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公开(公告)号：US20120226049A1
公开(公告)日：2012-09-06
申请号：US13508952
申请日：2010-11-29
申请人： Kazuyuki Yamagata
发明人： Kazuyuki Yamagata
IPC分类号： C07D277/28
CPC分类号： C07D277/32
摘要： A method for producing 5-(aminomethyl)-2-chlorothiazole, which comprises the step of mixing a compound represented by formula (2): a mineral acid and a nitrite salt together.
摘要翻译： 一种生产5-（氨基甲基）-2-氯噻唑的方法，其包括将式（2）表示的化合物：无机酸和亚硝酸盐一起混合的步骤。
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公开(公告)号：US20090018364A1
公开(公告)日：2009-01-15
申请号：US12282479
申请日：2007-03-15
申请人： Kazuyuki Yamagata , Shinzo Seko
发明人： Kazuyuki Yamagata , Shinzo Seko
IPC分类号： C07C273/18
CPC分类号： C07C273/1854 , C07C2601/14 , C07C275/70
摘要： An object of the present invention is to industrially advantageously produce N-nitroisoureas or a salt thereof which is useful as a synthetic intermediate for pharmaceuticals and pesticides. The present invention relates to a process for producing a compound represented by the formula (2): wherein R1, R2 and R3 are as defined below, or a salt thereof, which comprises reacting a compound represented by the formula (1): wherein R1 represents an optionally substituted straight-chain or branched C1 to C6 alkyl group, R2 and R3 are the same or different and represent an optionally substituted straight-chain or branched C1 to C6 alkyl group, a cycloalkyl group or a substituted aryl group, or R2 and R3 simultaneously represent a hydrogen atom, or a salt thereof with a nitrating agent in the presence of sulfur trioxide.
摘要翻译： 本发明的目的是在工业上有利地生产N-硝基异脲或其盐，其可用作药物和农药的合成中间体。 本发明涉及由式（2）表示的化合物的制备方法：其中R1，R2和R3如下所定义，或其盐，其包括使式（1）表示的化合物：其中R1 表示任选取代的直链或支链C1至C6烷基，R2和R3相同或不同，表示任选取代的直链或支链C1至C6烷基，环烷基或取代的芳基或R2 和R3同时在三氧化硫的存在下与硝化剂一起代表氢原子或其盐。
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3.发明授权Cephem compound, its production and its use for producing cephem antibiotics 失效Cephem化合物，其生产及其用于生产头孢类抗生素的用途
公开(公告)号：US5708165A
公开(公告)日：1998-01-13
申请号：US273912
申请日：1994-07-12
IPC分类号： C07D501/16 , C07D501/00 , C07D501/04 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/56 , C07D501/46
CPC分类号： C07D501/00 , Y02P20/55
摘要： A 3-�(E)-1-propenyl!cephem compound represented by formula (I): ##STR1## wherein R represents hydrogen, a protective group for an amino group, or the group shown by formula (II): ##STR2## in which R.sup.3 is a protective group for an amino group, R.sup.4 is a protective group for a hydroxyl group, and W is --CH.dbd. or --N.dbd.; R.sup.2 represents a protective group for a carboxyl group; and X represents hydrogen or chlorine. The compound is useful as an intermediate for producing cephem antibiotics and is prepared by isomerizing the corresponding 3-�(Z)-1-propenyl!cephem compound in an inert organic solvent in the presence of an aromatic thiol. The compound of formula (I) wherein X is chlorine can be converted into a 3-�(E)-3-ammonio-1-propenyl!cephem derivative through the reaction with a tertiary amine.
摘要翻译： 由式（I）表示的3 - [（E）-1-丙烯基]头孢烯化合物：其中R表示氢，氨基保护基或式（II）所示的基团： （II）其中R3是氨基的保护基，R4是羟基的保护基，W是-CH =或-N =; R2表示羧基的保护基; X表示氢或氯。 该化合物可用作生产头孢类抗生素的中间体，并且通过在惰性有机溶剂中在芳族硫醇存在下使相应的3 - [（Z）-1-丙烯基]头孢烯化合物异构化而制备。 其中X为氯的式（I）化合物可通过与叔胺的反应转化为3 - [（E）-3-氨基-1-丙烯基]头孢烯衍生物。
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公开(公告)号：US08754235B2
公开(公告)日：2014-06-17
申请号：US13508952
申请日：2010-11-29
申请人： Kazuyuki Yamagata
发明人： Kazuyuki Yamagata
IPC分类号： C07D277/32
CPC分类号： C07D277/32
摘要： A method for producing 5-(aminomethyl)-2-chlorothiazole, which comprises the step of mixing a compound represented by formula (2): a mineral acid and a nitrite salt together.
摘要翻译： 一种生产5-（氨基甲基）-2-氯噻唑的方法，其包括将式（2）表示的化合物：无机酸和亚硝酸盐一起混合的步骤。
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5.发明授权Cephem compound, its production and its use for producing cephem antibiotics 失效Cephem化合物，其生产及其用于生产头孢类抗生素的用途
公开(公告)号：US5969131A
公开(公告)日：1999-10-19
申请号：US932835
申请日：1997-09-18
IPC分类号： C07D501/16 , C07D501/00 , C07D501/04 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/56
CPC分类号： C07D501/00 , Y02P20/55
摘要： A 3-[(E)-1-propenyl]cephem compound represented by formula (I): ##STR1## wherein R represents hydrogen, a protective group for an amino group, or the group shown by formula (II): ##STR2## in which R.sup.3 is a protective group for an amino group, R.sup.4 is a protective group for a hydroxyl group, and W is --CH.dbd. or --N.dbd.; R.sup.2 represents a protective group for a carboxyl group; and X represents hydrogen or chlorine. The compound is useful as an intermediate for producing cephem antibiotics and is prepared by isomerizing the corresponding 3-[(Z)-1-propenyl]cephem compound in an inert organic solvent in the presence of an aromatic thiol. The compound of formula (I) wherein X is chlorine can be converted into a 3-[(E)-3-ammonio-1-propenyl]cephem derivative through the reaction with a tertiary amine.
摘要翻译： 由式（I）表示的3 - [（E）-1-丙烯基]头孢烯化合物：其中R表示氢，氨基保护基或式（II）所示的基团：其中R3为保护基 氨基的基团，R4是羟基的保护基，W是-CH =或-N =; R2表示羧基的保护基; X表示氢或氯。 该化合物可用作生产头孢类抗生素的中间体，并且通过在惰性有机溶剂中在芳族硫醇存在下使相应的3 - [（Z）-1-丙烯基]头孢烯化合物异构化而制备。 其中X为氯的式（I）化合物可通过与叔胺的反应转化为3 - [（E）-3-氨基-1-丙烯基]头孢烯衍生物。
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