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12 条记录 (耗时 0.02 秒)

    Process for the preparation of indole derivatives
    3.
    发明申请
    Process for the preparation of indole derivatives 审中-公开
    吲哚衍生物的制备方法

    公开(公告)号：US20050032875A1

    公开(公告)日：2005-02-10

    申请号：US10487269

    申请日：2002-08-13

    申请人： Heinz Wolleb ,  Annemarie Wolleb ,  Paul Van Der Schaaf ,  Roman Kolly ,  Nicole End

    发明人： Heinz Wolleb ,  Annemarie Wolleb ,  Paul Van Der Schaaf ,  Roman Kolly ,  Nicole End

    IPC分类号： C07D209/12 ,  B01J31/18 ,  B01J31/24 ,  C07D209/24 ,  C07D319/06 ,  C07D405/06 ,  C07F5/02 ,  A61K31/405

    CPC分类号： C07D405/06 ,  C07D209/24 ,  C07D319/06 ,  C07F5/025 ,  Y02P20/55

    摘要： A process for the preparation of compounds of formula (I) wherein R1 is unsubstituted or substituted C1-C8alkyl, R2, R3, R4 and R5 are each independently of the others hydrogen, unsubstituted or substituted C1-C8alkyl, C1-C8 alkoxy, phenoxy or benzyloxy, or halogen, Y1 and Y2 are each independently of the other hydrogen or a protecting group, or Y1 and Y2 together form a protecting bridge, and X1 is hydrogen, an organic radical or a cation, in which process a compound of formula (II) wherein R1 R2, R3, R4 and R5 are as defined above and Z1 is a leaving group, is reacted, in the presence of a catalytically effective amount of a palladium catalyst, with a compound of formula (III) wherein R6 is hydrogen, bromine, chlorine, iodine, —OSO2CF3, —COCI, —B(OH)2 or a mono- or di-ester derived from —B(OH)2, Y3 and Y4 are each a protecting group, or Y3 and Y4 together form a protecting bridge, and X1 is as defined above, to form a compound of formula (IV) and if desired the radicals Y3 and Y4 are converted into the radicals Y1 and Y2 where Y1 and Y2 are hydrogen.

    摘要翻译： 制备其中R 1为未取代或取代的C 1 -C 8烷基，R 2，R 3，R 4和R 5的式（I）化合物的方法各自独立地为氢，未取代或取代的C 1 -C 8烷基，C 1 -C 8烷氧基，苯氧基 或苄氧基或卤素，Y1和Y2各自独立地为另一个氢或保护基，或Y1和Y2一起形成保护桥，并且X 1是氢，有机基团或阳离子，其中式 （II）其中R1 R2，R3，R4和R5如上定义，Z1是离去基团，在催化有效量的钯催化剂存在下，与式（III）化合物反应，其中R 6是 氢，溴，氯，碘，-OSO 2 CF 3，-COCI，-B（OH）2或衍生自-B（OH）2，Y 3和Y 4的单酯或二酯各自为保护基，或Y 3和Y 4 一起形成保护桥，X1如上所定义，形成式（IV）的化合物，如果需要，基团Y 3和Y 4是 转化为Y1和Y2基团，其中Y1和Y2是氢。

    Phenolic antioxidants in crystalline form
    4.
    发明申请
    Phenolic antioxidants in crystalline form 失效
    酚类抗氧化剂呈结晶状

    公开(公告)号：US20060189820A1

    公开(公告)日：2006-08-24

    申请号：US10534513

    申请日：2003-11-17

    申请人： Daniel Rehm ,  Johannes Schafter ,  Paul Van Der Schaaf ,  Christian Guckel

    发明人： Daniel Rehm ,  Johannes Schafter ,  Paul Van Der Schaaf ,  Christian Guckel

    IPC分类号： C07C69/88 ,  C07C237/32

    CPC分类号： C07C231/22 ,  C07C67/52 ,  C07C69/732 ,  C07C231/24 ,  C08K5/13 ,  C08K5/20 ,  C08K2201/005 ,  C07C235/34

    摘要： The invention relates to a process for preparing solid particles of a phenolic antioxidant from the IRGANOX series in the form of crystals, particularly IRGANOX 1010 and 1098, the crystal particles obtainable by the process, the further processing of the crystal particles, an aqueous dispersion comprising the phenolic antioxidant, novel crystal modifications of pentaerythritol tetrakis[3-(3,5-di-tert-butyl-4-hydroxyphenyl)-propionate] (μ-form) and N,N′-hexane-1,6diyl-bis[3-(3,5-di-tert-butyl-4-hydroxyphenylpropionamide)] (β-form) and aqueous dispersion comprising the new crystal modifications.

    摘要翻译： 本发明涉及一种以IRGANOX系列形式制备酚类抗氧化剂固体颗粒的方法，特别是IRGANOX 1010和1098，可通过该方法获得的结晶颗粒，晶体颗粒的进一步加工，含水分散体 酚类抗氧化剂，季戊四醇四[3-（3,5-二叔丁基-4-羟基苯基）丙酸酯]（μ-型）和N，N'-己烷-1,6-二基 - 双[ 3-（3,5-二叔丁基-4-羟基苯基丙酰胺）]（β型）和包含新的晶体改性的水分散体。

    Crystalline forms of pitavastatin calcium
    7.
    发明申请
    Crystalline forms of pitavastatin calcium 审中-公开
    匹伐他汀钙的结晶形式

    公开(公告)号：US20060142582A1

    公开(公告)日：2006-06-29

    申请号：US10544752

    申请日：2004-02-02

    申请人： Paul Van Der Schaaf ,  Fritz Blatter ,  Martin Szelagiewicz ,  Kai-Uwe Schoning

    发明人： Paul Van Der Schaaf ,  Fritz Blatter ,  Martin Szelagiewicz ,  Kai-Uwe Schoning

    IPC分类号： C07D215/16

    CPC分类号： C07D215/14 ,  C07B2200/13

    摘要： The present invention is directed to new crystalline forms of Pitavastatin hernicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous form.

    摘要翻译： 本发明涉及匹伐他汀鞣酸盐的新结晶形式，以下称为多晶型A，B，C，D，E和F，以及无定形形式。 此外，本发明涉及制备这些结晶形式的方法和包含这些结晶形式或无定形形式的无定型形式和药物组合物。

    Process for the synthesis of amine ethers from secondary amino oxides
    10.
    发明申请
    Process for the synthesis of amine ethers from secondary amino oxides 有权
    从仲氨基氧化物合成胺醚的方法

    公开(公告)号：US20050043552A1

    公开(公告)日：2005-02-24

    申请号：US10919776

    申请日：2004-08-17

    申请人： Andreas Hafner ,  Hans Kirner ,  Franz Schwarzenbach ,  Paul Van Der Schaaf ,  Peter Nesvadba

    发明人： Andreas Hafner ,  Hans Kirner ,  Franz Schwarzenbach ,  Paul Van Der Schaaf ,  Peter Nesvadba

    IPC分类号： B01J27/122 ,  C07B61/00 ,  C07D209/44 ,  C07D211/94 ,  C07D217/26 ,  C07D241/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C08F4/00 ,  C08K5/3412 ,  C08K5/3435 ,  C08L101/00 ,  C09K15/30 ,  C09K21/10 ,  C07D303/08 ,  C07C239/10

    CPC分类号： C07D401/14 ,  C04B35/632 ,  C07D209/44 ,  C07D211/94 ,  C07D217/26 ,  C07D241/08 ,  C07D401/12 ,  C07D405/12 ,  C08K5/3412

    摘要： An amine ether of formula A wherein a is 1 or 2; and when a is 1, E is E′; when a is 2, E is L; E′ is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cydoalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or tricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15 aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E′ is a radical of formula (VII) as explained in claim 1; T′ is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)—R22; or T′ is C5-C12cycloalkyl; C5-C12 cycloalkyl which is interrupted by at least one O or —NR18—; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or —NR18—; or T′ is —C(G1)(G2)—T″; or C1-C18alkyl or C5-C12cycloalkyl substituted by T″ is hydrogen, halogen, NO2, cyano, or is a monovalent organic radical comprising 1-50 carbon atoms; or T″ and T′ together form a divalent organic linking group completing, together with the hindered amine nitrogen atom and the quaternary carbon atom substituted by G1 and G2, an optionally substituted five- or six-membered ring structure; and all other residues are as defined in claim 1, are obtained in good yield from the corresponding N-oxyl hindered amine precursor by reaction with a hydrocarbon E1—H or H—L—H in the presence of an organic hydroperoxide and a catalytic amount of copper or a copper compound. The products of present process find utility as polymerization regulators and/or light stabilizers for organic material.

    摘要翻译： 式A的胺醚，其中a为1或2; 当a为1时，E为E'; 当a为2时，E为L; E'是C 1 -C 36烷基; C3-C18烯基; C2-C18炔基; C5-C18环烷基; C5-C18环烯基; 7-12个碳原子的饱和或不饱和脂族二环或三环烃基团; C 2 -C 7烷基或被卤素取代的C 3 -C 7链烯基; 被C 1 -C 4烷基或苯基取代的C 7 -C 15芳烷基或C 7 -C 15芳烷基; 或E'是如权利要求1所述的式（VII）的基团; T'是叔C4-C18烷基或苯基，其各自为未取代的或被卤素，OH，COOR21或C（O）-R22取代; 或T'为C 5 -C 12环烷基; 被至少一个O或-NR 18 - 中断的C 5 -C 12环烷基; 具有7-18个碳原子的多环烷基或被至少一个O或-NR 18 - 中断的相同基团; 或T'为-C（G1）（G2）-T“; 或被T“取代的C 1 -C 18烷基或C 5 -C 12环烷基是氢，卤素，NO 2，氰基，或是包含1-50个碳原子的一价有机基团; 或T“和T'一起形成二价有机连接基团，与受阻胺氮原子和被G1和G2取代的季碳原子一起形成任选取代的五元或六元环结构; 并且所有其它残基如权利要求1中所定义，通过在有机氢过氧化物和催化量的铜或其盐的存在下与烃E1-H或HLH反应，由相应的N-氧基受阻胺前体以良好的产率获得 铜化合物。 本发明的产品可用作有机材料的聚合调节剂和/或光稳定剂。