BARIUM SALT OF BENZIMIDAZOLE DERIVATIVE
    6.
    发明申请
    BARIUM SALT OF BENZIMIDAZOLE DERIVATIVE 审中-公开
    苯并咪唑衍生物的钡盐

    公开(公告)号:US20110086884A1

    公开(公告)日:2011-04-14

    申请号:US12973499

    申请日:2010-12-20

    CPC分类号: C07D401/12 A61K31/4439

    摘要: The invention relates to crystalline barium salt of (S)-omeprazole, which is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole. The invention also relates to processes for preparing crystalline barium salt of (S)-omeprazole and pharmaceutical compositions that include the crystalline barium salt of (S)-omeprazole so prepared.

    摘要翻译: 本发明涉及(S) - 奥美拉唑的结晶钡盐,其为(S)-5-甲氧基-2 - [[(4-甲氧基-3,5-二甲基-2-吡啶基) - 甲基]亚磺酰基〕-1H 苯并咪唑。 本发明还涉及制备(S) - 奥美拉唑的结晶钡盐的方法和包括如此制备的(S) - 奥美拉唑的结晶钡盐的药物组合物。

    PROCESS FOR THE PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT
    7.
    发明申请
    PROCESS FOR THE PREPARATION OF ATAZANAVIR OR ITS BISULFATE SALT 审中-公开
    制备ATAZANAVIR或其BISULFATE盐的方法

    公开(公告)号:US20140343290A1

    公开(公告)日:2014-11-20

    申请号:US14235127

    申请日:2012-07-25

    IPC分类号: C07D213/42

    CPC分类号: C07D213/42

    摘要: The present invention relates to an improved process for the preparation of atazanavir bisulfate, an inhibitor of retroviral aspartate protease. The process of the present invention comprises conversion of 1,1-dimethylethyl[(2S,3R)-4-chloro-3-hydroxy-phenylbutan-2-yl]carbamate (Formula II) into 1-[4-(pyridine-2-yl)-phenyl]-4(S)-5 hydroxy-2-N-tert-butoxycarbonylamino-5(S)—N—(N-methoxycarbonyl-(L)-tert-leucyl)amino-6-phenyl-2-azahexane (Formula VII) without isolating intermediate compounds formed therein, followed by its subsequent conversion to atazanavir or its bisulfate salt.

    摘要翻译: 本发明涉及一种制备逆转录病毒天冬氨酸蛋白酶抑制剂阿扎那韦硫酸氢盐的改进方法。 本发明的方法包括将[(2S,3R)-4-氯-3-羟基 - 苯基丁-2-基]氨基甲酸酯(式II)的1,1-二甲基乙基酯转化为1- [4-(吡啶-2 - 基) - 苯基] -4(S)-5-羟基-2-N-叔丁氧基羰基氨基-5(S)-N-(N-甲氧基羰基 - (L) - 叔 - 亮氨酰基)氨基-6-苯基-2 (式Ⅶ),而不分离其中形成的中间体化合物,随后转化成阿扎那韦或其硫酸氢盐。

    BARIUM SALT OF BENZIMIDAZOLE DERIVATIVE
    8.
    发明申请
    BARIUM SALT OF BENZIMIDAZOLE DERIVATIVE 有权
    苯并咪唑衍生物的钡盐

    公开(公告)号:US20090259047A1

    公开(公告)日:2009-10-15

    申请号:US12467051

    申请日:2009-05-15

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12 A61K31/4439

    摘要: The invention relates to crystalline barium salt of (S)-omeprazole, which is (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1H-benzimidazole. The invention also relates to processes for preparing crystalline barium salt of (S)-omeprazole and pharmaceutical compositions that include the crystalline barium salt of (S)-omeprazole so prepared.

    摘要翻译: 本发明涉及(S) - 奥美拉唑的结晶钡盐,其为(S)-5-甲氧基-2 - [[(4-甲氧基-3,5-二甲基-2-吡啶基) - 甲基]亚磺酰基〕-1H 苯并咪唑。 本发明还涉及制备(S) - 奥美拉唑的结晶钡盐的方法和包括如此制备的(S) - 奥美拉唑的结晶钡盐的药物组合物。

    Processes for the Preparation of Substituted Sulfoxides
    9.
    发明申请
    Processes for the Preparation of Substituted Sulfoxides 有权
    制备取代的亚砜的方法

    公开(公告)号:US20080275245A1

    公开(公告)日:2008-11-06

    申请号:US11576867

    申请日:2005-10-04

    IPC分类号: C07D401/12

    CPC分类号: C07D401/12

    摘要: The present invention relates to a process for enantioselective synthesis of substituted pyridinylmethyl sulfinyl-benzimidazole of compound of Formula (I). The process includes enantioselective catalytic oxidation of a substituted pyridinylmethyl prochiral sulfide derivative of compound of Formula (II) with an oxidizing agent in the presence of a chiral transition metal complex and a base in the absence of an organic solvent.

    摘要翻译: 本发明涉及式(I)化合物的取代的吡啶基甲基亚磺酰基 - 苯并咪唑的对映选择性合成方法。 该方法包括式(II)化合物的取代的吡啶基甲基前手性硫化物衍生物在手性过渡金属络合物和碱的存在下,在不存在有机溶剂的情况下与氧化剂的对映选择性催化氧化。