专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US09061991B2 Method for producing 1-amino-1-alkoxycarbonyl-2-vinylcyclopropane 有权
标题翻译： 1-氨基-1-烷氧基羰基-2-乙烯基环丙烷的制备方法
公开(公告)号：US09061991B2
公开(公告)日：2015-06-23
申请号：US13579045
申请日：2011-02-16
申请人： Yuuki Asuma , Tatsuya Suzuki , Jun Takehara , Tsugihiko Hidaka , Kuniko Asada , Ryoma Miyake , Yasumasa Dekishima , Hiroshi Kawabata
发明人： Yuuki Asuma , Tatsuya Suzuki , Jun Takehara , Tsugihiko Hidaka , Kuniko Asada , Ryoma Miyake , Yasumasa Dekishima , Hiroshi Kawabata
IPC分类号： C07C1/32 , C07C13/04 , C07C67/343 , C07B53/00 , C07B57/00 , C07C67/313 , C07C227/04 , C07C227/32 , C07C269/02 , C07C247/22 , C12P41/00 , C12P7/62
CPC分类号： C07C67/343 , C07B53/00 , C07B57/00 , C07B2200/07 , C07C67/313 , C07C227/04 , C07C227/32 , C07C247/22 , C07C269/02 , C07C2601/02 , C12P7/62 , C12P41/005 , C07C69/743 , C07C229/48 , C07C271/24
摘要： It is an object of the present invention to provide a novel method for producing (1R,2S)/(1S,2R)-1-amino-1-alkoxycarbonyl-2-vinylcyclopropane which is useful as a synthetic intermediate of therapeutic agents for hepatitis C and a synthetic intermediate thereof. According to the present invention, when a trans-2-butene derivative having a leaving group at each of the 1- and 4-positions is reacted with a malonic ester in the presence of a base, a specific amount of an alkali metal alkoxide or an alkali metal hydride is used as the base, and further a specific amount of a malonic ester is used to produce a cyclopropane diester, and further, chiral or achiral 1-amino-1-alkoxy-carbonyl-2-vinylcyclopropane and a salt thereof are synthesized using the cyclopropane diester.
摘要翻译：本发明的目的是提供一种制备（1R，2S）/（1S，2R）-1-氨基-1-烷氧基羰基-2-乙烯基环丙烷的新方法，其可用作肝炎治疗剂的合成中间体 C及其合成中间体。根据本发明，当在碱存在下使具有1位和4位的离去基团的反式-2-丁烯衍生物与丙二酸酯反应时，将特定量的碱金属醇盐或使用碱金属氢化物作为碱，进一步使用特定量的丙二酸酯来制备环丙烷二酯，此外，手性或非手性1-氨基-1-烷氧基 - 羰基-2-乙烯基环丙烷及其盐使用环丙烷二酯合成。

2. 发明申请

US20130130338A1 NOVEL HYDROLASE PROTEIN 有权
标题翻译：新型水解蛋白
公开(公告)号：US20130130338A1
公开(公告)日：2013-05-23
申请号：US13813047
申请日：2011-08-31
申请人： Hiroshi Kawabata , Ryoma Miyake , Kuniko Asada , Ryouhei Katou
发明人： Hiroshi Kawabata , Ryoma Miyake , Kuniko Asada , Ryouhei Katou
IPC分类号： C12N9/14 , C12P7/62
CPC分类号： C12P7/62 , C12N9/14 , C12N9/18 , C12P41/005 , Y02P20/52
摘要： It is an object of the present invention to provide a novel hydrolase, which is used when dialkyl 2-vinylcyclopropane-1,1-dicarboxylate is hydrolyzed with an enzyme, so as to efficiently obtain (1S,2S)-1-alkoxycarbonyl-2-vinylcyclopropanecarboxylic acid that is useful as an intermediate for synthesizing therapeutic agents for hepatitis C. According to the present invention, there is provided a hydrolase protein, which consists of the amino acid sequence shown in any one of SEQ ID NOS. 2 to 5 and which has activity of catalyzing, at higher selectivity than the protein consisting of the amino acid sequence shown in SEQ ID NO. 1, a reaction of producing (1S,2S)-1-ethoxycarbonyl-2-vinylcyclopropanecarboxylic acid from diethyl 2-vinylcyclopropane-1,1-dicarboxylate.
摘要翻译：本发明的一个目的是提供一种新的水解酶，其在2-乙烯基环丙烷-1,1-二羧酸二烷基酯用酶水解时使用，以有效地获得（1S，2S）-1-烷氧基羰基-2 - 乙烯基环丙烷羧酸，其可用作合成丙型肝炎治疗剂的中间体。根据本发明，提供了水解酶蛋白质，其由SEQ ID NOS中任一项所示的氨基酸序列组成。 2至5，并且其具有以比由SEQ ID NO。所示的氨基酸序列组成的蛋白质更高的选择性催化的活性。 1，由2-乙烯基环丙烷-1,1-二羧酸二乙酯生成（1S，2S）-1-乙氧基羰基-2-乙烯基环丙烷羧酸的反应。

3. 发明授权

US09029107B2 Hydrolase protein 有权
标题翻译：水解酶蛋白
公开(公告)号：US09029107B2
公开(公告)日：2015-05-12
申请号：US13813047
申请日：2011-08-31
申请人： Hiroshi Kawabata , Ryoma Miyake , Kuniko Asada , Ryouhei Katou
发明人： Hiroshi Kawabata , Ryoma Miyake , Kuniko Asada , Ryouhei Katou
IPC分类号： C12N9/14 , C12P7/62 , C12N9/18 , C12P41/00
CPC分类号： C12P7/62 , C12N9/14 , C12N9/18 , C12P41/005 , Y02P20/52
摘要： It is an object of the present invention to provide a novel hydrolase, which is used when dialkyl 2-vinylcyclopropane-1,1-dicarboxylate is hydrolyzed with an enzyme, so as to efficiently obtain (1S,2S)-1-alkoxycarbonyl-2-vinylcyclopropanecarboxylic acid that is useful as an intermediate for synthesizing therapeutic agents for hepatitis C. According to the present invention, there is provided a hydrolase protein, which consists of the amino acid sequence shown in any one of SEQ ID NOS. 2 to 5 and which has activity of catalyzing, at higher selectivity than the protein consisting of the amino acid sequence shown in SEQ ID NO. 1, a reaction of producing (1S,2S)-1-ethoxycarbonyl-2-vinylcyclopropanecarboxylic acid from diethyl 2-vinylcyclopropane-1,1-dicarboxylate.
摘要翻译：本发明的一个目的是提供一种新的水解酶，其在2-乙烯基环丙烷-1,1-二羧酸二烷基酯用酶水解时使用，以有效地获得（1S，2S）-1-烷氧基羰基-2 - 乙烯基环丙烷羧酸，其可用作合成丙型肝炎治疗剂的中间体。根据本发明，提供了水解酶蛋白质，其由SEQ ID NOS中任一项所示的氨基酸序列组成。 2至5，并且其具有以比由SEQ ID NO。所示的氨基酸序列组成的蛋白质更高的选择性催化的活性。 1，由2-乙烯基环丙烷-1,1-二羧酸二乙酯生成（1S，2S）-1-乙氧基羰基-2-乙烯基环丙烷甲酸的反应。

4. 发明申请

US20130096339A1 METHOD FOR PRODUCING 1-AMINO-1-ALKOXYCARBONYL-2-VINYLCYCLOPROPANE 有权
标题翻译： 1-氨基-1-烷氧羰基-2-乙烯基环戊二烯的制备方法
公开(公告)号：US20130096339A1
公开(公告)日：2013-04-18
申请号：US13579045
申请日：2011-02-16
申请人： Yuuki Asuma , Tatsuya Suzuki , Jun Takehara , Tsugihiko Hidaka , Kuniko Asada , Ryoma Miyake , Yasumasa Dekishima , Hiroshi Kawabata
发明人： Yuuki Asuma , Tatsuya Suzuki , Jun Takehara , Tsugihiko Hidaka , Kuniko Asada , Ryoma Miyake , Yasumasa Dekishima , Hiroshi Kawabata
IPC分类号： C07C67/343
CPC分类号： C07C67/343 , C07B53/00 , C07B57/00 , C07B2200/07 , C07C67/313 , C07C227/04 , C07C227/32 , C07C247/22 , C07C269/02 , C07C2601/02 , C12P7/62 , C12P41/005 , C07C69/743 , C07C229/48 , C07C271/24
摘要： It is an object of the present invention to provide a novel method for producing (1R,2S)/(1S,2R)-1-amino-1-alkoxycarbonyl-2-vinylcyclopropane which is useful as a synthetic intermediate of therapeutic agents for hepatitis C and a synthetic intermediate thereof. According to the present invention, when a trans-2-butene derivative having a leaving group at each of the 1- and 4-positions is reacted with a malonic ester in the presence of a base, a specific amount of an alkali metal alkoxide or an alkali metal hydride is used as the base, and further a specific amount of a malonic ester is used to produce a cyclopropane diester, and further, chiral or achiral 1-amino-1-alkoxy-carbonyl-2-vinylcyclopropane and a salt thereof are synthesized using the cyclopropane diester.
摘要翻译：本发明的目的是提供一种制备（1R，2S）/（1S，2R）-1-氨基-1-烷氧基羰基-2-乙烯基环丙烷的新方法，其可用作肝炎治疗剂的合成中间体 C及其合成中间体。根据本发明，当在碱存在下使具有1位和4位的离去基团的反式-2-丁烯衍生物与丙二酸酯反应时，将特定量的碱金属醇盐或使用碱金属氢化物作为碱，进一步使用特定量的丙二酸酯来制备环丙烷二酯，此外，手性或非手性1-氨基-1-烷氧基 - 羰基-2-乙烯基环丙烷及其盐使用环丙烷二酯合成。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式