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    Bisulfite purification of an alpha-keto amide
    1.
    发明授权
    Bisulfite purification of an alpha-keto amide 有权
    亚硫酸氢盐净化α-酮酰胺

    公开(公告)号：US08222427B2

    公开(公告)日：2012-07-17

    申请号：US12518736

    申请日：2007-12-13

    申请人： George S. K. Wong ,  Jeonghan Park ,  Tetsuo Iwama ,  Anantha R. Sudhakar

    发明人： George S. K. Wong ,  Jeonghan Park ,  Tetsuo Iwama ,  Anantha R. Sudhakar

    IPC分类号： C07D209/00

    CPC分类号： C07D209/52

    摘要： This disclosure relates to novel processes useful in the purification of keto-amide, ketone and aldehyde compounds, which are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease and have application in the treatment of conditions caused by HCV. The processes of this disclosure relate to purification via a bisulfite adduct. In particular, this disclosure relates to processes useful in the purification of the keto-amide compound of Formula I, (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]-amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide:

    摘要翻译： 本公开涉及用于纯化酮酰胺，酮和醛化合物的新方法，其可用作丙型肝炎病毒（HCV）NS3蛋白酶的抑制剂，并且可用于治疗由HCV引起的病症。 本公开的方法涉及通过亚硫酸氢盐加合物的纯化。 特别地，本公开涉及用于纯化式I的酮酰胺化合物，（1R，5S）-N- [3-氨基-1-（环丁基甲基）-2,3-二氧代丙基] -3- [2（S） - [[[（1,1-二甲基乙基）氨基]羰基] - 氨基] -3,3-二甲基-1-氧代丁基] -6,6-二甲基-3-氮杂双环[3.1.0] -2（S） - 甲酰胺：

    Process for the preparation of a quinone derivative
    6.
    发明授权
    Process for the preparation of a quinone derivative 失效
    醌衍生物的制备方法

    公开(公告)号：US5476955A

    公开(公告)日：1995-12-19

    申请号：US203372

    申请日：1994-03-01

    申请人： Kimio Hamamura ,  Tetsuo Iwama ,  Chiaki Seki ,  Masayuki Konishi

    发明人： Kimio Hamamura ,  Tetsuo Iwama ,  Chiaki Seki ,  Masayuki Konishi

    IPC分类号： B01J23/04 ,  B01J31/02 ,  C07B61/00 ,  C07C46/00 ,  C07C49/683 ,  C07C49/753 ,  C07C50/06 ,  C07C50/14 ,  C07C50/28 ,  C07C50/32

    CPC分类号： C07C50/14 ,  C07C46/00 ,  C07C49/683 ,  C07C49/753

    摘要： Disclosed herein are a quinone derivative represented by the following formula: ##STR1## wherein E.sup.1 and E.sup.2 are identical with or different from each other and mean individually a lower alkyl or lower alkoxy group, or may form an aromatic ring together, E.sup.3 denotes a lower alkyl group, n stands for 0 or an integer of 1-9, and a linkage ------ is a single or double bond, such as a vitamin K derivative or coenzyme Q derivative; and a process for the preparation of the quinone derivative at a high yield without forming any geometric isomer; as well as a 1,4,4.sub.a,8.sub.a -tetrahydro-4.sub.a .alpha.-alkenyl-1.alpha.,4.alpha.-methanonaphthalene-5,8-dione derivative which is useful as an intermediate for the preparation of the quinone derivative.

    摘要翻译： 本文公开了由下式表示的醌衍生物：其中E1和E2彼此相同或不同，并且分别表示低级烷基或低级烷氧基，或者可以一起形成芳环，E3表示低级 烷基，n表示0或1-9的整数，键为单键或双键，例如维生素K衍生物或辅酶Q衍生物; 以及高产率制备醌衍生物而不形成任何几何异构体的方法; 以及可用作制备醌衍生物的中间体的1,4,4a，8a-四氢-4aα-烯基-1α，4α-甲基萘-5,8-二酮衍生物。

    BISULFITE PURIFICATION OF AN ALPHA-KETO AMIDE
    7.
    发明申请
    BISULFITE PURIFICATION OF AN ALPHA-KETO AMIDE 有权
    一种ALPHA-KETO酰胺的双相纯化

    公开(公告)号：US20090326244A1

    公开(公告)日：2009-12-31

    申请号：US12518736

    申请日：2007-12-13

    申请人： George S. K. Wong ,  Jeonghan Park ,  Tetsuo Iwama ,  Anantha R. Sudhakar

    发明人： George S. K. Wong ,  Jeonghan Park ,  Tetsuo Iwama ,  Anantha R. Sudhakar

    IPC分类号： C07D209/52

    CPC分类号： C07D209/52

    摘要： A process for purifying the alpha-keto amide is (1R,5S)—N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]-amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide via a bisulfite adduct is disclosed.

    摘要翻译： 纯化α-酮酰胺的方法是（1R，5S）-N- [3-氨基-1-（环丁基甲基）-2,3-二氧代丙基] -3- [2（S） - [[ 1,1-二甲基乙基）氨基]羰基] - 氨基] -3,3-二甲基-1-氧代丁基] -6,6-二甲基-3-氮杂双环[3.1.0]己-2（S） - 甲酰胺通过亚硫酸氢盐加合物 披露

    Tetrahydro-alkenyl-methanonaphthalene-5,8-dione derivatives
    8.
    发明授权
    Tetrahydro-alkenyl-methanonaphthalene-5,8-dione derivatives 失效
    四氢 - 烯基 - 甲烷基-5,8-二酮衍生物

    公开(公告)号：US5686635A

    公开(公告)日：1997-11-11

    申请号：US686484

    申请日：1996-07-26

    申请人： Kimio Hamamura ,  Tetsuo Iwama ,  Chiaki Seki ,  Masayuki Konishi

    发明人： Kimio Hamamura ,  Tetsuo Iwama ,  Chiaki Seki ,  Masayuki Konishi

    IPC分类号： B01J23/04 ,  B01J31/02 ,  C07B61/00 ,  C07C46/00 ,  C07C49/683 ,  C07C49/753 ,  C07C50/06 ,  C07C50/14 ,  C07C50/28 ,  C07C50/32 ,  C07C50/04

    CPC分类号： C07C50/14 ,  C07C46/00 ,  C07C49/683 ,  C07C49/753

    摘要： Disclosed herein are a quinone derivative represented by the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are identical with or different from each other and mean individually a lower alkyl or lower alkoxy group, or may form an aromatic ring together, R.sup.3 denotes a lower alkyl group, n stands for 0 or an integer of 1-9, and a linkage --- is a single or double bond, such as a vitamin K derivative or coenzyme derivative; and a process for the preparation of the quinone derivative at a high yield without forming any geometric isomer; as well as a 1,4,4.sub.a,8.sub.a -tetrahydro-4.sub.a .alpha.-alkenyl-1.alpha.,4.alpha.-methanonaphthalene-5,8-dione derivative which is useful as an intermediate for the preparation of the quinone derivative.

    摘要翻译： 本文公开了由下式表示的醌衍生物：其中R 1和R 2彼此相同或不同，并且分别表示低级烷基或低级烷氧基，或者可以一起形成芳环，R 3表示低级 烷基，n表示0或1-9的整数，键+ E，uns --- + EE是单键或双键，例如维生素K衍生物或辅酶衍生物; 以及高产率制备醌衍生物而不形成任何几何异构体的方法; 以及可用作制备醌衍生物的中间体的1,4,4a，8a-四氢-4aα-烯基-1α，4α-甲基萘-5,8-二酮衍生物。

    Process for the preparation of quinone derivative
    9.
    发明授权
    Process for the preparation of quinone derivative 失效
    醌衍生物的制备方法

    公开(公告)号：US5677471A

    公开(公告)日：1997-10-14

    申请号：US686412

    申请日：1996-07-26

    申请人： Kimio Hamamura ,  Tetsuo Iwama ,  Chiaki Seki ,  Masayuki Konishi

    发明人： Kimio Hamamura ,  Tetsuo Iwama ,  Chiaki Seki ,  Masayuki Konishi

    IPC分类号： B01J23/04 ,  B01J31/02 ,  C07B61/00 ,  C07C46/00 ,  C07C49/683 ,  C07C49/753 ,  C07C50/06 ,  C07C50/14 ,  C07C50/28 ,  C07C50/32 ,  C07C50/12

    CPC分类号： C07C50/14 ,  C07C46/00 ,  C07C49/683 ,  C07C49/753

    摘要： Disclosed herein are a quinone derivative represented by the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are identical with or different from each other and mean individually a lower alkyl or lower alkoxy group, or may form an aromatic ring together, R.sup.3 denotes a lower alkyl group, n stands for 0 or an integer of 1-9, and a linkage--is a single or double bond, such as a vitamin K derivative or coenzyme Q derivative; and a process for the preparation of the quinone derivative at a high yield without forming any geometric isomer; as well as a 1,4,4.sub.a,8.sub.a -tetrahydro-4.sub.a .alpha.-alkenyl-1.alpha.,4.alpha.-methanonaphthalene-5,8-dione derivative which is useful as an intermediate for the preparation of the quinone derivative.

    摘要翻译： 本文公开了由下式表示的醌衍生物：其中R 1和R 2彼此相同或不同，并且分别表示低级烷基或低级烷氧基，或者可以一起形成芳环，R 3表示低级 烷基，n表示0或1-9的整数，连接是单键或双键，例如维生素K衍生物或辅酶Q衍生物; 以及高产率制备醌衍生物而不形成任何几何异构体的方法; 以及可用作制备醌衍生物的中间体的1,4,4a，8a-四氢-4aα-烯基-1α，4α-甲基萘-5,8-二酮衍生物。