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公开(公告)号：US5037759A
公开(公告)日：1991-08-06
申请号：US277929
申请日：1988-11-30
CPC分类号： C12P41/002 , C12P17/12 , C12P7/40
摘要： The R-enantiomer of a compound of formula I: ##STR1## where Z is an optionally substituted cyclic organic moiety and C* represents an optically active carbon atom, may be prepared by supplying a substrate of formula II ##STR2## to a culture of a microorganism capable of oxidation of compound II into the R-enantiomer of I.
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2.发明授权Certain phenoxy (or 5-trifluoromethyl-pyridyl-oxy)-phenoxy-2-yl-propane derivatives 失效某些苯氧基（或5-三氟甲基 - 吡啶-2-基） - 苯氧基-2-戊基衍生物
公开(公告)号：US5110943A
公开(公告)日：1992-05-05
申请号：US705539
申请日：1991-05-24
CPC分类号： C12P41/002 , C12P17/12 , C12P7/40
摘要： The R-enantiomer of a compound of formula I: ##STR1## where Z is an optionally substituted cyclic organic moiety and C* represents an optically active carbon atom, may be prepared by supplying a substrate of formula II ##STR2## to a culture of a microorganism capable of oxidation of compound II into the R-enantiomer of I.
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3.发明授权Process for the preparation of a pharmaceutically active compound in a stereospecific form of the formula 失效用于制备具有下式的立体特异性形式的药学活性化合物的方法
公开(公告)号：US4886750A
公开(公告)日：1989-12-12
申请号：US674
申请日：1987-01-06
申请人： Mauro A. Bertola , Arthur F. Marx , Hein S. Koger , Wilhelmus J. Quax , Cornelis J. Van der Laken , Gareth T. Phillips , Brian W. Robertson , Peter D. Watts
发明人： Mauro A. Bertola , Arthur F. Marx , Hein S. Koger , Wilhelmus J. Quax , Cornelis J. Van der Laken , Gareth T. Phillips , Brian W. Robertson , Peter D. Watts
IPC分类号： C12N15/09 , A61K31/19 , A61K31/33 , A61P25/04 , A61P29/00 , C07C57/30 , C07D209/46 , C07H21/04 , C12N1/20 , C12N1/21 , C12N9/18 , C12N15/00 , C12P7/40 , C12P17/00 , C12P41/00 , C12R1/06 , C12R1/10 , C12R1/125 , C12R1/19 , C12R1/38 , C12R1/385 , C12R1/39 , C12R1/40 , C12R1/465 , C12R1/785
CPC分类号： C12P41/005 , C12N9/18 , C12P17/00 , C12P7/40 , Y10S435/822 , Y10S435/83 , Y10S435/836 , Y10S435/839 , Y10S435/849 , Y10S435/874 , Y10S435/886
摘要： A process for the preparation of a pharmaceutically active compound in a stereospecific form of the formula ##STR1## or a pharmaceutically acceptable salt or ester thereof, like an alkali metal salt or an alkaline earth metal salt or a pivaloyl ester, wherein R.sub.1 represents an optionally substituted aryl group such as a phenyl or naphthyl group optionally included in a heterocyclic ring system, which is optionally substituted, or represents a heteroaromatic ring system containing in addition to carbon atoms one or more atoms selected from nitrogen, sulphur and oxygen, this ring system being optionally substituted, which comprises subjecting a compound of the formula ##STR2## wherein R.sub.1 is an ester residue and preferably an alkyl group optionally substituted, to the action of a micro-organism having the ability for stereoselective hydrolysis of compound (II) into compound (I), having at least 80% by weight the S-configuration, and if desired converting compound (I) into the pharmaceutically acceptable salt or ester thereof.
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4.发明授权Process for the preparation of R-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol 失效制备R-2,2-R1，R2-1,3-二氧戊环-4-甲醇的方法
公开(公告)号：US5190867A
公开(公告)日：1993-03-02
申请号：US822653
申请日：1992-01-21
IPC分类号： C07D317/20 , C07D317/32 , C07D317/72 , C12P41/00
CPC分类号： C07D317/72 , C07D317/20 , C07D317/32 , C12P41/001 , C12R1/15 , C12R1/32 , C12R1/365
摘要： Process for the preparation of R-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol wherein R.sub.1 and R.sub.2 are H or alkyl groups or wherein R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a carbocyclic ring by subjecting a mixture of R- and S-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol to the action of a micro-organism or substances derived therefrom having the ability for stereoselective consumption of S-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol preferably until at least 80 wt % and more preferably all the S-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol is consumed. Various micro-organisms of the genus Rhodococcus, Nocardia and Corynebacterium are disclosed as suitable for the purpose. The R-isomer is a valuable intermediate for stereospecific synthesis of various biologically active compounds including S-metoprolol.
摘要翻译： 制备R-2,2-R1，R2-1,3-二氧戊环-4-甲醇的方法，其中R 1和R 2为H或烷基或其中R 1和R 2与它们所连接的碳原子一起形成 通过使R-和S-2,2-R1，R2-1,3-二氧戊环-4-甲醇的混合物经受微生物或其衍生物质的作用，具有立体选择性消耗S- 优选直到至少80重量％，更优选全部S-2,2-R 1，R 2，1,3-二氧戊环-4-甲醇被消耗 。 公开了红球菌属，诺卡氏菌属和棒状杆菌属的各种微生物，以适合此目的。 R-异构体是用于立体特异性合成各种生物活性化合物（包括S-美托洛尔）的有价值的中间体。
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公开(公告)号：US5043274A
公开(公告)日：1991-08-27
申请号：US340830
申请日：1989-04-20
IPC分类号： C12P7/52 , C12P7/40 , C12P7/62 , C12P41/00 , C12R1/01 , C12R1/06 , C12R1/07 , C12R1/08 , C12R1/32 , C12R1/365 , C12R1/38 , C12R1/465 , C12R1/645 , C12R1/80
CPC分类号： C12P41/00 , C12P7/40 , Y10S435/822 , Y10S435/911
摘要： A process for the preparation of S-2-(6-methoxy-2-naphthyl)propionic acid or a pharmaceutically acceptable salt or ester thereof, which comprises supplying R-2-(6-methoxy-2-naphthyl)-propionic acid or a pharmaceutically acceptable salt or ester thereof, to a microorganism having a stereospecific inverting enzyme system, or an extract of the microorganism containing said enzyme system, capable of converting the R enantiomer to the corresponding S enantiomer.
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公开(公告)号：US5108917A
公开(公告)日：1992-04-28
申请号：US212591
申请日：1988-06-28
IPC分类号： C12N1/20 , C12N9/16 , C12N9/18 , C12N15/55 , C12P7/40 , C12P17/00 , C12P41/00 , C12R1/02 , C12R1/07 , C12R1/085 , C12R1/445
CPC分类号： C12P7/40 , C12N9/16 , C12P41/005 , Y10S435/823 , Y10S435/882
摘要： A process is provided for the preparation of ibuprofen enriched in R isomer, which comprises subjecting an ester of ibuprofen, to the action of a micro-organism or substances derived thereof, that will stereoselectively hydrolyse the ester to form ibuprofen predominantly having R configuration.
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7.发明授权Process for producing 4-(2-methoxyethyl)-phenyl-glycidyl ether and/or metoprolol 失效制备4-（2-甲氧基乙基） - 苯基 - 缩水甘油醚和/或美托洛尔的方法
公开(公告)号：US4956284A
公开(公告)日：1990-09-11
申请号：US826791
申请日：1986-02-06
申请人： Gareth T. Phillips , Brian W. Robertson , Mauro A. Bertola , Hein S. Koger , Arthur F. Marx , Peter D. Watts
发明人： Gareth T. Phillips , Brian W. Robertson , Mauro A. Bertola , Hein S. Koger , Arthur F. Marx , Peter D. Watts
IPC分类号： C07C213/04 , C07D303/24 , C12P17/02
CPC分类号： C07C213/04 , C07D303/24 , C12P17/02 , Y10S435/863 , Y10S435/872 , Y10S435/874
摘要： A process for the preparation of metoprolol in a stereospecific form or a non-toxic, pharmaceutically acceptable acid addition salt thereof and/or a stereospecific form of 4-(2-methoxyethyl)-phenyl glycidyl ether which comprises subjecting 4-(2-methoxyethyl)-phenyl allyl ether to the action of a microorganism having the ability for stereoselective epoxidation of 4-(2-methoxyethyl)-phenyl allyl ether into 4-(2-methoxyethyl)-phenyl glycidyl ether having at least 80% by weight the S configuration, at least partly separating 4-(2-methoxyethyl)-phenyl glycidyl ether and/or reacting 4-(2-methoxyethyl)-phenyl glycidyl ether with isopropylamine and at least partly separating metoprolol and/or converting metoprolol into its non-toxic, pharmaceutically acceptable acid addition salt.
摘要翻译： 以立体特异性形式或无毒的药学上可接受的酸加成盐和/或立体特异性形式的4-（2-甲氧基乙基） - 苯基缩水甘油醚制备美托洛尔的方法，其包括使4-（2-甲氧基乙基） （4-甲氧基乙基） - 苯基烯丙基醚的4-（2-甲氧基乙基） - 苯基缩水甘油醚的立体选择性环氧化反应能力的微生物的作用，其具有至少80重量％的S 至少部分分离4-（2-甲氧基乙基） - 苯基缩水甘油醚和/或使4-（2-甲氧基乙基） - 苯基缩水甘油醚与异丙胺反应，并至少部分分离美托洛尔和/或将美托洛尔转化为无毒的 ，药学上可接受的酸加成盐。
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公开(公告)号：US5075233A
公开(公告)日：1991-12-24
申请号：US212631
申请日：1988-06-28
IPC分类号： C07C59/125 , A01N37/36 , C07C51/00 , C07C67/00 , C07D213/64 , C07D521/00 , C12N1/20 , C12N9/18 , C12P7/40 , C12P17/00 , C12P41/00 , C12R1/01 , C12R1/10 , C12R1/125 , C12R1/19 , C12R1/445
CPC分类号： C12P41/005 , C12N9/18 , C12P17/00 , C12P7/40
摘要： A process is provided for the enrichment in R isomer of an aryloxypropioic acid ester and for the stereoselective hydrolysis of an aryloxypropionic acid ester to form the corresponding aryloxypropionic acid in predominantly S configuration which comprises subjecting an aryloxypropionic acid ester of formula I ##STR1## wherein A is an ester residue and preferably an alkyl group, optionally substituted or branched, wherein R' is an optionally substituted aryl or heterocyclic ring system, containing in addition to carbon atoms one or more atoms selected from nitrogen, sulphur and oxygen, this ring system being optionally substituted and wherein B and D are for example a hydrogen or a halogen atom, to the action of a microorganism or substance derived thereof capable of stereoselective hydrolysis of the COOA group to form the corresponding carboxylic acid predominantly is S configuration.
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公开(公告)号：US5037751A
公开(公告)日：1991-08-06
申请号：US405553
申请日：1989-09-11
申请人： Mauro A. Bertola , Arthur F. Marx , Hein S. Koger , Wilhelmus J. Quax , Cornelis J. van der Laken , Gareth T. Phillips , Brian W. Robertson , Peter D. Watts
发明人： Mauro A. Bertola , Arthur F. Marx , Hein S. Koger , Wilhelmus J. Quax , Cornelis J. van der Laken , Gareth T. Phillips , Brian W. Robertson , Peter D. Watts
IPC分类号： C12N15/09 , A61K31/19 , A61K31/33 , A61P25/04 , A61P29/00 , C07C57/30 , C07D209/46 , C07H21/04 , C12N1/20 , C12N1/21 , C12N9/18 , C12N15/00 , C12P7/40 , C12P17/00 , C12P41/00 , C12R1/06 , C12R1/10 , C12R1/125 , C12R1/19 , C12R1/38 , C12R1/385 , C12R1/39 , C12R1/40 , C12R1/465 , C12R1/785
CPC分类号： C12P41/005 , C12N9/18 , C12P17/00 , C12P7/40 , Y10S435/822 , Y10S435/83 , Y10S435/836 , Y10S435/839 , Y10S435/849 , Y10S435/874 , Y10S435/886
摘要： A process for the preparation of a pharmaceutically active compound in a stereospecific form of the formula ##STR1## or a pharmaceutically acceptable salt or ester thereof, like an alkali metal salt or an alkaline earth metal salt or a pivaloyl ester, wherein R.sub.1 represents an optionally substituted aryl group such as a phenyl or naphthyl group optionally included in a heterocyclic ring system, which is optionally substituted, or represents a heteroaromatic ring system containing in addition to carbon atoms one or more atoms selected from nitrogen, sulphur and oxygen, this ring system being optionally substituted, which comprises subjecting a compound of the formula ##STR2## wherein R.sub.2 is an ester residue and preferably an alkyl group optionally substituted, to the action of a micro-organism having the ability for stereoselective hydrolysis of compound (II) into compound (I), having at least 80% by weight the S-configuration, and if desired converting compound (I) into the pharmaceutically acceptable salt or ester thereof.
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公开(公告)号：US4696901A
公开(公告)日：1987-09-29
申请号：US558749
申请日：1983-12-07
摘要： Hydrocarbon utilizing microorganisms are immobilized on a plastic carrier in an aqueous nutrient medium to which a minor amount of a water-immiscible hydrocarbon substrate has been added. The water-immiscible hydrocarbon is preferably hexadecane or dodecylcyclohexane and the plastic carrier is preferably polytetrafluoroethylene. Presence of the water-immiscible hydrocarbon substrate results in increased loading of microorganisms on the carrier.
摘要翻译： 利用微生物的碳氢化合物固定在塑料载体上的水性营养培养基中，少量的与水不混溶的烃基质已加入到其中。 与水不混溶的烃优选为十六烷或十二烷基环己烷，塑料载体优选为聚四氟乙烯。 与水不混溶的烃基质的存在导致载体上微生物的负载增加。
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