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1. 发明授权

US6028217A Optically active salts of 2-hydroxymethyl-3-phenylpropionic acid with cis-1-amino-2-indanol, .alpha.-methylbenzylamine, or 3-methyl-2-phenyl-1-butylamine 失效
标题翻译： 2-羟甲基-3-苯基丙酸与顺式-1-氨基-2-茚满醇，α-甲基苄胺或3-甲基-2-苯基-1-丁胺的光学活性盐
公开(公告)号：US6028217A
公开(公告)日：2000-02-22
申请号：US166124
申请日：1998-10-05
申请人： Hiroyuki Nohira , Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
发明人： Hiroyuki Nohira , Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
IPC分类号： C07B57/00 , C07C51/487 , C07C59/48 , C07C211/27 , C07C215/44 , C07B55/00
CPC分类号： C07C215/44 , C07C211/27 , C07C51/487 , C07C59/48
摘要： A compound selected from the group consisting of(a) optically active 2-hydroxymethyl-3-phenylpropionic acid cis-1-amino-2-indanol salt,(b) optically active 2-hydroxymethyl-3-phenylpropionic acid .alpha.-methylbenzylamine salt,(c) optically active 2-hydroxymethyl-3-phenylpropionic acid 3-methyl-2-phenyl-1-butylamine salt,(d) a salt of (S)-2-hydroxymethyl-3-phenylpropionic acid with (1R, 2S)-(+)-cis-1-amino-2-indanol,(e) a salt of (R)-2-hydroxymethyl-3-phenylpropionic acid with (1S, 2R)-(-)-cis-1-amino-2-indanol,(f) a salt of (R)-2-hydroxymethyl-3-phenylpropionic acid with (S)-(-)-.alpha.-methylbenzylamine,(g) a salt of (S)-2-hydroxymethyl-3-phenylpropionic acid with (R)-(+)-.alpha.-methylbenzylamine,(h) a salt of (S)-2-hydroxymethyl-3-phenylpropionic acid with (S)-(-)-3-methyl-2-phenyl-1-butylamine, and(i) a salt of (R)-2-hydroxymethyl-3-phenylpropionic acid with (R)-(+)-3-methyl-2-phenyl-1-butylamine.
摘要翻译：选自（a）光学活性2-羟甲基-3-苯基丙酸顺式-1-氨基-2-二氢化茚醇盐，（b）光学活性2-羟甲基-3-苯基丙酸α-甲基苄基胺盐的化合物，（c）光学活性的2-羟甲基-3-苯基丙酸3-甲基-2-苯基-1-丁胺盐，（d）（S）-2-羟甲基-3-苯基丙酸与（1R，2S）（±） - 顺式-1-氨基-2-茚满醇，（e）（R）-2-羟甲基-3-苯基丙酸与（1S，2R） - （ - ） - 顺式-1-氨基-2- （R）-2-羟甲基-3-苯基丙酸与（S） - （ - ） - α-甲基苄胺的盐，（g）（S）-2-羟甲基-3 （（R） - （+） - α-甲基苄基胺，（h）（S）-2-羟甲基-3-苯基丙酸与（S） - （ - ） - 3-甲基-2-苯基 -1-丁胺，和（i）（R）-2-羟甲基-3-苯基丙酸与（R） - （+） - 3-甲基-2-苯基-1-丁基胺的盐。

2. 发明授权

US6093846A Process for preparing optically active 2-hydroxy-methyl-3-phenylpropionic acid 失效
标题翻译：光学活性2-羟基 - 甲基-3-苯基丙酸的制备方法
公开(公告)号：US6093846A
公开(公告)日：2000-07-25
申请号：US450740
申请日：1999-11-30
申请人： Hiroyuki Nohira , Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
发明人： Hiroyuki Nohira , Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
IPC分类号： C07B57/00 , C07C51/487 , C07C59/48 , C07C211/27 , C07C215/44
CPC分类号： C07C215/44 , C07C211/27 , C07C51/487 , C07C59/48
摘要： A process for preparing optically active 2-hydroxymethyl-3-phenylpropionic acid by resolving (RS)-2-hydroxymethyl-3-phenylpropionic acid via crystallization of an optically active amine salt, where the amine is optically active cis-1-amino-2-indanol salt, optically active .alpha.-methylbenzylamine salt, or optically active 3-methyl-2-phenyl-1-butylamine salt.
摘要翻译：通过用光学活性胺盐的结晶拆分（RS）-2-羟甲基-3-苯基丙酸来制备光学活性的2-羟甲基-3-苯基丙酸的方法，其中胺是光学活性的顺式-1-氨基-2 - 茚满盐，光学活性α-甲基苄胺盐或光学活性3-甲基-2-苯基-1-丁胺盐。

3. 发明授权

US6031121A Method for producing optically active phenylpropionic acid derivative 失效
公开(公告)号：US6031121A
公开(公告)日：2000-02-29
申请号：US249848
申请日：1999-02-16
申请人： Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
发明人： Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
IPC分类号： C07C303/28 , C07C309/66 , C07C309/73 , C07C327/32 , C07C327/20
CPC分类号： C07C327/32 , C07C303/28
摘要： Optically active N-(S-2-acetylthiomethyl-1-oxo-3-phenylpropyl)-glycine benzyl ester useful as an enkephalin inhibitory agent or ACE inhibitory agent can be produced at low cost in an industrial manner, by a method comprising subjecting optically active 2-hydroxymethyl-3-phenylpropionic acid and glycine benzyl ester to condensation to subsequently convert the hydroxyl group into an elimination group, and substituting the elimination group with an acetylthio group.

4. 发明授权

US06242635B1 Process for producing propionic acid derivatives 失效
标题翻译：丙酸衍生物的制备方法
公开(公告)号：US06242635B1
公开(公告)日：2001-06-05
申请号：US09156900
申请日：1998-09-18
申请人： Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
发明人： Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
IPC分类号： C07C6700
CPC分类号： C07C67/333 , C07C51/09 , C07C51/36 , C07C51/367 , C07C67/303 , C07C67/31 , C07C67/343 , C07C59/48 , C07C69/732
摘要： A process for producing a 2-aralkyl-3-hydroxypropionic acid (or its ester), comprising the steps of: reacting a 3-hydroxy-2-methylene-3-arylpropionic acid ester, easily obtained by the reaction of an arylaldehyde with an acrylic acid ester, with an acid anhydride to form a 2-aralkylidene-3-acyloxypropionic acid ester; subjecting the same to hydrolysis or alcoholysis; and reducing the resulting 2-aralkylidene-3-hydroxypropionic acid or its ester. The reduction step may be conducted in the presence of a base.
摘要翻译：一种2-芳烷基-3-羟基丙酸（或其酯）的制备方法，包括以下步骤：将通过芳基醛反应容易得到的3-羟基-2-亚甲基-3-芳基丙酸酯与丙烯酸酯与酸酐反应形成2-芳烷叉-3-酰氧基丙酸酯; 使其同时进行水解或醇解; 并减少所得2-亚烷基-3-羟基丙酸或其酯。还原步骤可以在碱的存在下进行。

5. 发明授权

US06339170B2 Method for producing optically active phenylpropionic acid derivative 失效
标题翻译：光学活性苯丙酸衍生物的制备方法
公开(公告)号：US06339170B2
公开(公告)日：2002-01-15
申请号：US09811592
申请日：2001-03-20
申请人： Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
发明人： Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
IPC分类号： C07C22900
CPC分类号： C07C327/32 , C07C303/28 , C07C309/73 , C07C309/66
摘要： Optically active N-(S-2-acetylthiomethyl-1-oxo-3-phenylpropyl)-glycine benzyl ester useful as an enkephalin inhibitory agent or ACE inhibitory agent can be produced at low cost in an industrial manner, by a method comprising subjecting optically active 2-hydroxymethyl-3-phenylpropionic acid and glycine benzyl ester to condensation to subsequently convert the hydroxyl group into an elimination group, and substituting the elimination group with an acetylthio group.
摘要翻译：用作脑啡肽抑制剂或ACE抑制剂的光学活性N-（S-2-乙酰硫基甲基-1-氧代-3-苯基丙基） - 甘氨酸苄酯可以通过工业方式以低成本，通过光学活性2-羟甲基-3-苯基丙酸和甘氨酸苄酯缩合，随后将羟基转化为消除基团，并用乙酰硫基代替消除基团。

6. 发明授权

US06570039B2 Process for producing &agr;-aminoketones 失效
公开(公告)号：US06570039B2
公开(公告)日：2003-05-27
申请号：US09943361
申请日：2001-08-31
申请人： Tomoyuki Onishi , Naoko Hirose , Takayuki Suzuki , Takashi Nakano , Masakazu Nakazawa , Kunisuke Izawa
发明人： Tomoyuki Onishi , Naoko Hirose , Takayuki Suzuki , Takashi Nakano , Masakazu Nakazawa , Kunisuke Izawa
IPC分类号： C07C20974
CPC分类号： C07D263/04 , C07B2200/07 , C07C213/00 , C07C221/00 , C07C269/06 , C07D263/18 , C07D263/20 , C07D301/26 , C07C215/08 , C07C225/16 , C07C271/16 , C07C271/18
摘要： A process for producing &agr;-aminohalomethyl ketones or N-protected &agr;-aminohalomethyl ketones from specified 3-oxazolidin-5-one derivatives via 5-halomethyl-5-hydroxy-3-oxazolidine derivatives. By this process, &agr;-aminohalomethyl ketones and compounds relating to them can be obtained efficiently and economically in industrial scale.

7. 发明授权

US06169200A Method for producing &agr;-hydroxy-&bgr;-aminocarboxylic acids 失效
标题翻译： α-羟基-β-氨基羧酸的制备方法
公开(公告)号：US06169200A
公开(公告)日：2001-01-02
申请号：US09186272
申请日：1998-11-05
申请人： Takayuki Suzuki , Yutaka Honda , Kunisuke Izawa
发明人： Takayuki Suzuki , Yutaka Honda , Kunisuke Izawa
IPC分类号： C07C31728
CPC分类号： C07C323/29 , C07C317/28 , C07C327/30
摘要： The present invention provides a simple and inexpensive method for producing &agr;-hydroxy-&bgr;-aminocarboxylic acids and their esters. An ester of an N-protected &agr;-amino acid ester is converted into a &bgr;-ketosulfoxide, which is then processed with an acid to give an &agr;-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected &agr;-acyloxy-&bgr;-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce &agr;-hydroxy-&bgr;-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.
摘要翻译：本发明提供了用于生产α-羟基-β-氨基羧酸及其酯的简单和便宜的方法。将N-保护的α-氨基酸酯的酯转化为β-氧亚砜，然后用酸处理给予α-酮基咪唑。接下来，将其进行酰化，然后用碱处理，得到N-保护的α-酰氧基-β-氨基 - 硫代酯，然后皂化，得到目的化合物。根据本发明的方法，可以生产α-羟基-β-氨基羧酸衍生物，它们是从α-氨基酸生产各种HIV蛋白酶抑制剂，肾素抑制剂和制癌剂的中间体。该方法包括减少反应步骤，得到所需产物的方法中的选择性高，所得产物的产率高。

8. 发明授权

US5902887A Process for producing 3-amino-2-oxo-1-halogenopropane derivatives 失效
标题翻译： 3-氨基-2-氧代-1-卤代丙烷衍生物的制备方法
公开(公告)号：US5902887A
公开(公告)日：1999-05-11
申请号：US59370
申请日：1998-04-14
申请人： Yutaka Honda , Satoshi Katayama , Kunisuke Izawa , Masakazu Nakazawa , Takayuki Suzuki , Naoko Kanno
发明人： Yutaka Honda , Satoshi Katayama , Kunisuke Izawa , Masakazu Nakazawa , Takayuki Suzuki , Naoko Kanno
IPC分类号： C07C221/00 , C07C223/02 , C07C227/16 , C07C227/32 , C07C229/22 , C07C229/34 , C07C269/06 , C07C271/22 , C07C319/20 , C07C323/43 , C07D307/20 , C07C219/04
CPC分类号： C07C271/22 , C07C221/00 , C07C227/16 , C07C227/32 , C07C229/22 , C07C229/34 , C07C269/06 , C07C319/20 , C07C323/43 , Y02P20/55
摘要： Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.
摘要翻译：通过将保护的氨基酸与乙酸烷基酯的碱金属烯醇化物反应形成的化合物与用于2-位卤化的卤化剂反应，或将保护的氨基酸与卤代乙酸烷基酯的碱金属烯醇化物反应形成 4-氨基-3-氧代-2-卤代丁酸酯衍生物，并进行水解和脱羧以产生3-氨基-2-氧代-1-卤代丙烷衍生物或其盐。本发明的方法是可以容易地转化为3-氨基-1,2-环氧丙烷的3-氨基-2-氧代-1-卤代丙烷衍生物的有用方法。

9. 发明授权

US5883284A Method for producing .alpha.-hydroxy-.beta.-aminocarboxylic acids 失效
标题翻译： α-羟基-β-氨基羧酸的制备方法
公开(公告)号：US5883284A
公开(公告)日：1999-03-16
申请号：US98538
申请日：1998-06-17
申请人： Takayuki Suzuki , Yutaka Honda , Kunisuke Izawa
发明人： Takayuki Suzuki , Yutaka Honda , Kunisuke Izawa
IPC分类号： C07C317/28 , C07C323/29 , C07C327/30 , C07C323/43 , C07C323/25 , C07C323/41
CPC分类号： C07C323/29 , C07C317/28 , C07C327/30
摘要： The present invention provides a simple and inexpensive method for producing .alpha.-hydroxy-.beta.-aminocarboxylic acids and their esters.An ester of an N-protected .alpha.-amino acid ester is converted into a .beta.-ketosulfoxide, which is then processed with an acid to give an .alpha.-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected .alpha.-acyloxy-.beta.-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce .alpha.-hydroxy-.beta.-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.
摘要翻译：本发明提供了用于生产α-羟基-β-氨基羧酸及其酯的简单和便宜的方法。将N-保护的α-氨基酸酯的酯转化成β-酮亚砜，然后用酸处理，得到α-酮基二巯基。接下来，将其进行酰化，然后用碱处理，得到N-保护的α-酰氧基-β-氨基 - 硫代酯，然后皂化，得到目标化合物。根据本发明的方法，可以生产α-羟基-β-氨基羧酸衍生物，它们是从α-氨基酸生产各种HIV蛋白酶抑制剂，肾素抑制剂和制癌剂的中间体。该方法包括减少反应步骤，得到所需产物的方法中的选择性高，所得产物的产率高。

10. 再颁专利

USRE38796E1 Process for producing 3-amino-2-oxo-1-halogenopropane derivatives 失效
标题翻译： 3-氨基-2-氧代-1-卤代丙烷衍生物的制备方法
公开(公告)号：USRE38796E1
公开(公告)日：2005-09-13
申请号：US09595173
申请日：2000-06-16
申请人： Yutaka Honda , Satoshi Katayama , Kunisuke Izawa , Masakazu Nakazawa , Takayuki Suzuki , Naoko Kanno
发明人： Yutaka Honda , Satoshi Katayama , Kunisuke Izawa , Masakazu Nakazawa , Takayuki Suzuki , Naoko Kanno
IPC分类号： C07C221/00 , C07C223/02 , C07C227/16 , C07C227/32 , C07C229/22 , C07C229/34 , C07C269/06 , C07C271/22 , C07C319/20 , C07C323/43
CPC分类号： C07C271/22 , C07C221/00 , C07C227/16 , C07C227/32 , C07C229/22 , C07C229/34 , C07C269/06 , C07C319/20 , C07C323/43 , Y02P20/55
摘要： Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.
摘要翻译：通过将保护的氨基酸与乙酸烷基酯的碱金属烯醇化物反应形成的化合物与用于2-位卤化的卤化剂反应，或将保护的氨基酸与卤代乙酸烷基酯的碱金属烯醇化物反应形成 4-氨基-3-氧代-2-卤代丁酸酯衍生物，并进行水解和脱羧以产生3-氨基-2-氧代-1-卤代丙烷衍生物或其盐。本发明的方法是可以容易地转化为3-氨基-1,2-环氧丙烷的3-氨基-2-氧代-1-卤代丙烷衍生物的有用方法。

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