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公开(公告)号:US20150119573A1
公开(公告)日:2015-04-30
申请号:US14394079
申请日:2012-12-27
申请人: ASYMCHEM LABORATORIES (TIANJIN)CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD. , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO. LTD.
发明人: Hao Hong , James Gage , Chaoyong Chen , Jiangping Lu , Yan Zhou , Shuangyong Liu
IPC分类号: C07D475/04 , C07D317/32 , C07D317/26 , C07C221/00 , C07D239/50 , C07C209/62 , C07D317/28 , C07D303/48 , C07C225/06
CPC分类号: C07D475/04 , C07C209/62 , C07C221/00 , C07C225/06 , C07D239/50 , C07D303/48 , C07D317/26 , C07D317/28 , C07D317/32
摘要: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
摘要翻译: 披露了一种合成沙rop in二盐酸盐的方法。 本公开内容减少了沙棘蛋白二盐酸盐的合成途径,并且通过使用手性拆分试剂拆分外消旋体中间体或具有低antimer异构值的中间体,从而获得具有高antimer异构值的中间体。 原材料便宜,易于获得,成本显着降低,为大规模工业生产四氢叶酸二盐酸盐提供了有效的方案。
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公开(公告)号:US09371326B2
公开(公告)日:2016-06-21
申请号:US14394079
申请日:2012-12-27
申请人: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD , ASYMCHEM LABORATORIES (FUXIN) CO., LTD , JILIN ASYMCHEM LABORATORIES CO.,LTD
发明人: Hao Hong , James Gage , Chaoyong Chen , Jiangping Lu , Yan Zhou , Shuangyong Liu
IPC分类号: C07D475/04 , C07D239/50 , C07D239/48 , C07D239/47 , C07D303/48 , C07D317/26 , C07D317/28 , C07D317/32 , C07C209/62 , C07C221/00 , C07C225/06
CPC分类号: C07D475/04 , C07C209/62 , C07C221/00 , C07C225/06 , C07D239/50 , C07D303/48 , C07D317/26 , C07D317/28 , C07D317/32
摘要: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
摘要翻译: 披露了一种合成沙rop in二盐酸盐的方法。 本公开内容减少了沙棘蛋白二盐酸盐的合成途径,并且通过使用手性拆分试剂拆分外消旋体中间体或具有低antimer异构值的中间体,从而获得具有高antimer异构值的中间体。 原材料便宜,易于获得,成本显着降低,为大规模工业生产四氢叶酸二盐酸盐提供了有效的方案。
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公开(公告)号:US09365573B2
公开(公告)日:2016-06-14
申请号:US14391712
申请日:2012-12-27
申请人: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD , ASYMCHEM LABORATORIES (FUXIN) CO., LTD , JILIN ASYMCHEM LABORATORIES CO., LTD
发明人: Hao Hong , James Gage , Chaoyong Chen , Jiangping Lu , Yan Zhou , Shuangyong Liu
IPC分类号: C07D475/04 , C07D239/50 , C07D239/48 , C07D239/47 , C07D303/48 , C07D317/26 , C07D317/28 , C07D317/32 , C07C209/62 , C07C221/00 , C07C225/06 , C07D301/03 , C07D301/12 , C07D301/14
CPC分类号: C07D475/04 , C07C221/00 , C07D239/50 , C07D301/03 , C07D301/12 , C07D301/14 , C07D317/26 , C07D317/28 , C07D317/32
摘要: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
摘要翻译: 披露了一种合成沙rop in二盐酸盐的方法。 本公开内容减少了沙棘蛋白二盐酸盐的合成途径,以不对称合成方式引入手性中心,其中采用含有钐催化剂的四氢呋喃溶液作为催化剂,并通过方法获得具有高抗反义异构性值的目标化合物 的选择性催化。 产量提高,原料便宜,易于获得,成本显着降低,为大规模工业生产四氢叶酸二盐酸盐提供了有效的方案。
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公开(公告)号:US20170190684A1
公开(公告)日:2017-07-06
申请号:US15309469
申请日:2014-08-04
申请人: Asymchem Laboratories (Tianjin) Co., Ltd. , Asymchem Life Science (Tianjin) Co., Ltd. , Tianjin Asymchem Pharmaceutical Co., Ltd. , Asymchem Laboratories (Fuxin) Co., Ltd. , Jilin Asymchem Laboratories Co., Ltd.
发明人: Hao Hong , Chaoyong Chen , Jiuyuan Li , Litao Shen , Lina Guo , Hongying Tian
IPC分类号: C07D319/06 , C12P7/62 , C07C67/30 , C07C51/367 , C07C67/313
CPC分类号: C07D319/06 , C07C51/367 , C07C67/30 , C07C67/313 , C12P7/62
摘要: The present invention relates to a preparation method for a chiral intermediate for use in statins, acquired with chloroacetic acid and benzyl alcohol as starting materials via a series of reactions, namely etherification, condensation, substitution, and asymmetric reduction. The preparation method provided in the present invention has a novel route of synthesis, allows an intermediate compound to be introduced conveniently into the chiral center of a glycol via enzyme reduction, and not only is low in costs, but also is reliable in quality. The route of synthesis provided in the present invention uses raw materials of low costs, has an easy to operate process, and provides a final product of great purity and high yield.
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公开(公告)号:US10544119B2
公开(公告)日:2020-01-28
申请号:US15309469
申请日:2014-08-04
申请人: Asymchem Laboratories (Tianjin) Co., Ltd. , Asymchem Life Science (Tianjin) Co., Ltd. , Tianjin Asymchem Pharmaceutical Co., Ltd. , Asymchem Laboratories (Fuxin) Co., Ltd. , Jilin Asymchem Laboratories Co., Ltd.
发明人: Hao Hong , Chaoyong Chen , Jiuyuan Li , Litao Shen , Lina Guo , Hongying Tian
IPC分类号: C07D319/06 , C12P7/62 , C07C51/367 , C07C67/30 , C07C67/313
摘要: The present invention relates to a preparation method for a chiral intermediate for use in statins, acquired with chloroacetic acid and benzyl alcohol as starting materials via a series of reactions, namely etherification, condensation, substitution, and asymmetric reduction. The preparation method provided in the present invention has a novel route of synthesis, allows an intermediate compound to be introduced conveniently into the chiral center of a glycol via enzyme reduction, and not only is low in costs, but also is reliable in quality. The route of synthesis provided in the present invention uses raw materials of low costs, has an easy to operate process, and provides a final product of great purity and high yield.
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公开(公告)号:US20150105555A1
公开(公告)日:2015-04-16
申请号:US14391712
申请日:2012-12-27
申请人: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO., LTD.
发明人: Hao Hong , James Gage , Chaoyong Chen , Jiangping Lu , Yan Zhou , Shuangyong Liu
IPC分类号: C07D475/04 , C07D317/32 , C07D317/26 , C07D301/12 , C07C221/00 , C07D239/50 , C07D301/14 , C07D301/03 , C07D317/28
CPC分类号: C07D475/04 , C07C221/00 , C07D239/50 , C07D301/03 , C07D301/12 , C07D301/14 , C07D317/26 , C07D317/28 , C07D317/32
摘要: Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
摘要翻译: 披露了一种合成沙rop in二盐酸盐的方法。 本公开内容减少了沙棘蛋白二盐酸盐的合成途径,以不对称合成方式引入手性中心,其中采用含有钐催化剂的四氢呋喃溶液作为催化剂,并通过方法获得具有高抗反义异构性值的目标化合物 的选择性催化。 产量提高,原料便宜,易于获得,成本显着降低,为大规模工业生产四氢叶酸二盐酸盐提供了有效的方案。
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