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公开(公告)号:US09328100B2
公开(公告)日:2016-05-03
申请号:US14683883
申请日:2015-04-10
IPC分类号: C07D409/10 , C07D309/10
CPC分类号: C07D409/10 , C07D309/10 , Y02P20/55
摘要: The present application discloses a stereoselective process for the preparation of β-C-arylglucosides that does not require the use of conventional carbohydrate protecting groups. In one embodiment, the stereoselective process comprises the preparation of the compound of formula I: the process comprising: a) contacting 1,6-anhydro-β-D-glucopyranose with a compound of formula II, R1R2R3Al, in a solvent to form a first reaction mixture; b) contacting the first reaction mixture of step a) with a second reaction mixture to form a third reaction mixture, wherein the second reaction mixture is prepared by contacting an organoaluminum compound of formula III, R4aR5bAlXc, with a compound of formula IV, ArM; and c) contacting the third reaction mixture with a reagent to form the compound of the formula I.
摘要翻译: 本申请公开了用于制备不需要使用常规碳水化合物保护基团的β-芳基葡糖苷的立体选择性方法。 在一个实施方案中,立体选择性方法包括式I化合物的制备方法:该方法包括:a)在溶剂中使1,6-脱水-β-D-吡喃葡萄糖与式II化合物R1R2R3Al接触形成 第一反应混合物; b)使步骤a)的第一反应混合物与第二反应混合物接触以形成第三反应混合物,其中第二反应混合物通过使式III的有机铝化合物与式IV的化合物ArM; 和c)使第三反应混合物与试剂接触以形成式I的化合物。
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公开(公告)号:US20150291569A1
公开(公告)日:2015-10-15
申请号:US14683883
申请日:2015-04-10
IPC分类号: C07D409/10 , C07D309/10
CPC分类号: C07D409/10 , C07D309/10 , Y02P20/55
摘要: The present application discloses a stereoselective process for the preparation of β-C-arylglucosides that does not require the use of conventional carbohydrate protecting groups.
摘要翻译: 本申请公开了用于制备不需要使用常规碳水化合物保护基团的β-芳基葡糖苷的立体选择性方法。
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公开(公告)号:US08952139B2
公开(公告)日:2015-02-10
申请号:US13671461
申请日:2012-11-07
发明人: Julian Paul Henschke , Chen-Wei Lin , Ping-Yu Wu , Chi-Nung Hsiao , Jyh-Hsiung Liao , Tsung-Yu Hsiao
IPC分类号: C07H1/00 , C07H7/06 , C07H3/00 , C08B37/00 , C07D309/00
CPC分类号: C07D309/00 , C07D309/10
摘要: The present invention provides processes (e.g., arylation reaction) for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors. A representative process of the present application includes the preparation of the compound of formula IV starting from a compound of the formula II with a metalated aryl compound, as disclosed below:
摘要翻译: 本发明提供用于立体选择性制备可以用作合成结构单元或药物(包括SGLT2抑制剂)的C-芳基葡糖苷的方法(例如,芳基化反应)。 本申请的代表性方法包括从式II化合物与金属化芳基化合物开始制备式IV化合物,如下所述:
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公开(公告)号:US09834533B2
公开(公告)日:2017-12-05
申请号:US15430409
申请日:2017-02-10
发明人: Tsung-Yu Hsiao , Jyh-Hsiung Liao
IPC分类号: C07D309/10 , C07D407/12
CPC分类号: C07D309/10 , C07D407/12
摘要: The present invention provides processes for preparing SGLT2 inhibitors, such as dapagliflozin and empagliflozin.
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公开(公告)号:US10118937B1
公开(公告)日:2018-11-06
申请号:US15860949
申请日:2018-01-03
发明人: Tsung-Yu Hsiao , Jyh-Hsiung Liao
摘要: A process for making ixazomib citrate of formula VI comprising reacting a compound of formula V with citric acid to form ixazomib citrate of formula VI: wherein R is hydrogen or an amide protecting group.
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公开(公告)号:US20170240520A1
公开(公告)日:2017-08-24
申请号:US15430409
申请日:2017-02-10
发明人: Tsung-Yu Hsiao , Jyh-Hsiung Liao
IPC分类号: C07D309/10 , C07D407/12
CPC分类号: C07D309/10 , C07D407/12
摘要: The present invention provides processes for preparing SGLT2 inhibitors, such as dapagliflozin and empagliflozin.
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公开(公告)号:US20140128595A1
公开(公告)日:2014-05-08
申请号:US13671461
申请日:2012-11-07
发明人: Julian Paul Henschke , Chen-Wei Lin , Ping-Yu Wu , Chi-Nung Hsiao , Jyh-Hsiung Liao , Tsung-Yu Hsiao
IPC分类号: C07H1/00
CPC分类号: C07D309/00 , C07D309/10
摘要: The present invention provides processes for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors.
摘要翻译: 本发明提供立体选择性制备可用作合成结构单元或药物(包括SGLT2抑制剂)的C-芳基葡糖苷的方法。
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