公开(公告)号：US5276190A

公开(公告)日：1994-01-04

申请号：US950713

申请日：1992-09-25

申请人： Wilhelmus H. J. Boesten ,  Harold M. Moody ,  Quirinus B. Broxterman

发明人： Wilhelmus H. J. Boesten ,  Harold M. Moody ,  Quirinus B. Broxterman

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。

公开(公告)号：US5916762A

公开(公告)日：1999-06-29

申请号：US940984

申请日：1997-09-30

申请人： Wilhelmus H. J. Boesten ,  Harold M. Moody ,  Eric C. Roos

发明人： Wilhelmus H. J. Boesten ,  Harold M. Moody ,  Eric C. Roos

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。

公开(公告)号：US07029885B2

公开(公告)日：2006-04-18

申请号：US09457765

申请日：1999-12-10

申请人： Harold M. Moody ,  Wilhelmus H. J. Boesten

发明人： Harold M. Moody ,  Wilhelmus H. J. Boesten

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。