Processes for producing 1-benzyl-4-[(5,6-dimethoxy-1indanon)-2-yl]methylpiperidine and hydrochloride
    3.
    发明授权
    Processes for producing 1-benzyl-4-[(5,6-dimethoxy-1indanon)-2-yl]methylpiperidine and hydrochloride 有权
    1-苄基-4 - [(5,6-二甲氧基-1茚满酮)-2-基]甲基哌啶和盐酸盐的制备方法

    公开(公告)号:US07795438B2

    公开(公告)日:2010-09-14

    申请号:US10580908

    申请日:2005-04-27

    IPC分类号: C07D211/32

    CPC分类号: C07D211/32 B01J25/02

    摘要: Processes for preparing 1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-yl]methylpiperidine (donepezil), which is useful as an intermediate for medicines, and for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride (donepezil hydrochloride), which is useful as a medicine. The process for donepezil hydrochloride production comprises catalytically hydrogenating the compound represented by the structural formula (III) [1-benzyl-4-[(5,6-dimethoxy-lindanon)-2-ylidene]methylpiperidine] with a Raney nickel catalyst under mild conditions and subsequently treating it with hydrochloric acid. Thus, impurities are further diminished. The operations are simple and the process is suitable for industrial production.

    摘要翻译: 用于制备1-苄基-4 - [(5,6-二甲氧基 - 茚满酮)-2-基]甲基哌啶(多奈哌齐)的方法,其可用作药物的中间体,并用于制备1-苄基-4 - [(5 ,6-二甲氧基-1-茚满酮)-2-基]甲基哌啶盐酸盐(盐酸多奈哌齐),其可用作药物。 盐酸多奈哌齐的方法包括用温和的阮内镍催化剂催化氢化由结构式(III)[1-苄基-4 - [(5,6-二甲氧基 - 茚满酮)-2-亚基]甲基哌啶]代表的化合物 然后用盐酸处理。 因此,杂质进一步减少。 操作简单,适用于工业生产。

    ONE-POT METHODS FOR PREPARING CINNAMIDE DERIVATIVES
    4.
    发明申请
    ONE-POT METHODS FOR PREPARING CINNAMIDE DERIVATIVES 审中-公开
    用于制备氰化物衍生物的一种方法

    公开(公告)号:US20080306272A1

    公开(公告)日:2008-12-11

    申请号:US12121454

    申请日:2008-05-15

    IPC分类号: C07D401/02

    CPC分类号: C07D401/10 Y02P20/55

    摘要: A compound represented by the following formula (1): wherein R represents a 4-fluorophenyl group and the like; Q represents —CH(CH3)— and the like; and n represents 1 and the like and a pharmaceutically acceptable salt thereof can be prepared in one-pot by reacting a compound represented by the following formula (2): wherein R1 represents a 4-fluorophenyl group and the like; and Q and n have the same meaning as described above, with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base and, if necessary, removing a protecting group.

    摘要翻译: 由下式(1)表示的化合物:其中R表示4-氟苯基等; Q表示-CH(CH 3) - 等; 和n表示1等的化合物及其药学上可接受的盐可以通过使由下式(2)表示的化合物反应而制备:其中R1表示4-氟苯基等; 和Q和n具有与上述相同的含义,与3-甲氧基-4-(4-甲基-1H-咪唑-1-基)苯甲醛在碱存在下反应,如果需要,除去保护基。

    Process for producing 1-benzyl-4-[ (5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine or hydrochloride thereof
    5.
    发明申请
    Process for producing 1-benzyl-4-[ (5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine or hydrochloride thereof 失效
    1-苄基-4 - [(5,6-二甲氧基-1-茚满酮)-2-基]甲基哌啶或其盐酸盐的制备方法

    公开(公告)号:US20070088055A1

    公开(公告)日:2007-04-19

    申请号:US11546444

    申请日:2006-10-12

    申请人: Akio Imai

    发明人: Akio Imai

    IPC分类号: C07D211/06 A61K31/445

    CPC分类号: C07D211/32

    摘要: 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine or hydrochloride thereof, which is useful as a drug, can be produced in high purity by safer and easier operations suitable for industrial production by subjecting 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methyl-piperidine or a solvate thereof to catalytic hydrogenation in the presence of a palladium-alumina catalyst and if necessary, converting the thus obtained compound to its hydrochloride.

    摘要翻译: 可用作药物的1-苄基-4 - [(5,6-二甲氧基-1-茚满酮)-2-基]甲基哌啶或其盐酸盐可以通过适合于工业生产的更安全和更容易的操作而以高纯度制备 通过在钯 - 氧化铝催化剂的存在下使1-苄基-4 - [(5,6-二甲氧基-1-茚满酮)-2-亚基]甲基 - 哌啶或其溶剂合物进行催化氢化,如果需要, 从而得到化合物至其盐酸盐。

    Solid catalyst component for &agr;-olefin polymerization, catalyst for &agr;-olefin polymerization, and process for producing &agr;-olefin polymer
    6.
    发明授权
    Solid catalyst component for &agr;-olefin polymerization, catalyst for &agr;-olefin polymerization, and process for producing &agr;-olefin polymer 失效
    用于α-烯烃聚合的固体催化剂组分,用于α-烯烃聚合的催化剂和用于生产α-烯烃聚合物的方法

    公开(公告)号:US06187883B1

    公开(公告)日:2001-02-13

    申请号:US08910830

    申请日:1997-08-13

    IPC分类号: C08F444

    摘要: The present invention relates to a solid catalyst component for &agr;-olefin polymerization having a narrow particle size distribution of not less than 6.0 in terms of the value of N in a Rosin-Rammler function of particle size distribution and giving a catalytic activity of not less than 10,000 ((g-polymer produced/g-solid catalyst component)/hour) in polymerization. The catalyst component is obtained by a process which comprises reducing a titanium compound with an organomagnesium compound in the presence of an organosilicon compound and an ester to obtain a solid product, then treating the solid product with: (a) a mixture of titanium tetrachloride and an ether, (b) an organic acid halide, and (c) a mixture of titanium tetrachloride and an ether optionally containing an ester.

    摘要翻译: 本发明涉及一种用于α-烯烃聚合的固体催化剂组分,其具有窄的粒度分布,在松散Rammler的粒度分布函数中的N值不小于6.0,并且给出的催化活性不低于 ((g-聚合物生产/ g-固体催化剂组分)/小时)。 催化剂组分通过包括在有机硅化合物和酯存在下还原钛化合物以获得固体产物的方法获得,然后用以下物质处理固体产物:(a)四氯化钛和 醚,(b)有机酰卤,和(c)任选含有酯的四氯化钛和醚的混合物。

    Modified diene polymer rubbers
    8.
    发明授权
    Modified diene polymer rubbers 失效
    改性二烯聚合物橡胶

    公开(公告)号:US5219938A

    公开(公告)日:1993-06-15

    申请号:US848095

    申请日:1992-03-09

    IPC分类号: B60C1/00 C08C19/42

    CPC分类号: B60C1/0016 C08C19/42

    摘要: A process for preparing modified diene polymer rubbers having an increased impact resilience, a reduced hardness at low temperatures and an improved processability, and useful as rubber materials for automobile tires and other industries which comprises producing a conjugated diene polymer having alkali metal end or ends, and reacting the alkali metal-containing polymer with (a) a silicon or tin compound of the formula: R.sub.a MX.sub.b wherein R is an alkyl group, an alkenyl group, a cycloalkenyl group or an aromatic hydrocarbon atom, a is 0, 1 or 2 and b is 2, 3 or 4, and (b) at least one member selected from the group consisting of a nitro compound; a phosphoryl chloride compound of the formula (1): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are an alkyl group; an aminosilane compound of the formula (2): ##STR2## wherein R.sup.5, R.sup.6 and R.sup.7 are an alkyl group or an alkoxyl group, R.sup.8 and R.sup.9 are an alkyl group, and n is an integer; an acrylamide compound of the formula (3): ##STR3## wherein R.sup.10 is hydrogen atom or methyl group, R.sup.11 and R.sup.12 are an alkyl group, and m is an integer; and an aminovinylsilane compound of the formula (4): ##STR4## wherein R.sup.13, R.sup.14, R.sup.15, R.sup.16 and R.sup.17 are an alkyl group.

    摘要翻译: 一种制备具有增加的冲击弹性,在低温下降低的硬度和改善加工性能的改性二烯聚合物橡胶的方法,并且可用作汽车轮胎和其它工业的橡胶材料,其包括制备具有碱金属末端或末端的共轭二烯聚合物, 并使含碱金属的聚合物与(a)下式的硅或锡化合物:其中R是烷基,烯基,环烯基或芳族烃原子,其中R是一个或多个, b是2,3或4,和(b)至少一种选自硝基化合物; 式(1)的磷酰氯化合物:其中R1,R2,R3和R4是烷基; (2)的氨基硅烷化合物:其中R5,R6和R7是烷基或烷氧基,R8和R9是烷基,n是整数; 式(3)的丙烯酰胺化合物:其中R 10是氢原子或甲基,R 11和R 12是烷基,m是整数; 和式(4)的氨基乙烯基硅烷化合物:其中R 13,R 14,R 15,R 16和R 17是烷基。

    Process for preparing diene polymer rubbers
    10.
    发明授权
    Process for preparing diene polymer rubbers 失效
    二烯聚合物橡胶的制备方法

    公开(公告)号:US4957976A

    公开(公告)日:1990-09-18

    申请号:US415380

    申请日:1989-09-29

    IPC分类号: C08C19/42

    CPC分类号: C08C19/42

    摘要: A process for preparing modified diene polymer rubbers having an increased impact resilience and a reduced hardness at low temperatures and useful as rubber materials for automobile tires and other industries which comprises producing an alkali metal-containing conjugated diene polymer, and reacting the alkali metal-containing polymer with a modifier selected from the group consisting of a nitro compound, a phosphoryl chloride compound of the formula: ##STR1## wherein R.sup.1 to R.sup.4 are independently an alkyl group, and an aminosilane compound of the formula: ##STR2## wherein R.sup.5 to R.sup.7 are independently an alkyl group or an alkoxyl group, R.sup.8 and R.sup.9 are independently an alkyl group, and n is an integer, said alkali metal-containing diene polymer being prepared by a living anionic polymerization using an alkali metal-based catalyst or by an addition reaction of a diene polymer having conjugated diene units and an alkali metal-based catalyst in a hydrocarbon solvent. The modified diene polymers can be incorporated with usual rubber additives to provide rubber compositions for various purposes, and the cured products shown an increased impact resilience and a reduced hardness at low temperatures.

    摘要翻译: 一种制备改性二烯聚合物橡胶的方法,该改性二烯聚合物橡胶在低温下具有增加的冲击弹性和降低的硬度,并且可用作汽车轮胎和其它工业的橡胶材料,其包括制备含碱金属的共轭二烯聚合物,并使含碱金属的 聚合物,其选自硝基化合物,下式的磷酰氯化合物:其中R 1至R 4独立地为烷基,并且具有下式的氨基硅烷化合物:(IMAGE)( 2)其中R5至R7独立地为烷基或烷氧基,R8和R9独立地为烷基,n为整数,所述含碱金属的二烯聚合物通过使用碱金属 - 或通过在烃溶剂中具有共轭二烯单元的二烯聚合物和碱金属类催化剂的加成反应。 改性二烯聚合物可与通常的橡胶添加剂结合以提供用于各种目的的橡胶组合物,并且固化产物显示了在低温下增加的冲击弹性和降低的硬度。