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1. 发明授权

US10138224B2 Preparation method of rociletinib 有权
公开(公告)号：US10138224B2
公开(公告)日：2018-11-27
申请号：US15952202
申请日：2018-04-12
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong Xu
IPC分类号： C07D239/48 , C07D403/12
摘要： Disclosed is a method for preparing Rociletinib. 2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5 -(trifluoromethyl)-pyrimidin-4-one is obtained by means of a condensation reaction of easily obtainable raw materials 5-(trifluoromethyl)uracil and 4-(4-acetylpiperazin-1-yl)-2-methoxyaniline, an intermediate is subjected to a halogenation reaction and an amination reaction to produce Rociletinib (I). The preparation method has easily obtainable raw materials, a simple process, is economic and environmentally friendly, and is suitable for industrial production.

2. 发明授权

US10039775B2 Preparation method for antitumor drug AP26113 有权
公开(公告)号：US10039775B2
公开(公告)日：2018-08-07
申请号：US15822092
申请日：2017-11-24
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong Xu
IPC分类号： A61K31/675 , C07F9/6558
摘要： Disclosed is a preparation method for an antitumor drug AP26113 (I). The method comprises the following preparation steps: cyclizing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and N,N-dimethylamino acrylate, condensing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and 4-(dimethyl phosphitylate)aniline, and chlorinating N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and a chlorinating agent, sequentially, so as to prepare AP26113 (I). The preparation method adopts easily-obtained raw materials, causes few side reactions, and is economical, environmentally friendly, and suitable for industrial production.

3. 发明授权

US09688685B2 Method for preparing volasertib and intermediate thereof 有权
公开(公告)号：US09688685B2
公开(公告)日：2017-06-27
申请号：US15361248
申请日：2016-11-25
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong Xu
IPC分类号： C07D475/04 , C07D487/04 , C07D475/00 , C07D295/135
CPC分类号： C07D487/04 , C07D295/135 , C07D475/00
摘要： Disclosed is a method for preparing Volasertib (I), comprising the following steps: an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) is nucleophilically substituted with an intermediate N-[trans-4-[4-(cylopropylmethyl)-1-piperazinyl]cyclohexyl]-4-halo-3-methoxylbenzamide (III), so as to prepare Volasertib (I). The preparation method has a simple process, mild conditions and few side effects, which meets the requirements for industrial enlargement. In addition, also disclosed are an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) and an intermediate N-[trans-4-[4-(cylopropylmethyl)-1-piperazinyl]cyclohexyl]-4-halo-3-methoxylbenza-mide (III) of Volasertib and the preparation methods thereof.

4. 发明申请

US20180230133A1 Preparation Method of Rociletinib 审中-公开
公开(公告)号：US20180230133A1
公开(公告)日：2018-08-16
申请号：US15952202
申请日：2018-04-12
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong XU
IPC分类号： C07D403/12
CPC分类号： C07D403/12 , C07D239/48
摘要： Disclosed is a method for preparing Rociletinib. 2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5 -(trifluoromethyl)-pyrimidin-4-one is obtained by means of a condensation reaction of easily obtainable raw materials 5-(trifluoromethyl)uracil and 4-(4-acetylpiperazin-1-yl)-2-methoxyaniline, an intermediate is subjected to a halogenation reaction and an amination reaction to produce Rociletinib (I). The preparation method has easily obtainable raw materials, a simple process, is economic and environmentally friendly, and is suitable for industrial production.

5. 发明申请

US20170174625A1 PREPARATION METHOD OF NINTEDANIB 有权
公开(公告)号：US20170174625A1
公开(公告)日：2017-06-22
申请号：US15453892
申请日：2017-03-08
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong XU
IPC分类号： C07D209/34
CPC分类号： C07D209/34
摘要： Disclosed is a preparation method of nintedanib (I), comprising the following steps: carrying out a condensation reaction on 4-(R acetate-2-yl)-3-nitrobenzoate (II) and trimethyl orthobenzoate to obtain (E)-4-[(2-methoxybenzylidene) R acetate-2-yl]-3-nitrobenzoate (III); carrying out a substitution reaction on the compound (EI) and N-(4-aminophenyl)-N-methyl-2-(4-methyl piperazine-1-yl) acetamide (IV) under the action of an acid-binding agent to generate (Z)-4-{[2-(N-methyl-2-(4-methyl piperazine-1-yl) acetamido-aniline) benzylidene] R acetate-2-yl}-3-nitrobenzoate (V); and sequentially carrying out reduction reactions and cyc-lization reactions on the compound (V) to prepare the nintedanib (I). The preparation method has an easily obtained raw material and a simple process, is economical and environmentally friendly, and is suitable for industrial production.

6. 发明申请

US20170073350A1 Method for Preparing Volasertib and Intermediate thereof 有权
标题翻译：挥发性胆固醇及其中间体的制备方法
公开(公告)号：US20170073350A1
公开(公告)日：2017-03-16
申请号：US15361248
申请日：2016-11-25
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong XU
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D295/135 , C07D475/00
摘要： Disclosed is a method for preparing Volasertib (I), comprising the following steps: an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) is nucleophilically substituted with an intermediate N-[trans-4-[4-(cylopropylmethyl)-1-piperazinyl]cyclohexyl]-4-halo-3-methoxylbenzamide (III), so as to prepare Volasertib (I). The preparation method has a simple process, mild conditions and few side effects, which meets the requirements for industrial enlargement. In addition, also disclosed are an intermediate 2-amino-7-ethyl-7,8-dihydro-5-methyl-8-isopropyl-(7R)-6(5H)-pteridinone (II) and an intermediate N-[trans-4-[4-(cylopropylmethyl)-1-piperazinyl]cyclohexyl]-4-halo-3-methoxylbenza-mide (III) of Volasertib and the preparation methods thereof.
摘要翻译：公开了一种制备Volasertib（I）的方法，包括以下步骤：中间体2-氨基-7-乙基-7,8-二氢-5-甲基-8-异丙基 - （7R）-6（5H） - 蝶啶酮（II）用中间体N- [反式-4- [4-（环丙基甲基）-1-哌嗪基]环己基] -4-卤代-3-甲氧基苯甲酰胺（III）进行亲核取代，以制备Volasertib（I）。制备方法工艺简单，条件温和，副作用少，符合工业化扩大要求。此外，还公开了中间体2-氨基-7-乙基-7,8-二氢-5-甲基-8-异丙基 - （7R）-6（5H） - 蝶啶酮（II）和中间体N- [反式 4- [4-（环丙基甲基）-1-哌嗪基]环己基] -4-卤代-3-甲氧基苯并二氮（III）及其制备方法。

7. 发明申请

US20160264584A1 Method for Preparing Ibrutinib 有权
标题翻译： Ibrutinib的制备方法
公开(公告)号：US20160264584A1
公开(公告)日：2016-09-15
申请号：US15159600
申请日：2016-05-19
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong Xu
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Provided is a method for preparing Ibrutibin (I), and steps of preparing same comprise: 4-benzyloxybenzoyl chloride (II) is used as a raw material, condensation and methoxidation reactions occur among 4-benzyloxybenzoyl chloride (II), malononitrile, and dimethyl sulfate to generate 4-benzyloxyphenyl(methoxy)vinylidenedicyanomethane (III), pyrazole cyclization occurs between the intermediate (III) and 1-(3R-hydrazino-1-piperidino)-2-propylene-1-ketone (IV) to acquire 1-[(3R)-[3-(4-benzyloxyphenyl)-4-nitrile-5 -amino-1H-pyrazole]-1-piperidino]-2 propylene-1-ketone (V), and pyrimidine cyclization occurs between an intermediate (V) and a cyclizing agent to prepare Ibrutinib (I). In the preparation method, the raw material is readily available, and the process is simple, economical, environmentally friendly, and is suitable for industrial production.
摘要翻译：本发明提供Ibrutibin（I）的制备方法，其制备方法包括：使用4-苄氧基苯甲酰氯（II）作为原料，在4-苄氧基苯甲酰氯（II），丙二腈和二甲基甲酰胺中发生缩合和甲氧化反应硫酸盐以产生4-苄氧基苯基（甲氧基）亚乙烯基二甲基甲烷（III），在中间体（III）和1-（3R-肼基-1-哌啶子基）-2-丙烯-1-酮（IV）之间发生吡唑环化， [（3R） - [3-（4-苄氧基苯基）-4-腈-5-氨基-1H-吡唑] -1-哌啶子基] -2丙烯-1-酮（V），嘧啶环化发生在中间体 V）和环化剂以制备Ibrutinib（I）。在制备方法中，原料易于获得，工艺简单，经济，环保，适用于工业生产。

8. 发明申请

US20180093950A1 RIBOCICLIB INTERMEDIATE AND PREPARATION METHOD THEREFOR 有权
公开(公告)号：US20180093950A1
公开(公告)日：2018-04-05
申请号：US15821754
申请日：2017-11-22
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong XU
IPC分类号： C07D207/36 , C07D471/04
CPC分类号： C07D207/36 , C07D471/04 , C07D487/04
摘要： Disclosed are an intermediate N-cyclopentyl-2-methoxy-5-(N,N-dimethyl-formamido)-3-pyrrylformonitrile (II) for preparing ribociclib and a preparation method therefor. The preparation method comprises the following preparation steps: carrying out halogenating reaction on N,N-dimethyl-2-carbonyl-propanamide (IV) to obtain N,N-dimethyl-1-halo-2-carbonyl-propanamide (V); carrying out substitution reaction on the intermediate (V) and malononitrile to prepare N,N-dimethyl-1,1-dicyano-3-carbonyl-butyramide (VI); carrying out cyclization reaction on the intermediate (VI) to prepare 2-methoxy-5-(N,N-dimethyl-formamido)-3-pyrrylformonitrile (VII); and carrying out coupling reaction on the intermediate (VII) and bromocyclopentane to obtain the intermediate N-cyclopentyl-2-methoxy-5-(N,N-dimethyl-formanido)-3-pyrrylformonitrile (II) for preparing ribociclib. The intermediate (II) and N-[5-(1-piperazino)-2-piperidyl]guanidine (III) are subjected to condensation reaction to prepare ribociclib. The preparation method has the advantages of accessible raw materials, simple process, high economy and environmental friendliness, and is suitable for industrial production.

9. 发明申请

US20180071324A1 PREPARATION METHOD FOR ANTITUMOR DRUG AP26113 审中-公开
公开(公告)号：US20180071324A1
公开(公告)日：2018-03-15
申请号：US15822092
申请日：2017-11-24
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
发明人： Xuenong XU
IPC分类号： A61K31/675
CPC分类号： A61K31/675 , C07F9/6558 , C07F9/65583
摘要： Disclosed is a preparation method for an antitumor drug AP26113 (I). The method comprises the following preparation steps: cyclizing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and N,N-dimethylamino acrylate, condensing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and 4-(dimethyl phosphitylate)aniline, and chlorinating N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and a chlorinating agent, sequentially, so as to prepare AP26113 (I). The preparation method adopts easily-obtained raw materials, causes few side reactions, and is economical, environmentally friendly, and suitable for industrial production.

10. 发明授权

US09845315B2 Method for preparing Afatinib and intermediate thereof 有权
公开(公告)号：US09845315B2
公开(公告)日：2017-12-19
申请号：US14957607
申请日：2015-12-03
申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD. , Xuenong Xu
发明人： Xuenong Xu
IPC分类号： C07D405/12 , C07D307/20
CPC分类号： C07D405/12 , C07D307/20
摘要： Revealed in the present invention is a method for preparing Afatinib (I): using 2-nitrile-4-[4-(N,N-dimethylamino-1-oxo-2-buten-l-yl]amino-5-[(S)-(tetrahydrofuran-3-yl)oxy]aniline (II) and 4-fluoro-3-chloroaniline (III) as starting materials, and respectively performing a condensation and cyclization reaction with N,N-dimethylformamide dimethylacetal (IV) to prepare Afatinib (I), wherein the method significantly reduces the manufacturing steps of Afatinib and greatly lower the costs. In addition, also provided in the present invention is a method for preparing an intermediate of Afatinib, wherein the method has a stable process, uses readily available starting materials, has a low cost, and all the reactions are classic reactions, suitable for meeting amplification requirements in the industry.

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