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1. 发明授权

US4371699A Process for preparation of optically active N-mercaptoalkanoylamino acids 失效
标题翻译：光学活性N-巯基烷酰氨基酸的制备方法
公开(公告)号：US4371699A
公开(公告)日：1983-02-01
申请号：US214780
申请日：1980-12-09
申请人： Takehisa Ohashi , Masami Shimazaki , Kazunori Kan , Hideo Kondo , Kiyoshi Watanabe
发明人： Takehisa Ohashi , Masami Shimazaki , Kazunori Kan , Hideo Kondo , Kiyoshi Watanabe
IPC分类号： C07C51/60 , C07D207/16 , C07D211/60 , C07D277/06 , C07K5/078
CPC分类号： C07K5/06165 , C07C51/60 , C07D207/16 , C07D211/60 , C07D277/06
摘要： A process is disclosed wherein an optically active N-mercaptoalkanoylamino acid is prepared by(1) reacting an optically active .beta.-hydroxyalkanoic acid, with a halogenating reagent to prepare an optically active .beta.-haloalkanoyl halide(2) reacting the .beta.-haloalkanoyl halide with an amino acid to produce an optically active N-.beta.-haloalkanoylamino acid and(3) reacting the N-.beta.-haloalkanoylamino acid with a reagent capable of converting the halogen into the thiol group, the configuration of the formulas (II), (III), (IV), (V), and (VI) being retained in all the optically active compounds throughout the process to prepare the compound represented by formula (I). The product of the present invention, for example, N-(3-mercapto-2-D-methylpropanoyl)-L-proline inhibits the enzymatic conversion of angiotensin I into angiotensin II and therefore is useful for relieving angiotensin-related hypertension.
摘要翻译：公开了一种方法，其中光学活性N-巯基烷酰基氨基酸通过（1）使光学活性β-羟基链烷酸与卤化试剂反应制备光学活性β-卤代烷酰基卤化物（2）使β-卤代烷酰卤与氨基酸以产生光学活性的N-β-卤代烷酰基氨基酸和（3）使N-β-卤代烷酰基氨基酸与能够将卤素转化成硫醇基团的试剂反应，式（II），（III ），（IV），（V）和（VI）在整个过程中保留在所有光学活性化合物中以制备由式（I）表示的化合物。本发明的产物，例如N-（3-巯基-2-D-甲基丙酰基）-L-脯氨酸抑制血管紧张素I的酶促转化为血管紧张素II，因此可用于缓解血管紧张素相关的高血压。

2. 发明授权

US4384139A Process for preparation of an optically active .beta.-mercaptoalkanoic acid 失效
标题翻译：光学活性β-巯基链烷酸的制备方法
公开(公告)号：US4384139A
公开(公告)日：1983-05-17
申请号：US294028
申请日：1981-08-18
申请人： Takehisa Ohashi , Masami Shimazaki , Kenji Nomura , Kazunori Kan , Kiyoshi Watanabe
发明人： Takehisa Ohashi , Masami Shimazaki , Kenji Nomura , Kazunori Kan , Kiyoshi Watanabe
IPC分类号： C07B53/00 , C07B31/00 , C07C53/19 , C07C53/50 , C07C67/00 , C07C313/00 , C07C319/02 , C07C319/14 , C07C323/52 , C07C51/363
CPC分类号： C07C53/50 , C07C323/00 , C07C53/19
摘要： A process is disclosed wherein an optically active .beta.-mercaptoalkanoic acid represented by formula (I): ##STR1## wherein R.sub.1 is lower alkyl having from 1 to 4 carbon atoms, is prepared by(1) reacting an optically active .beta.-hydroxyalkanoic acid represented by formula (II): ##STR2## wherein R.sub.1 is the same as defined above, with a halogenating reagent to prepare an optically active .beta.-haloalkanoyl halide represented by formula (III): ##STR3## wherein X is halogen and R.sub.1 is the same as defined above; (2) reacting the .beta.-haloalkanoyl halide with water or an aqueous alkaline solution to prepare an optically active .beta.-haloalkanoic acid represented by formula (IV): ##STR4## wherein X and R.sub.1 are each the same as defined above, or a salt thereof, respectively; and(3) reacting the .beta.-haloalkanoic acid or the salt thereof with a reagent capable of converting the halogen into the thiol group, the configuration of the compound (II), (III), and (IV) being retained throughout the process to prepare the compound represented by formula (I). The product of the present invention is useful as an intermediate for preparation of an antihypertensive agent such as N-(3-mercapto-2-D-methylpropanoyl)-L-proline.
摘要翻译：公开了一种方法，其中式（I）表示的光学活性β-巯基链烷酸：其中R1是具有1-4个碳原子的低级烷基，其通过以下步骤制备：（1）使光学活性β- （II）表示的羟基链烷酸：其中R1与上述定义相同，与卤化试剂反应，制备式（III）表示的光学活性β-卤代烷酰基卤化物：（III）其中X是卤素且R 1与上述定义相同; （2）使β-卤代烷酰基卤化物与水或碱性水溶液反应以制备由式（Ⅳ）表示的光学活性β-卤代链烷酸：其中X和R 1各自与上述定义相同，或其盐; 和（3）使β-卤代烷酸或其盐与能够将卤素转化成硫醇基的试剂反应，化合物（II），（III）和（IV）的构型在整个过程中被保留制备由式（I）表示的化合物。本发明的产品可用作制备抗高血压药如N-（3-巯基-2-D-甲基丙酰基）-L-脯氨酸的中间体。

3. 发明授权

US4460780A Process for preparation of optically active thiol compounds 失效
标题翻译：光学活性硫醇化合物的制备方法
公开(公告)号：US4460780A
公开(公告)日：1984-07-17
申请号：US457377
申请日：1983-01-12
申请人： Takehisa Ohashi , Masami Shimazaki , Kenji Nomura , Yasushi Nose , Kiyoshi Watanabe
发明人： Takehisa Ohashi , Masami Shimazaki , Kenji Nomura , Yasushi Nose , Kiyoshi Watanabe
IPC分类号： C07D207/16 , C07D277/06
CPC分类号： C07D277/06 , C07D207/16
摘要： An improved process for preparation of an optically active N-(3-mercapto-2-D-methylpropanoyl)-L-amino acid represented by formula (I): ##STR1## from an N-(3-chloro-2-D-methylpropanoyl)-L-amino acid represented by formula (II): ##STR2## (Y in (I) and (II): CH.sub.2 or sulfur; Q in (II): hydrogen, Na, K or NH.sub.4),which is characterized by reacting the compound (II) with an alkali trithiocarbonate, of which the molar ratio to the compound (II) is not less than 1.5, in an aqueous medium at a temperature of from about 60.degree. C. to about 90.degree. C., and hydrolyzing the resulting product with an acid.It is preferable to use sodium trithiocarbonate as the alkali trithiocarbonate, mineral acid as the acid, or water or aqueous alcohol as an aqueous medium.
摘要翻译：由式（I）表示的光学活性N-（3-巯基-2-D-甲基丙酰基）-L-氨基酸的改进方法：从N-（3-氯-2 （II）表示的（ⅰ）和（II）中的Y：CH 2或硫;（II）中的Q：氢，Na，K或 NH4），其特征在于使化合物（II）与碱性三硫代碳酸酯反应，其中化合物（II）的摩尔比不小于1.5，在水介质中在约60℃至约60℃至约90℃，并用酸水解所得产物。优选使用三硫代碳酸钠作为碱式三硫代碳酸酯，无机酸作为酸，或水或含水醇作为水性介质。

4. 发明授权

US4310635A Fermentative production of D(-)-.beta.-hydroxyisobutyric acid 失效
标题翻译：发酵生产D（ - ） - β-羟基异丁酸
公开(公告)号：US4310635A
公开(公告)日：1982-01-12
申请号：US201337
申请日：1980-10-27
申请人： Junzo Hasegawa , Masahiro Ogura , Shigeki Hamaguchi , Masami Shimazaki , Hajime Kawaharada , Kiyoshi Watanabe
发明人： Junzo Hasegawa , Masahiro Ogura , Shigeki Hamaguchi , Masami Shimazaki , Hajime Kawaharada , Kiyoshi Watanabe
IPC分类号： C12P7/42
CPC分类号： C12P7/42 , Y10S435/911 , Y10S435/913 , Y10S435/917 , Y10S435/921 , Y10S435/938 , Y10S435/94 , Y10S435/942
摘要： A process is disclosed wherein D(-)-.beta.-hydroxyisobutyric acid is produced fermentatively from isobutyric acid or methacrylic acid by the stereoselective action of microorganisms having the ability to convert isobutyric acid or methacrylic acid into D(-)-.beta.-hydroxyisobutyric acid in an aqueous medium, and D(-)-.beta.-hydroxyisobutyric acid is recovered from the aqueous medium.
摘要翻译：公开了一种方法，其中通过具有将异丁酸或甲基丙烯酸转化为D（ - ） - β-羟基异丁酸的能力的微生物的立体选择性作用，从（异）酸或甲基丙烯酸发酵得到D（ - ） - β-羟基异丁酸）从水介质中回收水性介质和D（ - ） - β-羟基异丁酸。

5. 发明授权

US4163839A Isocoformycin and a process for the production thereof 失效
标题翻译：异青霉素及其制备方法
公开(公告)号：US4163839A
公开(公告)日：1979-08-07
申请号：US858928
申请日：1977-12-09
申请人： Hamao Umezawa , Tomio Takeuchi , Shinichi Kondo , Masami Shimazaki
发明人： Hamao Umezawa , Tomio Takeuchi , Shinichi Kondo , Masami Shimazaki
IPC分类号： C07H19/052 , C07H19/16 , C07H19/04 , A61K31/70
CPC分类号： C07H19/16 , C07H19/052
摘要： A novel, unique nucleoside, 3-.beta.-D-ribofuranosyl-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-7-ol, named isocoformycin, of the formula ##STR1## is provided by ring expansion of derivatives of 9-.beta.-D-ribofuranosyl-6-hydroxymethyl-1,6-dihydropurine. Isocoformycin markedly inhibits deaminating enzymes which inactivate formycin and adenine arabinoside (also known as ara-A and Vidarabine). Formycin and adenine arabinoside are used as antiviral and antitumor agents in mammals and birds and isocoformycin is advantageous to prolong the activity and effect of formycin and adenine arabinoside.
摘要翻译：一种新颖独特的核苷，3β-D-呋喃核糖基-3,6,7,8-四氢咪唑并[4,5-d] [1,3]二氮杂-醇，命名为异青霉素，式为“IMAGE” 由9-β-D-呋喃核糖基-6-羟甲基-1,6-二氢嘌呤衍生物的环扩展提供。异青霉素显着抑制脱氨酶，其使得霉菌和阿拉伯糖腺苷（也称为ara-A和阿糖腺苷）失活。霉菌素和阿拉伯糖腺苷在哺乳动物和鸟类中用作抗病毒和抗肿瘤剂，异青霉素有利于延长霉素和阿拉伯糖腺苷的活性和作用。

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