independently of one another, 1, 2 or 3; n is 0 or 1; X1 is a secondary phosphine group or a cyclic phosphonite group, and X2 and X3 are each, independently of one another, a secondary phosphine group. The compounds of the formula (I) are valuable ligands for enantioselective catalysts for the hydrogenation of prochiral, unsaturated compounds.

    Porphyrin derivatives and their use in photodynamic therapy
    10.
    发明授权
    Porphyrin derivatives and their use in photodynamic therapy 有权
    卟啉衍生物及其在光动力疗法中的应用

    公开(公告)号：US07244841B2

    公开(公告)日：2007-07-17

    申请号：US10744863

    申请日：2003-12-23

    申请人： William Love ,  Derek Brundish ,  William Rhys-Williams ,  Xiang Dong Feng ,  Benoit Pugin

    发明人： William Love ,  Derek Brundish ,  William Rhys-Williams ,  Xiang Dong Feng ,  Benoit Pugin

    IPC分类号： C07B47/00 ,  C07D487/22

    CPC分类号： C07D487/22

    摘要： A compound of formula I: wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4 and Z have meanings given in the description, and metallated forms of such compounds, which are useful in the treatment of medical conditions for which a photodynamic compound is indicated. Pharmaceutical formulations and methods of treatment of a medical condition for which a photodynamic agent is indicated are also disclosed. Sterilizing solutions comprising a compound of the invention, and the use thereof, are also disclosed.

    摘要翻译： 式I的化合物：其中X 1，X 2，X 3，X 4，Y，SUB Y 1，Y 3，Y 3，Y 4和Z具有在说明书中给出的含义，并且这样的金属化形式 化合物，其可用于治疗其中指示光动力学化合物的医学病症。 还公开了治疗指示光动力剂的医疗状况的药物制剂和方法。 还公开了包含本发明化合物的灭菌溶液及其用途。