METHOD FOR PRODUCING 1-BIPHENYLMETHYLIMIDAZOLE COMPOUND
    1.
    发明申请
    METHOD FOR PRODUCING 1-BIPHENYLMETHYLIMIDAZOLE COMPOUND 有权
    1-二苯基甲基咪唑化合物的制备方法

    公开(公告)号:US20110092713A1

    公开(公告)日:2011-04-21

    申请号:US12996697

    申请日:2009-06-08

    摘要: The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof.The present invention provides a method for producing a compound having the formula (5) (R1, Ra: H, an alkyl group) by oxidizing a compound having the formula (1) (Ra: H, an alkyl group) using an oxidizing agent in the presence of a radical initiation reagent, and then reacting with an ammonia-generating reagent and a compound having the formula R1CHO(R1: H, an alkyl group) or a compound having the formula R1C(ORb)3 (R1: H, an alkyl group; Rb: an alkyl group).

    摘要翻译: 本发明提供了具有优异的血管紧张素II受体拮抗作用的1-联苯甲基咪唑化合物或其中间体的制备方法。 本发明提供通过使用氧化剂氧化具有式(1)的化合物(Ra:H,烷基)的方法来制备具有式(5)的化合物(R1,Ra:H,烷基) 然后与产生氨的试剂和具有式R1CHO(R1:H,烷基)的化合物或具有式R1C(ORb)3的化合物(R1:H, 烷基; Rb:烷基)。

    Method for producing 1-biphenylmethylimidazole compound
    2.
    发明授权
    Method for producing 1-biphenylmethylimidazole compound 有权
    1-联苯甲基咪唑化合物的制备方法

    公开(公告)号:US08735598B2

    公开(公告)日:2014-05-27

    申请号:US12996697

    申请日:2009-06-08

    摘要: The present invention provides a method for producing a 1-biphenylmethylimidazole compound having superior angiotensin II receptor antagonistic activity, or an intermediate thereof.The present invention provides a method for producing a compound having the formula (5) (R1, Ra: H, an alkyl group) by oxidizing a compound having the formula (1) (Ra: H, an alkyl group) using an oxidizing agent in the presence of a radical initiation reagent, and then reacting with an ammonia-generating reagent and a compound having the formula R1CHO(R1: H, an alkyl group) or a compound having the formula R1C(ORb)3 (R1: H, an alkyl group; Rb: an alkyl group).

    摘要翻译: 本发明提供了具有优异的血管紧张素II受体拮抗作用的1-联苯甲基咪唑化合物或其中间体的制备方法。 本发明提供通过使用氧化剂氧化具有式(1)的化合物(Ra:H,烷基)的方法来制备具有式(5)的化合物(R1,Ra:H,烷基) 然后与产生氨的试剂和具有式R1CHO(R1:H,烷基)的化合物或具有式R1C(ORb)3的化合物(R1:H, 烷基; Rb:烷基)。

    Process for reductive dehalogenation
    3.
    发明授权
    Process for reductive dehalogenation 失效
    还原脱卤方法

    公开(公告)号:US07199260B2

    公开(公告)日:2007-04-03

    申请号:US10541204

    申请日:2004-01-07

    IPC分类号: C07C69/74

    摘要: A method of producing 2-fluorocyclopropane-1-carboxylic acid ester, which comprise by allowing a compound represented by the following formula (1): wherein X represents a chlorine atom, a bromine atom or an iodine atom; and R1 represents an alkyl group having 1 to 8 carbon atoms, an aryl group having 6 to 12 carbon atoms, an alkenyl group having 2 to 8 carbon atoms, or an aralkyl group composed of an aryl group having 6 to 12 carbon atoms and an alkylene group having 1 to 6 carbon atoms; to react with a reducing agent in the presence of a phase transfer catalyst. According to the production method of the present invention, the reaction time of dehalogenation can be greatly shortened.

    摘要翻译: 2-氟环丙烷-1-羧酸酯的制备方法,其包括使下式(1)表示的化合物:

    Process for reductive dehaloganation
    4.
    发明申请
    Process for reductive dehaloganation 失效
    还原脱卤法的工艺

    公开(公告)号:US20060052626A1

    公开(公告)日:2006-03-09

    申请号:US10541204

    申请日:2004-01-07

    IPC分类号: C07C69/74

    摘要: A method of producing 2-fluorocyclopropane-1-carboxylic acid ester, which comprise by allowing a compound represented by the following formula (1): wherein X represents a chlorine atom, a bromine atom or an iodine atom; and R1 represents an alkyl group having 1 to 8 carbon atoms, an aryl group having 6 to 12 carbon atoms, an alkenyl group having 2 to 8 carbon atoms, or an aralkyl group composed of an aryl group having 6 to 12 carbon atoms and an alkylene group having 1 to 6 carbon atoms; to react with a reducing agent in the presence of a phase transfer catalyst. According to the production method of the present invention, the reaction time of dehalogenation can be greatly shortened.

    摘要翻译: 2-氟环丙烷-1-羧酸酯的制备方法,其包括使下式(1)表示的化合物:

    Method for producing quinolone carboxylic acid derivative
    6.
    发明授权
    Method for producing quinolone carboxylic acid derivative 有权
    喹诺酮羧酸衍生物的制备方法

    公开(公告)号:US07875722B2

    公开(公告)日:2011-01-25

    申请号:US12569938

    申请日:2009-09-30

    摘要: The present invention relates to a method for producing a quinolone compound having high antibacterial activity and high safety, at high yield and in a simple manner.A quinolonecarboxylic acid derivative (1) of interest is produced through a one-pot manner by reacting a compound (2) with a salt of a cyclic amine (3) and with a boron derivative in a solvent in the presence of a base.

    摘要翻译: 本发明涉及以高产率和简单的方式生产具有高抗菌活性和高安全性的喹诺酮化合物的方法。 通过使化合物(2)与环胺(3)的盐与硼衍生物在溶剂中在碱的存在下反应,通过一锅方式制备目标的喹诺酮羧酸衍生物(1)。

    Process for producing 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid
    8.
    发明授权
    Process for producing 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid 失效
    5-甲基-4,5,6,7-四氢噻唑并[5,4-c]吡啶-2-甲酸的制备方法

    公开(公告)号:US08058440B2

    公开(公告)日:2011-11-15

    申请号:US12941622

    申请日:2010-11-08

    IPC分类号: C07D513/04

    CPC分类号: C07D513/04

    摘要: 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid of formula (5) or a salt thereof, is prepared by reacting reacting 2-bromo-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (3) or a salt thereof, with a metal cyanide, to obtain 2-cyano-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (4) or a salt thereof, and hydrolyzing the 2-cyano-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine of formula (4) or a salt thereof.

    摘要翻译: 式(5)的5-甲基-4,5,6,7-四氢噻唑并[5,4-c]吡啶-2-甲酸或其盐通过使2-溴-5-甲基-4 ,式(3)的5,6,7-四氢噻唑并[5,4-c]吡啶或其盐与金属氰化物反应,得到2-氰基-5-甲基-4,5,6,7-四氢噻唑 (4)的[5,4-c]吡啶或其盐,并水解式(4)的2-氰基-5-甲基-4,5,6,7-四氢噻唑并[5,4-c] )或其盐。