公开(公告)号：US07795438B2

公开(公告)日：2010-09-14

申请号：US10580908

申请日：2005-04-27

申请人： Akio Imai ,  Hiroshi Nishimura

发明人： Akio Imai ,  Hiroshi Nishimura

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。

公开(公告)号：US20090171094A1

公开(公告)日：2009-07-02

申请号：US11994494

申请日：2006-07-12

申请人： Kazuhide Ashizawa ,  Akio Imai

发明人： Kazuhide Ashizawa ,  Akio Imai

IPC分类号： C07D211/32

CPC分类号： C07D211/32

摘要： 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine p-toluenesulfonate or a solvate thereof.

摘要翻译： 1-苄基-4 - [（5,6-二甲氧基-1-茚满酮）-2-基]甲基哌啶对甲苯磺酸盐或其溶剂合物。

公开(公告)号：US20080306272A1

公开(公告)日：2008-12-11

申请号：US12121454

申请日：2008-05-15

申请人： Naoyuki Shimomura ,  Seiji Yoshikawa ,  Yoshihiko Hisatake ,  Akio Imai

发明人： Naoyuki Shimomura ,  Seiji Yoshikawa ,  Yoshihiko Hisatake ,  Akio Imai

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。

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。

公开(公告)号：US06187883B1

公开(公告)日：2001-02-13

申请号：US08910830

申请日：1997-08-13

申请人： Makoto Satoh ,  Teruyoshi Kiyota ,  Akio Imai

发明人： Makoto Satoh ,  Teruyoshi Kiyota ,  Akio Imai

IPC分类号： C08F444

CPC分类号： C08F10/00 ,  C08F110/06 ,  Y10S526/908 ,  C08F4/6565 ,  C08F2500/17 ,  C08F2500/18

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。

公开(公告)号：US5854164A

公开(公告)日：1998-12-29

申请号：US731439

申请日：1996-10-15

申请人： Hiroyuki Shiraishi ,  Eiji Nakaishi ,  Takahiro Hino ,  Akio Imai

发明人： Hiroyuki Shiraishi ,  Eiji Nakaishi ,  Takahiro Hino ,  Akio Imai

IPC分类号： C08F4/651 ,  C08F4/653 ,  C08F4/654 ,  C08F10/00 ,  C08F210/16

CPC分类号： C08F10/00 ,  C08F210/16

摘要： A solid catalyst component (A) for olefin polymerization comprising Mg, Ti, a halogen and a cyclic organic nitrogen compound (C), a solid catalyst comprising the solid catalyst component and an organoaluminum compound, and a process for producing an olefin polymer with the catalyst. According to the present invention, there can be provided an olefin polymerization catalyst having a high catalyst activity per titanium enough to make the removal of catalyst residues unnecessary and a process for producing an olefin polymer having a low content of low molecular weight component with the catalyst.

摘要翻译： 包含Mg，Ti，卤素和环状有机氮化合物（C）的固体催化剂组分（A），包含固体催化剂组分和有机铝化合物的固体催化剂，以及烯烃聚合物的制备方法 催化剂。 根据本发明，可以提供一种对每个钛具有高催化活性的烯烃聚合催化剂，足以使催化剂残留物不必要地除去，以及用催化剂制备低含量低分子量组分的烯烃聚合物的方法 。

公开(公告)号：US5219938A

公开(公告)日：1993-06-15

申请号：US848095

申请日：1992-03-09

申请人： Akio Imai ,  Tomoaki Seki ,  Keisaku Yamamoto

发明人： Akio Imai ,  Tomoaki Seki ,  Keisaku Yamamoto

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。

公开(公告)号：US4981760A

公开(公告)日：1991-01-01

申请号：US378000

申请日：1989-07-11

申请人： Yukio Naito ,  Kohzoh Miyazaki ,  Yuji Gotoh ,  Masashi Hamba ,  Akio Imai ,  Kiyoyuki Sugimori

发明人： Yukio Naito ,  Kohzoh Miyazaki ,  Yuji Gotoh ,  Masashi Hamba ,  Akio Imai ,  Kiyoyuki Sugimori

IPC分类号： B32B27/32 ,  C08F10/00 ,  C08F110/02 ,  C08F210/02 ,  C08F210/16 ,  C08F297/08 ,  C08J5/18 ,  C08L23/00 ,  C08L23/06 ,  C08L23/08

CPC分类号： C08J5/18 ,  C08F210/02 ,  C08F210/16 ,  C08F297/08 ,  C08L23/0815 ,  C08F110/02 ,  C08J2323/08 ,  C08L23/06 ,  Y10T428/31855 ,  Y10T428/31938

摘要： An ethylene-.alpha.-olefin copolymer comprising ethylene and an .alpha.-olefin having from 3 to 10 carbon atoms, the copolymer having an .alpha.-olefin content of from 1.0 to 8.0 mol %, a density of from 0.900 to 0.930 g/cm.sup.3, and a melt flow rate of from 0.1 to 100 g/10 min., the programed-temperature thermogram of said copolymer as determined with a differential scanning calorimeter after being completely melted and then gradually cooled showing an endothermic peak (a) in a range of from 75.degree. to 100.degree. C. and an endothermic peak (b) in a range of from 120.degree. to 140.degree. C., with the ratio of an endotherm at the endothermic peak (b), .DELTA.Hb, to an endotherm at the endothermic peak (a), .DELTA.Ha, i.e., .DELTA.Hb/.DELTA.Ha, being from 0.03 to 2.0. The copolymer provides a film exhibiting excellent physical properties required for packaging film.

公开(公告)号：US4957976A

公开(公告)日：1990-09-18

申请号：US415380

申请日：1989-09-29

申请人： Hiroyoshi Takao ,  Akio Imai ,  Tomoski Seki ,  Mitsuji Tsuji

发明人： Hiroyoshi Takao ,  Akio Imai ,  Tomoski Seki ,  Mitsuji Tsuji

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。

公开(公告)号：US4743652A

公开(公告)日：1988-05-10

申请号：US5400

申请日：1987-02-02

申请人： Nobuyuki Yoshida ,  Yasushi Okamoto ,  Akio Imai ,  Tomoaki Seki ,  Hiroshi Furukawa ,  Yuichi Saito

发明人： Nobuyuki Yoshida ,  Yasushi Okamoto ,  Akio Imai ,  Tomoaki Seki ,  Hiroshi Furukawa ,  Yuichi Saito

IPC分类号： C08F236/00 ,  C08C19/30 ,  C08C19/44 ,  C08F8/00 ,  C08F212/00 ,  C08F212/06 ,  C08F236/10 ,  C08F8/42

CPC分类号： C08C19/44

摘要： An elastomeric copolymer of an aromatic vinyl compound and butadiene prepared by a solution polymerization method, which has a glass transition temperature of not less than -50.degree. C. and contains polymer chains modified with a trifunctional or tetrafunctional coupling agent, and which contains not less than 3% by weight to less than 23% by weight, based on the whole polymer chains, of polymer chains having a molecular weight of at least 5 times a molecular weight corresponding to a peak appearing on the low molecular weight side of a high performance liquid chromatogram of the elastomeric copolymer. The elastomeric copolymer has an excellent processability and shows a low rolling resistance and a high wet grip characteristic when used as a rubber component in tires.

摘要翻译： 通过溶液聚合法制备的芳族乙烯基化合物和丁二烯的弹性体共聚物，其具有不低于-50℃的玻璃化转变温度，并且包含用三官能或四官能偶联剂改性的聚合物链，并且不少于 基于整个聚合物链，分子量至少为分子量的5倍的聚合物链的3重量％至小于23重量％，该分子量对应于高性能的低分子量侧上出现的峰 弹性共聚物的液相色谱图。 弹性体共聚物在轮胎中用作橡胶组分时具有优异的加工性能，并且具有低滚动阻力和高湿抓地性能。