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公开(公告)号：US12084402B2
公开(公告)日：2024-09-10
申请号：US17611712
申请日：2019-05-21
发明人： Hao Hong , Jiangping Lu , Enxuan Zhang , Wei Shen , Honglei Yan , Zhen Zhang
IPC分类号： C07C245/16
CPC分类号： C07C245/16
摘要： Provided is a preparation process of diazomethane. The preparation process includes: step S1, taking N-methylurea as a raw material to continuously prepare, in a continuous reactor, a first product system containing N-methyl-N-nitrosourea: step S2, performing continuous extraction and continuous back-extraction on the first product system to obtain an N-methyl-N-nitrosourea solution; step S3, enabling the N-methyl-N-nitrosourea solution to continuously react with an alkaline solution in a continuous reactor to obtain a second product system containing the diazomethane; and step S4, performing continuously liquid separation, water freezing and removal on the second product system, to obtain the diazomethane.
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公开(公告)号：US09926283B2
公开(公告)日：2018-03-27
申请号：US15124083
申请日：2014-03-07
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 , Jiuyuan Li , Litao Shen , Lei Zhang , Changming Dong
IPC分类号： C07D239/42 , C07F9/6512
CPC分类号： C07D239/42 , C07B2200/13 , C07F9/6512 , Y02P20/55
摘要： Provided are an intermediate compound for preparing rosuvastatin calcium and a preparation method of the rosuvastatin calcium. The method comprises: using the foregoing intermediate compound as a raw material, and subjecting the raw material to a step of Wittig reaction, a step of protecting group removal and hydrolysis and a step of calcium salt formation, so as to obtain the rosuvastatin calcium. The product, which is prepared from the intermediate compound, can be substantially enhanced in stereoselectivity and also notably improved in purity and yield; in addition, the method for preparing rosuvastatin calcium from the intermediate compound is simple, convenient and low in cost.
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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：US20240117395A1
公开(公告)日：2024-04-11
申请号：US18275833
申请日：2021-07-06
发明人： Hao Hong , Gage James , Yi Xiao , Na Zhang , Xuecheng Jiao , Yulei Ma , Huiyan Mou , Zujian Wang , Kaihua Sun , Ru Jia , Fang Liu , Wenjing Liu
CPC分类号： C12P17/14 , C12N9/1096 , C12P13/001 , C12P17/12 , C12Y206/01
摘要： Provided is a method for synthesizing a chiral amine compound. A transaminase is used to transaminate a ketone substrate under the action of an amino donor, to obtain the chiral amine compound; and the conserved amino acid sequence region of the transaminase at least includes a region 1 (MAGLWCVN) and a region 2 (YNTFFKT). With the transaminase with the specific conserved amino acid sequence region to synthesize a large sterically hindered chiral amine, the enzyme catalytic reaction volume is small, the synthesizing route is short, the product yield is high, a high-cost noble metal is not required for catalysis under the synthesizing conditions, three wastes are reduced, and the production cost is saved.
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公开(公告)号：US10961516B2
公开(公告)日：2021-03-30
申请号：US16344779
申请日：2016-11-04
申请人： ASYMCHEM LABORATORIES (TIANJIN) CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD. , TIANJIN ASYMCHEM PHARMACEUTICALS CO., LTD. , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO., LTD.
发明人： Hao Hong , Gage James , Jiangping Lu , Na Zhang , Wenyan Yu , Fang Liu , Yanjun Li , Xin Huang , Juan Gao , Kejian Zhang , Yulei Ma , Junlu Wei
摘要： Provided are a proline hydroxylase and uses thereof. The proline hydroxylase comprises (a) a protein having the amino acid sequence as shown in SEQ ID NO: 2; (b) a protein having an amino acid sequence of SEQ HD NO: 2 with a mutation of one or more amino acids and having a proline hydroxylase activity; or (c) a protein retaining the mutation of one or more amino acids as in (b), and having the proline hydroxylase activity and having at least 78% homology with the amino acid sequence of the protein in (b). Protein having the amino acid sequence as shown in SEQ HD NO: 2 and mutants obtained by genetically engineering have higher catalytic specificity or significantly increased catalytic activity when compared to proline hydroxylases in prior art.
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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：US10131883B2
公开(公告)日：2018-11-20
申请号：US15309690
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.
摘要： The application provides a Diketoreductase (DKR) mutant, its nucleotide coding sequence, and an expression cassette, recombinant vector and host cell containing the sequence, as well as a method for application of the mutant to the preparation of 3R,5S-dicarbonyl compound. An ee value of the obtained 3R,5S-dicarbonyl compound is higher than 99%, and a de value is about 90%. The DKR mutant is a key pharmaceutical intermediate, and particularly provides an efficient catalyst for synthesis of a chiral dicarbonyl hexanoic acid chain of a statin drug.
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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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公开(公告)号：US11827909B2
公开(公告)日：2023-11-28
申请号：US17118169
申请日：2020-12-10
申请人： ASYMCHEM LABORATORIES (TIANJIN) CO., LTD. , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD. , TIANJIN ASYMCHEM PHARMACEUTICALS CO., LTD. , ASYMCHEM LABORATORIES (FUXIN) CO., LTD. , JILIN ASYMCHEM LABORATORIES CO., LTD.
发明人： Hao Hong , Gage James , Jiangping Lu , Na Zhang , Wenyan Yu , Fang Liu , Yanjun Li , Xin Huang , Juan Gao , Kejian Zhang , Yulei Ma , Junlu Wei
CPC分类号： C12N9/0071 , C12N15/70 , C12N15/81 , C12Y114/11002
摘要： Provided are a proline hydroxylase and uses thereof. The proline hydroxylase comprises having the amino acid sequence of SEQ ID NO: 2 with the exception of a mutation of one or more amino acids; wherein the mutation of one or more amino acids must comprises E27K, and the mutation of one or more amino acids selected from the group consisting of: H14R, L16N, T25R, F26L, E27K, D30S, S33N, E34N, E34G, E34L, E34S, E34D, Y35W, Y35K, S37W, S37F, S37E, S37N, S37T, S37C, W40F, K41E, D54G, H55Q, S57L, I58T, I58Y, I58A, I58R, I58V, I58S, I58C, K86P, T91A, F95Y, C97Y, I98V, K106V, K106T, K106Q, F111S, K112E, K112R, S154A, K162E, L166M, I118F, I118V, I118R, H119R, H119F, I120V, K123D, K123N, K123Q, K123S, K123I, K123T, T130N, D134G, V135K, N165H, D173G, K209R, I223V and S225A, and having proline hydroxylase activity.
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公开(公告)号：US10399071B2
公开(公告)日：2019-09-03
申请号：US15039189
申请日：2014-09-10
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 , Jiuyuan Li , Changming Dong , Xin Zhang , Gage James
IPC分类号： B01J31/00 , B01J31/06 , C07D477/06 , C08F212/08 , C07D477/04 , C08F12/22 , C08F12/26 , C08F12/32 , C08F12/34 , C08F212/14 , B01J23/46 , B01J31/28 , C08J9/00 , C08J9/14
摘要： A polymer containing a carboxyl group, a preparation method and an application thereof, a supported catalyst and a preparation method thereof and preparation methods of penem antibiotic intermediate are disclosed. The polymer has high rigidity and hardness, thus the mechanical properties of the polymer is effectively improved. Meanwhile, in the polymer, the carboxyl group is used as a main functional group, and is used as a carrier to prepare, by means of a coordination reaction between the carboxyl group and a heavy metal, a supported metal catalyst which has better connection stability between the metal and the polymer. The above two factors can improve the stability of the supported metal catalyst, such that the catalyst can be recycled without losing the catalytic activity. Meanwhile, loss of a heavy metal active ingredient and production cost can be reduced.
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