[PHILLIS, Andrew Toroa 费安杰, YE, Weiping 叶伟平, ZHOU, Zhangtao 周章涛, WANG, Yang 王杨, WANG, Daogong 王道功, LUO, Fuyuan 罗富元] No.3, Binhai 10th Road North, Petrochemical Area, Daya Bay 中国广东省惠州市大亚湾石化区滨海十路北3号, Guangdong 516081Huizhou, Guangdong 516081 A method for preparing a β-nitro or azido alcohol by means of high-selectivity asymmetric catalytic carbonyl reduction. The route of the method is as follows: wherein R1, R2, R3, R4 and R5 are independently selected from any one of H, halogen, a nitro, a cyano, an alkyl, an aryl, a phenolic hydroxyl and an ether group. RuCl[(S,S)-TsDPEN](p-cymene) is used for the asymmetric catalytic reduction of a β-nitro (or azido) ketone, such that a β-nitro (or azido) alcohol having a high optical activity can be rapidly and efficiently constructed. The method is applicable to a wider range of substrates, and is applicable to all substrates which are sensitive to acids.

[ZHOU, Zhangtao 周章涛, YE, Weiping 叶伟平, PHILLIS, Andrew Toroa 费安杰, WANG, Yang 王杨, WANG, Daogong 王道功, LUO, Fuyuan 罗富元] No.3, Binhai 10th Road North, Petrochemical Area, Daya Bay 中国广东省惠州市大亚湾石化区滨海十路北3号, Guangdong 516081Huizhou, Guangdong 516081 Provided is a method for obtaining a high-selectivity β-chiral branched-chain chiral amino acid. The synthetic route of the method for obtaining a high-selectivity β-chiral branched-chain chiral amino acid is: R1 is an alkyl or an aryl; R2 is an alkyl or an aryl; R3 is an alkyl; and R4 is a benzoyl or an acetyl. By using the method for preparing a β-chiral branched-chain chiral amino acid compound, a β-chiral branched-chain chiral amino acid having multiple chiral centers can be efficiently constructed in one step. Different from a traditional enzymatically catalyzed fermentation process, the present solution has better substrate generality and a lower cost, is more environmentally friendly, and can prepare various β-chiral branched-chain chiral amino acid compounds with complex structures.

[ZHOU, Zhangtao 周章涛, YE, Weiping 叶伟平, PHILLIS, Andrew Toroa 费安杰, XU, Li 徐力, HUANG, Zhining 黄志宁, FU, Li 傅利] No.3, Binhai 10th Road North, Petrochemical Area, Daya Bay 中国广东省惠州市大亚湾石化区滨海十路北3号, Guangdong 516081Huizhou, Guangdong 516081 A method for synthesizing (R)-5-(2,2-dimethyl-4H-benzo[d][1,3]dioxin-6-yl)oxazolidin-2-one. The synthesis route of the method is: where X is Br, Cl or I, preferably Br. Preferably, chiral phenyloxazolidin-2-one is prepared from a 2-bromoacetophenone compound in a high-selectivity manner by means of protection, nucleophilic attack, asymmetric transfer hydrogenation, and finally CDI ring closing.

[YE, Weiping 叶伟平, PHILLIS, Andrew Toroa 费安杰, ZHOU, Zhangtao 周章涛, WU, Chunlin 吴春林, HUANG, Zhining 黄志宁, WANG, Daogong 王道功] No.3, Binhai 10th Road North, Petrochemical Area, Daya Bay 中国广东省惠州市大亚湾石化区滨海十路北3号, Guangdong 516081Huizhou, Guangdong 516081 Provided is a method for synthesizing (1R)-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)oxazolidin-2-one, the route of the method being as follows: [Route 1], wherein X is Br, Cl or I, and R1 and R2 are protective groups that can be removed. The method for synthesizing (1R)-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)oxazolidin-2-one has the advantages of novel process route, high yield and high atom economy. Provided is a method for synthesizing (1R)-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)oxazolidi

[YE, Weiping 叶伟平, PHILLIS, Andrew Toroa 费安杰, ZHOU, Zhangtao 周章涛, XIE, Yangyin 谢阳银, XI, Lingang 习林刚, XIANG, Wei 向卫] 801, 8th Floor, Building 1, Shenzhen Biomedical Innovation Industrial Park, No.14, Jinhui Road, Kengzi Street, Pingshan District, 中国广东省深圳市坪山区坑梓街道金辉路14号深圳市生物医药产业园区1号楼8层801, Guangdong 518122Shenzhen, Guangdong 518122 A method for synthesizing 5-bromo-1H-3-amino-1,2,4-triazole. The method has a route as (aa), in which a mixture of sodium bromate and sodium bromide is employed to serve as a brominated reagent; and a reaction route as (bb). The synthesis of 5-bromo-1H-3-amino-1,2,4-triazole per the method has a novel process route and a total molar yield of greater than 50%. The reaction is highly safe and easy to industrialize, and has a high yield, inexpensive costs, and relatively mild reaction conditions.

[HUANG, Zhining 黄志宁, ZHOU, Zhangtao 周章涛, YE, Weiping 叶伟平, PHILLIS, Andrew Toroa 费安杰, MI, Chenggen 米成根, YANG, Manxin 杨曼欣] No.3, Binhai 10th Road North, Petrochemical Area, Daya Bay, 中国广东省惠州市大亚湾石化区滨海十路北3号, Guangdong 516081Huizhou, Guangdong 516081 A method for synthesizing a key intermediate compound 1 of fexuprazan, which is a potassium ion competitive blocker. The method comprises using 2,4-difluorobenzylamine as a raw material, and sequentially conducting condensation reaction, benzyl protection, ring formation under basic conditions, methylation, deprotection, and the like to obtain a target product. The described method has a yield greater than 50% and has characteristics such as mild reaction conditions, low costs, and the like.

[PHILLIS, Andrew Toroa 费安杰, YE, Weiping 叶伟平, ZHOU, Zhangtao 周章涛, WANG, Hui 汪辉, WANG, Daogong 王道功, HAN, Xiaodong 韩小东, HUANG, Furen 黄富任, YU, Lu 于璐, WU, Chunlin 吴春林, YAN, Kailun 严凯伦, ZHANG, Yilin 张毅琳] {801, 8th Floor, Building 1, Shenzhen Biomedical Innovation Industrial Park, No.14, Jinhui Road, Kengzi Street, Pingshan District, 中国广东省深圳市坪山区坑梓街道金辉路14号深圳市生物医药产业园区1号楼8层801, Guangdong 518122Shenzhen, Guangdong 518122;CN CN(CN)(CN)} A method for synthesizing 4-Hydroxy-N,N,2-trimethylbenzimidazole-6-carboxamide. A route of the method is as follows: [Formula (I)-Formula (V)]. The method for synthesizing 4-Hydroxy-N,N,2-trimethylbenzimidazole-6-carboxamide of the present invention has the characteristics of a novel process route, cheap and easily-available raw materials, high chemical purity (greater than 99.0%), and easiness in production and scale-up.

[ZHOU, Zhangtao 周章涛, YE, Weiping 叶伟平, PHILLIS, Andrew Toroa 费安杰, WANG, Hui 汪辉, WANG, Daogong 王道功, HAN, Xiaodong 韩小东, HUANG, Furen 黄富任, YAN, Kailun 严凯伦, ZHANG, Yilin 张毅琳, WU, Chunlin 吴春林, YU, Lu 于璐] {801, 8th Floor, Building 1, Shenzhen Biomedical Innovation Industrial Park 中国广东省深圳市坪山区坑梓街道金辉路14号深圳市生物医药产业园区1号楼8层801, Guangdong 518122No.14, Jinhui Road, Kengzi Street, Pingshan DistrictShenzhen, Guangdong 518122;CN CN(CN)(CN)} Provided is a method for synthesizing 4-hydroxy-N,N,2-trimethylbenzimidazole-6-formamide. The method route is as shown in (I) below. The total molar yield of 4-hydroxy-N,N,2-trimethylbenzimidazole-6-formamide synthesized by using the method is greater than 70%.

[YE, Weiping 叶伟平, ZHOU, Hongyu 周宏宇, PHILLIS, Andrew Toroa 费安杰, WANG, Yang 王扬, WU, Jie 吴杰, FU, Li 傅利, LUO, Fuyuan 罗富元, LIN, Liujun 林柳君, ZHOU, Zhangtao 周章涛] {No.3, Binhai 10th Road North 中国广东省惠州市大亚湾石化区滨海十路北3号, Guangdong 516081Petrochemical Area, Daya BayHuizhou, Guangdong 516081;CN CN(CN)(CN)} A dynamic combined micro-channel continuous flow reactor, comprising a reaction tube, a rotating shaft (30), a first heat exchanger (10), a second heat exchanger (11), a coupler (60) and a driving device (70), wherein the reaction tube comprises a first-half reaction tube (20) and a second-half reaction tube (21); the inner diameter of the reaction tube is greater than the outer diameter of the rotating shaft (30), and the rotating shaft (30) is coaxially arranged inside the reaction tube; the driving device (70) is configured to be capable of driving the rotating shaft (30) to rotate relative to the reaction tube; and the first-half reaction tube (20) and the second-half reaction tube (21) are two half cylinders of the same shape and size, and are assembled together to form the reaction tube having a cylindrical space therein. A reactor pipeline has the same size as a common tubular reactor, and micro-reaction channels are formed in the reaction tube by means of baffle structures, which have recesses, on the tube inner wall and the rotating shaft (30), such that the mass and heat transfer efficiency of the tubular reactor is improved.

[YE, Weiping 叶伟平, ZHOU, Zhangtao 周章涛, PHILLIS, Andrew Toroa 费安杰, WANG, Hui 汪辉, WANG, Daogong 王道功, HAN, Xiaodong 韩小东, WU, Chunlin 吴春林, YU, Lu 于璐, HUANG, Furen 黄富任, YAN, Kailun 严凯伦, ZHANG, Yilin 张毅琳] {801, 8th Floor, Building 1, Shenzhen Biomedical Innovation Industrial Park 中国广东省深圳市坪山区坑梓街道金辉路14号深圳市生物医药产业园区1号楼8层801, Guangdong 518122No.14, Jinhui Road, Kengzi Street, Pingshan DistrictShenzhen, Guangdong 518122;CN CN(CN)(CN)} A method for synthesizing 4-hydroxy-N,N,2-trimethylbenzimidazole-6-carboxamide. The process comprises: a method of the present invention for synthesizing 4-hydroxy-N,N,2-trimethylbenzimidazole-6-carboxamide. The method has the characteristics of a novel process, inexpensive and easily obtainable raw materials, chemical purity greater than or equal to 99%, and ease in scaling production. A method for synthesizing 4-hydroxy-N,N,2-trimethylbenzimidazole-6-carboxamide. The process comprises: a method of the present invention for synthesizing 4-hydroxy-N,N,2-trimethylbenzimidazole-6-carboxamide. The method has the characteristics of a novel process, inexpensive and easily obtainable raw materials, chemical purity greater than or equal to 99%, and ease in scaling production.