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1. 发明授权

US06376685B1 Process for producing optically active threo-3-amino-1,2-epoxy compounds 失效
标题翻译：光学活性苏氨酸-3-氨基-1,2-环氧化合物的制备方法
公开(公告)号：US06376685B1
公开(公告)日：2002-04-23
申请号：US09600215
申请日：2000-07-12
申请人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
发明人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
IPC分类号： C07D30102
CPC分类号： C07C303/28 , C07D303/36 , C07C309/66
摘要： Highly pure optically active threo-3-amino-1,2-epoxy compounds appropriate for materials for manufacturing drugs and a process for producing the same on an industrial scale. An optically active threo-3-amino-1,2-diol derivative is subjected in an organic solvent in the presence of a base to alkylsufonylation or arylsulfonylation to thereby give the corresponding optically active threo-3-amino-2-hydroxy-1-sulfonyloxy compound. Next, the resultant product is subjected to epoxidation in the presence of a base to give the corresponding optically active threo-3-amino-1,2-epoxy compound. The thus obtained epoxy compound is purified by using an organic solvent and water, thus giving a highly pure epoxy compound.
摘要翻译：适用于制造药物的材料的高纯度旋光活性苏氨酸-3-氨基-1,2-环氧化合物及其制备方法。光学活性的苏氨酸-3-氨基-1,2-二醇衍生物在碱的存在下在有机溶剂中进行烷基磺酰化或芳基磺酰化，得到相应的光学活性的苏氨酸-3-氨基-2-羟基-1- 磺酰氧基化合物。接着，将所得产物在碱的存在下进行环氧化，得到相应的光学活性的苏氨酸-3-氨基-1,2-环氧化合物。由此获得的环氧化合物通过使用有机溶剂和水进行纯化，从而得到高纯度的环氧化合物。

2. 发明授权

US06452026B1 Process for producing optically active threo-3-amino-1,2-epoxy compounds 失效
公开(公告)号：US06452026B1
公开(公告)日：2002-09-17
申请号：US09997875
申请日：2001-11-30
申请人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
发明人： Yukihiro Sagawa , Jouji Sekine , Hisao Sato
IPC分类号： C07D30102
CPC分类号： C07C303/28 , C07D303/36 , C07C309/66
摘要： Highly pure optically active threo-3-amino-1,2-epoxy compounds appropriate for materials for manufacturing drugs and a process for producing the same on an industrial scale. An optically active threo-3-amino-1,2-diol derivative is subjected in an organic solvent in the presence of a base to alkylsufonylation or arylsulfonylation to thereby give the corresponding optically active threo-3-amino-2-hydroxy-1-sulfonyloxy compound. Next, the resultant product is subjected to epoxidation in the presence of a base to give the corresponding optically active threo-3-amino-1,2-epoxy compound. The thus obtained epoxy compound is purified by using an organic solvent and water, thus giving a highly pure epoxy compound.

3. 发明授权

US5900503A Process for producing optically active cyanohydrins 失效
标题翻译：光学活性氰醇的制备方法
公开(公告)号：US5900503A
公开(公告)日：1999-05-04
申请号：US68605
申请日：1998-05-11
申请人： Yoshinobu Miyazawa , Taichi Koshigoe , Kouichi Ohkawa , Jouji Sekine , Shinichiro Saeki
发明人： Yoshinobu Miyazawa , Taichi Koshigoe , Kouichi Ohkawa , Jouji Sekine , Shinichiro Saeki
IPC分类号： C07C253/34 , C07C255/43 , C07C255/00
CPC分类号： C07C253/34 , C07B2200/07 , Y02P20/55
摘要： An optically active cyanohydrin represented by the following general formula (1): ##STR1## wherein each of R1 and R2 is a hydrogen atom or an amino-protecting group, and the configurations relating to the carbon atoms at the *2-position and *3-position are as follows: in the case of the carbon atom at the *2-position being in R-configuration, the carbon atom at the *3-position is in S-configuration, and in the case of the carbon atom at the *2-position being in S-configuration, the carbon atom at the *3-position is in R-configuration, can be efficiently produced by crystallizing one of the optically active cyanohydrins while treating a mixture of cyanohydrin diastereomers in the presence of an amine and an organic solvent to change the configuration relating to the carbon atom at the 2-position and thereby cause isomerization.
摘要翻译： PCT No.PCT / JP97 / 00319 Sec。 371日期：1998年5月11日 102（e）日期1998年5月11日PCT提交1997年2月7日PCT公布。公开号WO97 / 25082 日期：1997年8月14日由以下通式（1）表示的光学活性羟腈：其中R1和R2各自为氢原子或氨基保护基，并且与* 2位上的碳原子相关的构型和* 3位如下：在*构型的* 2位的碳原子的情况下，* 3位的碳原子为S构型，在碳的情况下在*构型的* 2位上的原子是3-构型的碳原子，可以通过使光学活性的氰醇中的一种结晶化，同时在存在的条件下处理氰醇非对映异构体的混合物的胺和有机溶剂，以改变与2-位上的碳原子相关的构型，从而引起异构化。

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