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公开(公告)号：US5276190A
公开(公告)日：1994-01-04
申请号：US950713
申请日：1992-09-25
IPC分类号： C07C213/00 , C07C215/08 , C07C215/28 , C07C319/20 , C07C323/24 , C07C323/29 , C07C209/68
CPC分类号： C07C319/20 , C07C213/00
摘要： The invention relates to a method for the preparation of an .alpha.,.alpha.-disubstituted .alpha.-amino alcohol from the corresponding amide with the aid of sodium in the presence of an alcohol as solvent. The conversion of amino acid amide to amino alcohol proceeds virtually quantitatively. Moreover, the reduction of the amino acid amide to the corresponding amino alcohol proceeds with retention of optical activity.
摘要翻译： 本发明涉及在醇作为溶剂的存在下，借助于钠从相应的酰胺制备（α），（α） - 二取代（α） - 氨基醇的方法。 氨基酸酰胺向氨基醇的转化实际上是定量的。 此外，将氨基酸酰胺还原成相应的氨基醇进行保留光学活性。
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公开(公告)号：US5468901A
公开(公告)日：1995-11-21
申请号：US88553
申请日：1993-07-09
IPC分类号： C07B53/00 , C07C319/20 , C07C319/28 , C07C323/52 , C07C323/60 , C07C233/05 , C07C237/06
CPC分类号： C07C319/28
摘要： The invention relates to a process for preparing optically active methionine amide in high ee purities in which a mixture of D- and L-methionine amide or the Schiff bases thereof is at least partly converted, optionally in the presence of 0.5-4 equivalents of an aldehyde, relative to the amount of methionine amide, and water, in the presence of an organic solvent, using less than 1.2 equivalents of L- or D-mandelic acid, respectively, relative to the amount of D- or L-methionine amide, respectively, or the Schiff bases thereof, present in the mixture of D- and L-methionine amide or the Schiff bases thereof, into a salt of methionine amide and mandelic acid, a portion consisting substantially of one of the diastereoisomers of the salt is separated from the reaction mixture obtained, and the salt is converted into the optically active methionine. A high degree of optical purity is obtained. This process can be advantageously combined with a preparation of D,L-methionine amide from D,L-methionine nitrile by returning the residual methionine amide obtained after separation of the diastereomeric salt and recovery of the mandelic acid to the preparation of D,L-methionine amide where racemization of the recycled methionine amide takes place in situ. A high overall efficiency can thus obtained in spite of a relatively low efficiency of conversion into the diastereoisomeric salt, relative to the amount of D- and L-methionine amide, or the Schiff bases thereof, used.
摘要翻译： 本发明涉及在高纯度中制备光学活性甲硫氨酰胺的方法，其中D-和L-甲硫氨酸酰胺或其席夫碱的混合物至少部分转化，任选地在0.5-4当量的 相对于甲硫氨酸酰胺的量和水，在有机溶剂的存在下，分别使用相对于D-或L-甲硫氨酸酰胺的量小于1.2当量的L-或D-扁桃酸， 或者其存在于D-和L-甲硫氨酸酰胺或其席夫碱的混合物中的席夫碱分成蛋氨酸酰胺和扁桃酸的盐，基本上由盐的非对映异构体组成的部分被分离 从得到的反应混合物中，将盐转化成光学活性的甲硫氨酸。 获得高度的光学纯度。 该方法可以有利地与D，L-甲硫氨酸腈制备D，L-甲硫氨酸酰胺，通过返回分离非对映异构盐后得到的残留的甲硫氨酰胺，并将扁桃酸回收制备D，L- 甲硫氨酰胺，其中回收的甲硫氨酸酰胺的外消旋化在原位发生。 因此，相对于使用的D-和L-甲硫氨酸酰胺或其席夫碱的量，尽管转化为非对映异构体盐的效率相对较低，因此可以获得高的整体效率。
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3.发明授权Process for preparing optically active 2-amino-&ohgr;-oxoalkanoic acid derivatives 失效光学活性2-氨基-ω-氧代链烷酸衍生物的制备方法公开(公告)号：US06291701B1
公开(公告)日：2001-09-18
申请号：US09640916
申请日：2000-08-18
IPC分类号： C07C25511
CPC分类号： B32B3/00 , A45D34/02 , A45D40/0087 , B32B29/06 , C07C229/22 , C07C231/06 , C07C237/04 , C07C253/00 , C07D317/28 , C07D317/30 , C07D319/06 , C12P13/04 , C12P41/006 , G09F5/04 , C07C255/24
摘要： A process is disclosed for preparing an (S)-2-amino-&ohgr;-oxoalkanoic acid derivative in which the corresponding aldehyde is converted into the corresponding acetal-protected aldehyde, the acetal-protected aldehyde is converted into the corresponding aminonitrile, the aminonitrile is converted into the corresponding amino acid amide, the amino acid amide is subjected to an enzymatic, enantioselective hydrolysis in which the (R)-enantiomer of the amino acid amide remains and the (S)-enantiomer is converted into the (S)-amino acid, and the (S)-amino acid is isolated. Preferably,the reaction mixture obtained after the conversion of the aminonitrile into the amino acid amide is treated with a benzaldehyde to form the Schiff base of the amino acid amide. The Schiff base is separated out and is converted into the free amino acid amide.
摘要翻译： 公开了一种制备（S）-2-氨基-ω-氧代链烷酸衍生物的方法，其中相应的醛转化成相应的缩醛保护的醛，缩醛保护的醛转化成相应的氨基腈，氨基腈是 转化为相应的氨基酸酰胺，氨基酸酰胺进行酶，对映选择性水解，其中氨基酸酰胺的（R） - 对映异构体残留，（S） - 对映异构体转化为（S） - 氨基 酸，并分离出（S） - 氨基酸。 优选将氨基腈转化成氨基酸酰胺后得到的反应混合物用苯甲醛处理，形成氨基酸酰胺的席夫碱。 将席夫碱分离出并转化成游离氨基酸酰胺。
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4.发明授权Process for preparing optically active 2-amino-&ohgr;-oxoalkanoic acid derivatives 失效光学活性2-氨基-ω-氧代链烷酸衍生物的制备方法公开(公告)号：US06222052B1
公开(公告)日：2001-04-24
申请号：US09641619
申请日：2000-08-18
IPC分类号： C07D31730
CPC分类号： B32B3/00 , A45D34/02 , A45D40/0087 , B32B29/06 , C07C229/22 , C07C231/06 , C07C237/04 , C07C253/00 , C07D317/28 , C07D317/30 , C07D319/06 , C12P13/04 , C12P41/006 , G09F5/04 , C07C255/24
摘要： A process is disclosed for preparing an (S)-2-amino-&ohgr;-oxoalkanoic acid derivative in which the corresponding aldehyde is converted into the corresponding acetal-protected aldehyde, the acetal-protected aldehyde is converted into the corresponding aminonitrile, the aminonitrile is converted into the corresponding amino acid amide, the amino acid amide is subjected to an enzymatic, enantioselective hydrolysis in which the (R)-enantiomer of the amino acid amide remains and the (S)-enantiomer is converted into the (S)-amino acid, and the (S)-amino acid is isolated. Preferably, the reaction mixture obtained after the conversion of the aminonitrile into the amino acid amide is treated with a benzaldehyde to form the Schiff base of the amino acid amide. The Schiff base is separated out and is converted into the free amino acid amide.
摘要翻译： 公开了一种制备（S）-2-氨基-ω-氧代链烷酸衍生物的方法，其中相应的醛转化成相应的缩醛保护的醛，缩醛保护的醛转化成相应的氨基腈，氨基腈是 转化为相应的氨基酸酰胺，氨基酸酰胺进行酶，对映选择性水解，其中氨基酸酰胺的（R） - 对映异构体残留，（S） - 对映异构体转化为（S） - 氨基 酸，并分离出（S） - 氨基酸。 优选将氨基腈转化成氨基酸酰胺后得到的反应混合物用苯甲醛处理，形成氨基酸酰胺的席夫碱。 将席夫碱分离出并转化成游离氨基酸酰胺。
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公开(公告)号：US06720169B1
公开(公告)日：2004-04-13
申请号：US09640796
申请日：2000-08-18
IPC分类号： C12P1300
CPC分类号： B32B3/00 , A45D34/02 , A45D40/0087 , B32B29/06 , C07C229/22 , C07C231/06 , C07C237/04 , C07C253/00 , C07D317/28 , C07D317/30 , C07D319/06 , C12P13/04 , C12P41/006 , G09F5/04 , C07C255/24
摘要： A process is disclosed for preparing an (S)-2-amino-&ohgr;-oxoalkanoic acid derivative in which the corresponding aldehyde is converted into the corresponding acetal-protected aldehyde, the acetal-protected aldehyde is converted into the corresponding aminonitrile, the aminonitrile is converted into the corresponding amino acid amide, the amino acid amide is subjected to an enzymatic, enantioselective hydrolysis in which the (R)-enantiomer of the amino acid amide remains and the (S)-enantiomer is converted into the (S)-amino acid, and the (S)-amino acid is isolated. Preferably, the reaction mixture obtained after the conversion of the aminonitrile into the amino acid amide is treated with a benzaldehyde to form the Schiff base of the amino acid amide. The Schiff base is separated out and is converted into the free amino acid amide.
摘要翻译： 公开了一种制备（S）-2-氨基-ω-氧代链烷酸衍生物的方法，其中相应的醛转化成相应的缩醛保护的醛，缩醛保护的醛转化成相应的氨基腈，氨基腈是 转化为相应的氨基酸酰胺，氨基酸酰胺进行酶，对映选择性水解，其中氨基酸酰胺的（R） - 对映异构体残留，（S） - 对映异构体转化为（S） - 氨基 酸，并分离出（S） - 氨基酸。 优选将氨基腈转化成氨基酸酰胺后得到的反应混合物用苯甲醛处理，形成氨基酸酰胺的席夫碱。 将席夫碱分离出并转化成游离氨基酸酰胺。
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公开(公告)号：US5916762A
公开(公告)日：1999-06-29
申请号：US940984
申请日：1997-09-30
IPC分类号： C07D499/00 , C12P37/04 , C07D499/18 , C12P37/00
CPC分类号： C07D499/00 , C12P37/04
摘要： Process for the recovery of ampicillin from a mixture containing ampicillin and 6-aminopenicillic acid (6-APA), in which a mixture of ampicillin and 6-APA, with a pH higher than 7, which apart from any solid ampicillin being present is homogeneous at a pH between 7 and 8.5, is subjected to a pH lowering till a pH lower than 8.2 is reached, and the solid substance present is recovered. The process is in particular suitable to be applied to the reaction mixture which is obtained after the enzymatic acylation reaction of 6-APA with a phenylglycidine derivative as acylation agent. Pure ampicillin can thus be recovered in a simple way.
摘要翻译： 从含有氨苄青霉素和6-氨基青蒿酸（6-APA）的混合物中回收氨苄青霉素的方法，其中氨苄西林和6-APA的混合物，pH高于7，除了存在任何固体氨苄青霉素之外 在pH7〜8.5之间，进行pH降低，直至达到低于8.2的pH值，并回收存在的固体物质。 该方法特别适用于6-APA与苯基甘氨啶衍生物作酰化剂的酰化反应后获得的反应混合物。 因此，可以简单的方式回收纯氨苄青霉素。
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公开(公告)号：US07029885B2
公开(公告)日：2006-04-18
申请号：US09457765
申请日：1999-12-10
IPC分类号： C12N9/00
CPC分类号： C12P37/04
摘要： Ampicillin is produced in a batch process by enzymatic acylation of 6-aminopenicillanic acid (6-APA) with the aid of phenylglycine derivative such as D-phenylglycine amide. High conversions of phenylglycine derivative may be achieved by having the total concentration in the reaction mixture of 6-APA and ampicillin greater than 250 mM and the molar ration of total quantity of phenylglycine derivative to total quantity of 6-APA less than 2.5. Higher yields of ampicillin may be achieved when the amount of dissolved 6-APA is kept low, e.g. below 300 mM.
摘要翻译： 通过6-苯基甘氨酸衍生物如D-苯基甘氨酸酰胺的酶促酰基化6-氨基青霉烷酸（6-APA），分批生产氨苄青霉素。 苯基甘氨酸衍生物的高转化率可以通过使6-APA和氨苄青霉素的反应混合物中的总浓度大于250mM，苯基甘氨酸衍生物的总量与6-APA总量的摩尔比小于2.5来实现。 当溶解的6-APA的量保持较低时，可以获得较高的氨苄青霉素产量。 低于300mM。
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公开(公告)号：US06222013B1
公开(公告)日：2001-04-24
申请号：US09425023
申请日：1999-10-25
IPC分类号： C07K100
CPC分类号： C07K5/06026 , C07C227/18 , C07C305/06 , C07D207/16 , C07K1/107 , C07K5/0613
摘要： A process is disclosed for the esterification of an amino acid or peptide in which the amino acid or peptide is converted into the corresponding ester in the presence of a hydrosulphate have the general formula ROSO3H, where R represents an alkyl group, with the hydrosulphate being prepared, in the presence of the amino acid or peptide, from chlorosulphonic acid and an alcohol having the general formula ROH, where R has the same meaning as above. The chlorosulphonic acid to amino acid or peptide molar ratio preferably is between 0.8 and 2.0, in particular between 1.0 and 1.3. A primary alcohol, in particular methanol, is preferably used as alcohol. The amino acid used may be for example an &agr;-amino acid chosen from the group comprising p-hydroxyphenylglycine, phenylglycine, phenylalanine, tyrosine, proline and valine; L-alanyl-L-proline or an ester of L-aspartyl-L-phenylalanine, for example, may be used as peptide.
摘要翻译： 公开了一种氨基酸或肽的酯化方法，其中氨基酸或肽在硫酸氢盐存在下转化成相应的酯，具有通式ROSO 3 H，其中R表示烷基，其中制备硫酸氢盐 在氨基酸或肽的存在下，由氯磺酸和具有通式ROH的醇，其中R具有与上述相同的含义。 氯磺酸与氨基酸或肽的摩尔比优选在0.8和2.0之间，特别是在1.0和1.3之间。 优选使用伯醇，特别是甲醇作为醇。 所使用的氨基酸可以是例如选自对羟基苯基甘氨酸，苯基甘氨酸，苯丙氨酸，酪氨酸，脯氨酸和缬氨酸的α-氨基酸; 例如，L-丙氨酰-L-脯氨酸或L-天冬氨酰基-L-苯丙氨酸的酯可用作肽。
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公开(公告)号：US5859241A
公开(公告)日：1999-01-12
申请号：US821519
申请日：1997-03-21
IPC分类号： C07D281/10
CPC分类号： C07D281/10
摘要： Process for the preparation of a 1,5-benzothiazepine derivative, or a salt thereof, of formula 1 ##STR1## where R1 represents H, an alkyl group or an alkoxy group and R.sub.2 represents H or a halogen, in which process a propanoic acid derivative of formula 2 ##STR2## where R.sub.1 and R.sub.2 are as defined above and R.sub.3 represents H or an alkyl group is subjected to an intramolecular cyclisation reaction in a non-halogenated solvent in the presence of a carboxylic acid. Preferably, R.sub.2 is H and R.sub.1 is OCH.sub.3. Trichloroacetic acid is preferably used as .alpha.-chlorinated acid. The benzothiazepine obtained on cyclisation can be subjected to an alkylation reaction and/or an acylation reaction to obtain known pharmaceutical products, in particular diltiazem.
摘要翻译： 制备式1的1,5-苯并硫氮杂衍生物或其盐的方法，其中R 1表示H，烷基或烷氧基，R 2表示H或卤素，其中丙酸 式2的酸衍生物其中R 1和R 2如上所定义，R 3表示H或烷基在羧酸存在下在非卤化溶剂中进行分子内环化反应。 R2优选为H，R1为OCH3。 三氯乙酸优选用作α-氯代酸。 通过环化获得的苯并硫氮杂化物可进行烷基化反应和/或酰化反应，以获得已知的药物产品，特别是地尔硫卓。
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10.发明授权Process for preparing an .alpha.-amino acid, the corresponding ester and amide 失效制备α-氨基酸的方法，相应的酯和酰胺
公开(公告)号：US5336805A
公开(公告)日：1994-08-09
申请号：US928317
申请日：1992-08-12
IPC分类号： C07C227/10 , C07C227/18 , C07C229/08 , C07C229/36 , C07C231/14 , C07C229/00
CPC分类号： C07C231/14 , C07C227/10
摘要： Process for preparing an a-amino acid having the general formula (1) of ##STR1## where R represents an aryl group or a substituted aryl, cycloalkyl or alkyl group, in which process glyoxylic acid, or a precursor or derivative thereof, is contacted in the presence of sulphamic acid with an unsaturated compound chosen from the group of aromatics, cycloalkenes and alkenes. By applying the process higher efficiencies are obtained.The acid obtained as reaction product can be esterified and amidated without prior isolation.
摘要翻译： 制备具有通式（1）的化合物（1）的α-氨基酸的方法，其中R表示芳基或取代的芳基，环烷基或烷基，其中乙醛酸或其前体或衍生物 在氨基磺酸存在下与选自芳族化合物，环烯烃和烯烃的不饱和化合物接触。 通过应用该方法，可获得更高的效率。 作为反应产物获得的酸可以在没有预先分离的情况下酯化和酰胺化。
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