利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

32 条记录 (耗时 0.025 秒)

    Process for preparation of erythromycin compounds
    1.
    发明授权
    Process for preparation of erythromycin compounds 失效
    红霉素化合物的制备方法

    公开(公告)号：US06906039B2

    公开(公告)日：2005-06-14

    申请号：US10480275

    申请日：2002-06-12

    申请人： Hiroyuki Miyata ,  Akira Takama ,  Yasuhito Yamamoto ,  Kikuo Ataka

    发明人： Hiroyuki Miyata ,  Akira Takama ,  Yasuhito Yamamoto ,  Kikuo Ataka

    IPC分类号： C07H17/08 ,  A61K31/7048 ,  A61K31/70

    CPC分类号： C07H17/08

    摘要： The present invention is to provide a process for producing a 2′-O-acetyl-4″-O-formyl-8,9-anhydroerythromycin A 6,9-hemiketal compound 4, and it provide a process for producing an erythromycin compound which comprises reacting a formylating agent with a 2′-O-acetylerythromycin A compound 2 to obtain 2′-O-acetyl-4″-O-formylerythromycin A compound 3, then, acting an acid on Compound 3 to subject to hemiketalation, and then adding an aqueous basic solution in an aqueous solution to precipitate Compound 4 as free crystals.

    摘要翻译： 本发明提供一种制备2'-O-乙酰基-4'-O-甲酰基-8,9-脱水红霉素A 6,9-半缩酮化合物 4的方法， 提供一种生产红霉素化合物的方法，其包括使甲酰化试剂与2'-O-乙酰红霉素A化合物 2反应，得到2'-O-乙酰基-4'-O-甲酰基红霉素A 化合物 3，然后在化合物 3上加入酸，进行半辛化，然后在水溶液中加入碱性水溶液沉淀化合物 4作为自由晶体。

    2-silyloxy-tetrahydrothienopyridine, salt thereof and process for preparing the same
    2.
    发明授权
    2-silyloxy-tetrahydrothienopyridine, salt thereof and process for preparing the same 失效
    2-甲基氧基 - 四氢噻吩并吡啶及其盐及其制备方法

    公开(公告)号：US5874581A

    公开(公告)日：1999-02-23

    申请号：US817001

    申请日：1997-03-31

    申请人： Kikuo Ataka ,  Hiroyuki Miyata ,  Masahiko Kohno ,  Naoyuki Yokota ,  Yasuhito Yamamoto

    发明人： Kikuo Ataka ,  Hiroyuki Miyata ,  Masahiko Kohno ,  Naoyuki Yokota ,  Yasuhito Yamamoto

    IPC分类号： C07F7/18 ,  C07D471/04

    CPC分类号： C07F7/1856

    摘要： A 2-silyloxy-4,5,6,7-tetrahydrothieno�3,2-c!pyridine represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represent an alkyl group having 1 to 10 carbon atoms or an aryl group,and a salt thereof and a process for preparing the same, and a 5-alkyl-2-silyloxy-4,5,6,7-tetrahydrothieno�3,2-c!-pyridine represented by the formula (IV): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 represent the same meanings as described above; R.sup.4 represents a hydrogen atom, an alkoxycarbonyl group having 2 to 10 carbon atoms, an acyl group having 2 to 10 carbon atoms or a cyclo-alkylcarbonyl group having 4 to 10 carbon atoms; andR.sup.5 represents a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms,which is useful as a synthetic intermediate of an antiplatelet medicine and an elastase inhibitor, etc., and a process for preparing the same.

    摘要翻译： PCT No.PCT / JP95 / 02023 Sec。 371日期1997年3月31日 102（e）1997年3月31日PCT PCT 1995年10月4日PCT公布。 公开号WO96 / 11203 日期：1996年4月18日由式（I）表示的2-甲硅烷氧基-4,5,6,7-四氢噻吩并[3,2-c]吡啶：其中R 1，R 2和R 3各自独立地表示 具有1-10个碳原子的烷基或芳基，及其盐及其制备方法，和5-烷基-2-甲硅烷氧基-4,5,6,7-四氢噻吩并[3,2- （IV）表示的c]吡啶：其中R 1，R 2和R 3表示与上述相同的含义; R 4表示氢原子，碳原子数2〜10的烷氧基羰基，碳原子数2〜10的酰基或碳原子数4〜10的环烷基羰基。 R5表示卤素原子，碳原子数1〜4的烷基或碳原子数1〜4的烷氧基，可用作抗血小板药和弹性蛋白酶抑制剂的合成中间体等， 准备一样

    7a-alkoxy-4H-pyrano[3,2-d]-oxazol-2(3H)-one and process for producing the same
    3.
    发明授权
    7a-alkoxy-4H-pyrano[3,2-d]-oxazol-2(3H)-one and process for producing the same 失效
    7a-烷氧基-4H-吡喃并[3,2-d] - 恶唑-2（3H） - 酮及其制备方法

    公开(公告)号：US06723860B2

    公开(公告)日：2004-04-20

    申请号：US09988042

    申请日：2001-11-16

    申请人： Hiroyuki Miyata ,  Takashi Honma ,  Yasuhito Yamamoto ,  Kikuo Ataka

    发明人： Hiroyuki Miyata ,  Takashi Honma ,  Yasuhito Yamamoto ,  Kikuo Ataka

    IPC分类号： C07D49504

    CPC分类号： C07D498/04

    摘要： The present invention provides a novel 7a-alkoxy-4H-pyrano-[3,2-d]-oxazol-2(3H)-one represented by the formula (I): wherein R1 and R2 each represent a hydrogen atom, an alkyl group, an alkenyl group, an aryl group or an aralkyl group; R3 represents an alkyl group, a cyclo-alkyl group, an alkenyl group, an aryl group or an aralkyl group, provided that a 2-alkenyl group is excluded from the alkenyl group of R3; and R4 represents an alkyl group, an aryl group, an alkoxycarbonyl group or a cyano group, and a process for producing the same which comprises reacting 5-alkoxy-2(3H)-oxazolone with an &agr;,&bgr;-unsaturated ketone in the presence of a Lewis acid in a solvent.

    摘要翻译： 本发明提供由式（I）表示的新的7a-烷氧基-4H-吡喃并[3,2-d]恶唑-2（3H） - 酮：其中R 1和R 2各自代表 氢原子，烷基，烯基，芳基或芳烷基; R 3表示烷基，环烷基，烯基，芳基或芳烷基，条件是从R 3的烯基中排除2-烯基; 和R 4代表烷基，芳基，烷氧基羰基或氰基，及其制备方法，其包括使5-烷氧基-2（3H） - 恶唑酮与α，β-不饱和酮 在溶剂中存在路易斯酸。

    Trifluoro-substituted benzoic acid, esters thereof, and process for producing the same
    4.
    发明授权
    Trifluoro-substituted benzoic acid, esters thereof, and process for producing the same 失效
    三氟取代的苯甲酸及其酯，及其制备方法

    公开(公告)号：US6160171A

    公开(公告)日：2000-12-12

    申请号：US242441

    申请日：1999-02-17

    申请人： Yasuhito Yamamoto ,  Yasuhiro Yoneda ,  Kikuo Ataka ,  Naoyuki Yokota

    发明人： Yasuhito Yamamoto ,  Yasuhiro Yoneda ,  Kikuo Ataka ,  Naoyuki Yokota

    IPC分类号： C07C63/70 ,  C07C69/76 ,  C07C51/363

    CPC分类号： C07C69/76 ,  C07C63/70

    摘要： The present invention is to provide a trifluoro-substituted benzoic acid, an ester thereof, particularly 2,3,4-trifluoro-5-iodobenzoic acid, 2,3,4-trifluoro-5-trifluoromethylbenzoic acid, esters thereof, which are useful as a starting material for synthesizing a quinolonecarboxylic acid compound useful as a medicine, an anti-bacterial agent or an antiviral agent, and processes for preparing these compounds and 2,4,5-trifluoro-3-iodobenzoic acid, 2,4,5-trifluoro-3-trifluoromethylbenzoic acid and esters thereof.

    摘要翻译： PCT No.PCT / JP97 / 02856 Sec。 371日期1999年2月17日 102（e）1999年2月17日PCT PCT 1997年8月19日PCT公布。 出版物WO98 / 07682 日期：1998年2月26日本发明提供三氟取代的苯甲酸，其酯，特别是2,3,4-三氟-5-碘苯甲酸，2,3,4-三氟-5-三氟甲基苯甲酸，酯 可用作合成可用作药物的喹诺酮羧酸化合物的起始原料，抗菌剂或抗病毒剂，以及制备这些化合物和2,4,5-三氟-3-碘代苯甲酸的方法， 2,4,5-三氟-3-三氟甲基苯甲酸及其酯。

    Trifluoro-substituted benzoic acid, esters thereof and processes for preparing the same
    5.
    发明授权
    Trifluoro-substituted benzoic acid, esters thereof and processes for preparing the same 失效
    三氟取代的苯甲酸，其酯及其制备方法

    公开(公告)号：US06307091B1

    公开(公告)日：2001-10-23

    申请号：US09678694

    申请日：2000-10-03

    申请人： Yasuhito Yamamoto ,  Yasuhiro Yoneda ,  Kikuo Ataka ,  Naoyuki Yokota

    发明人： Yasuhito Yamamoto ,  Yasuhiro Yoneda ,  Kikuo Ataka ,  Naoyuki Yokota

    IPC分类号： C07C6308

    CPC分类号： C07C69/76 ,  C07C63/70

    摘要： The present invention is to provided a trifluoro-substituted benzoic acid, an ester thereof, particularly 2,3,4-trifluoro-5-iodobenzonic acid, 2,3,4-trifluoro-5-trifluoromethylbenzonic acid, esters thereof, which are useful as a starting material for synthesizeing a quinolonecarboxylic acid compound useful as a medicine, an anti-bacterial agent or an antiviral agent, and processes for preparing these compounds and 2,4,5-trifluoro-3-iodobenzonic acid, 2,4,5-trifluoro-3-trifluoromethylbenzoic acid and esters thereof.

    摘要翻译： 本发明提供三氟取代的苯甲酸，其酯，特别是2,3,4-三氟-5-碘苯甲酸，2,3,4-三氟-5-三氟甲基苯甲酸及其酯，它们是有用的 作为合成可用作药物的喹诺酮羧酸化合物的起始原料，抗菌剂或抗病毒剂，以及制备这些化合物的方法和2,4,5-三氟-3-碘苯甲酸，2,4,5 三氟-3-三氟甲基苯甲酸及其酯。

    Processes for preparing optically active (S or R)-β-amino acid and optically active (R or S)-β-amino acid ester, and β-amino acid 2-alkoxyethyl ester and optically active (S or R)-β amino acid 2-alkoxyethyl ester
    6.
    发明授权
    Processes for preparing optically active (S or R)-β-amino acid and optically active (R or S)-β-amino acid ester, and β-amino acid 2-alkoxyethyl ester and optically active (S or R)-β amino acid 2-alkoxyethyl ester 有权
    用于制备光学活性（S或R） - 氨基酸和光学活性（R或S） - 氨基酸酯和和 - 氨基酸2-烷氧基乙酯和光学活性（S或R） - ＆bgr 氨基酸2-烷氧基乙酯

    公开(公告)号：US07915019B2

    公开(公告)日：2011-03-29

    申请号：US11664878

    申请日：2005-10-11

    申请人： Tadayoshi Konegawa ,  Hiroyuki Miyata ,  Yasuhito Yamamoto

    发明人： Tadayoshi Konegawa ,  Hiroyuki Miyata ,  Yasuhito Yamamoto

    IPC分类号： C12P13/00 ,  C07B55/00

    CPC分类号： C12P41/005 ,  C07C227/18 ,  C07C229/34 ,  C12P13/04 ,  C12P13/222

    摘要： A process for preparing an optically active (S or R)-β-amino acid represented by formula (II): wherein R represents an alkyl group, alkenyl group, alkynyl group, cycloalkyl group, aralkyl group, aryl group or heteroaryl group each of which may have a substituent(s), and * represents an asymmetric carbon atom, and an optically active (R or S)-β-amino acid ester represented by formula (III): wherein R has the same meaning as defined above, R1 represents an alkyl group which may have a substituent(s), and * represents an asymmetric carbon atom, provided that it has a reverse absolute configuration to that of the compound of the formula (II), which comprises selectively hydrolyzing water and one of enantiomers of a β-amino acid ester represented by formula (I): wherein R and R1 have the same meanings as defined above, which is a racemic mixture, in the presence of a hydrolase in an organic solvent.

    摘要翻译： 一种制备由式（II）表示的光学活性（S或R） - 氨基酸的方法：其中R表示烷基，烯基，炔基，环烷基，芳烷基，芳基或杂芳基 其可以具有取代基，*表示不对称碳原子，以及由式（III）表示的光学活性（R或S） - （ - ） - 氨基酸酯：其中R具有与上述相同的含义 R 1表示可以具有取代基的烷基，*表示不对称碳原子，条件是其具有与式（II）化合物相反的绝对构型，其包括选择性水解水和一种 由式（I）表示的α-氨基酸酯的对映异构体：其中R和R 1具有与上述定义相同的含义，其是在有机溶剂中的水解酶存在下的外消旋混合物。

    PROCESS FOR PREPARING OPTICALLY ACTIVE (S OR R)-ALPHA-AMINO ACID AND OPTICALLY ACTIVE (R OR S)-ALPHA-AMINO ACID ESTER
    8.
    发明申请
    PROCESS FOR PREPARING OPTICALLY ACTIVE (S OR R)-ALPHA-AMINO ACID AND OPTICALLY ACTIVE (R OR S)-ALPHA-AMINO ACID ESTER 有权
    制备光学活性（S或R） - 氨基酸和光学活性（R或S） - 氨基 - 氨基酸酯的方法

    公开(公告)号：US20090042260A1

    公开(公告)日：2009-02-12

    申请号：US12064589

    申请日：2006-08-25

    申请人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa

    发明人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa

    IPC分类号： C12P13/04

    CPC分类号： C12P13/04 ,  C12P41/005

    摘要： The present invention discloses a process for preparing an optically active (S or R)-α-amino acid represented by the formula (II): wherein R represents an alkyl group, alkenyl group, alkynyl group, cycloalkyl group, aralkyl group, heteroarylalkyl group, aryl group or heteroaryl group, each of which may have a substituent(s), and * represents an asymmetric carbon atom, and an optically active (R or S)-α-amino acid ester represented by the formula (III): wherein R1 represents an alkyl group which may have a substituent(s), and * represents an asymmetric carbon atom, provided that it has an opposite absolute configuration to that of the compound of the formula (II), which comprises selectively reacting water with one of enantiomers of an α-amino acid ester which is a racemic mixture and represented by the formula (I): wherein R and R1 have the same meanings as defined above, in the presence of a lipase or a protease in an organic solvent.

    摘要翻译： 本发明公开了一种制备由式（II）表示的光学活性（S或R）-α-氨基酸的方法：其中R表示烷基，烯基，炔基，环烷基，芳烷基，杂芳基烷基 ，芳基或杂芳基，每个可以具有取代基，*表示不对称碳原子，和由式（III）表示的光学活性（R或S）-α-氨基酸酯：其中 R 1表示可以具有取代基的烷基，*表示不对称碳原子，条件是其具有与式（II）化合物相反的绝对构型，其包括选择性地使水与 由式（I）表示的外消旋混合物的α-氨基酸酯的对映异构体：其中R和R 1具有与上述相同的含义，在有机溶剂中存在脂肪酶或蛋白酶。

    Process for preparing optically active (S or R)-α amino acid and (R or S)-α amino acid ester in one phase organic reaction medium
    9.
    发明授权
    Process for preparing optically active (S or R)-α amino acid and (R or S)-α amino acid ester in one phase organic reaction medium 有权
    在一相有机反应介质中制备光学活性（S或R）-α氨基酸和（R或S）-α氨基酸酯）的方法

    公开(公告)号：US08143052B2

    公开(公告)日：2012-03-27

    申请号：US12064589

    申请日：2006-08-25

    申请人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa

    发明人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa

    IPC分类号： C12P41/00

    CPC分类号： C12P13/04 ,  C12P41/005

    摘要： The present invention discloses a process for preparing an optically active (S or R)-α-amino acid represented by the formula (II): wherein R represents an alkyl group, alkenyl group, alkynyl group, cycloalkyl group, aralkyl group, heteroarylalkyl group, aryl group or heteroaryl group, each of which may have a substituent(s), and * represents an asymmetric carbon atom, and an optically active (R or S)-α-amino acid ester represented by the formula (III): wherein R1 represents an alkyl group which may have a substituent(s), and * represents an asymmetric carbon atom, provided that it has an opposite absolute configuration to that of the compound of the formula (II), which comprises selectively reacting water with one of enantiomers of an α-amino acid ester which is a racemic mixture and represented by the formula (I): wherein R and R1 have the same meanings as defined above, in the presence of a lipase or a protease in an organic solvent.

    摘要翻译： 本发明公开了一种制备由式（II）表示的光学活性（S或R）-α-氨基酸的方法：其中R表示烷基，烯基，炔基，环烷基，芳烷基，杂芳基烷基 ，芳基或杂芳基，每个可以具有取代基，*表示不对称碳原子，和由式（III）表示的光学活性（R或S）-α-氨基酸酯：其中 R 1表示可以具有取代基的烷基，*表示不对称碳原子，条件是其具有与式（II）化合物相反的绝对构型，其包括选择性地使水与 由式（I）表示的α-氨基酸酯的对映异构体：其中R和R 1具有与上述相同的含义，在有机溶剂中存在脂肪酶或蛋白酶的情况下。

    3-Amino-3-arylpropionic acid n-alkyl esters, process for production thereof, and process for production of optically active 3-amino-3-arylpropionic acids and esters of the antipodes thereto
    10.
    发明申请
    3-Amino-3-arylpropionic acid n-alkyl esters, process for production thereof, and process for production of optically active 3-amino-3-arylpropionic acids and esters of the antipodes thereto 审中-公开
    3-氨基-3-芳基丙酸正烷基酯，其制备方法及其制备光学活性3-氨基-3-芳基丙酸和对映体的酯的方法

    公开(公告)号：US20060178433A1

    公开(公告)日：2006-08-10

    申请号：US10549322

    申请日：2004-03-17

    申请人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa ,  Kazuma Sakata

    发明人： Yasuhito Yamamoto ,  Hiroyuki Miyata ,  Tadayoshi Konegawa ,  Kazuma Sakata

    IPC分类号： A61K31/24 ,  C07C229/34

    CPC分类号： C12P41/005 ,  C07B2200/07 ,  C07C229/34 ,  C07D317/60 ,  C12P13/04

    摘要： The present invention is to provide an n-alkyl 3-amino-3-arylpropionate represented by the formula (I): wherein Ar1 represents an aryl group which may have a substituent(s), provided that a phenyl group and 4-methoxyphenyl group are excluded, R1 represents an n-propyl group or an n-butyl group, and a process for preparing the same, and its optically active compound and an optically active (S or R)-3-amino-3-arylpropionic acid represented by the formula (III-a): wherein Ar represents an aryl group which may have a substituent(s), and * represents an asymmetric carbon, and a process for preparing an optically active n-alkyl (R or S)-3-amino-3-arylpropionate represented by the formula (IV-a): wherein Ar and R1 have the same meanings as defined above, * represents an asymmetric carbon, provided that it has a reverse absolute configuration to the compound of the formula (III-a).

    摘要翻译： 本发明提供由式（I）表示的3-氨基-3-芳基丙酸正烷基酯：其中Ar 1表示可以具有取代基的芳基，条件是 除了苯基和4-甲氧基苯基之外，R 1表示正丙基或正丁基，及其制备方法，其光学活性化合物和光学活性化合物 由式（III-a）表示的（S或R）-3-氨基-3-芳基丙酸：其中Ar表示可以具有取代基的芳基，*表示不对称碳， 制备由式（IV-a）表示的光学活性正烷基（R或S）-3-氨基-3-芳基丙酸酯：其中Ar和R 1具有与上述相同的含义， *表示不对称碳，条件是其具有与式（III-a）化合物相反的绝对构型。