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1.发明授权Process for producing 1-phenyl-1,3-propanediols having high optical purtiy 失效具有高光学纯度的1-苯基-1,3-丙二醇的方法
公开(公告)号：US5395983A
公开(公告)日：1995-03-07
申请号：US182566
申请日：1994-01-18
CPC分类号： C07C29/78 , C07C33/26 , C07B2200/07
摘要： R or S-1-phenyl-1,3-propanediols having optical purity of 100% ee were obtained by recrystallization of R or S-1-phenyl-1,3-propanediols having optical purity of 20% ee to below 100% ee, the last diols are represented by the formula, ##STR1## It is possible to obtain optically pure 1-phenyl-3-propanediols from optically impure 1-phenyl-1,3-propanediols by a simple method.
摘要翻译： 光学纯度为100％ee的R或S-1-苯基-1,3-丙二醇通过将光学纯度为20％ee的R或S-1-苯基-1,3-丙二醇重结晶至低于100％ee ，最后的二醇由下式表示：通过简单的方法可以从光学上不纯的1-苯基-1,3-丙二醇获得光学上纯的1-苯基-3-丙二醇。
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2.发明授权Process for producing an optically active 1,5-disubstituted-2,4-O-isopropylidene-2,4-dihydroxypentane 失效光学活性1,5-二取代-2,4-O-异亚丙基-2,4-二羟基戊烷的制造方法
公开(公告)号：US5449793A
公开(公告)日：1995-09-12
申请号：US241994
申请日：1994-05-12
IPC分类号： C07D319/06 , C12P7/62 , C12P17/06 , C12P41/00
CPC分类号： C12P17/06 , C07D319/06 , C12P41/004 , C12P7/62
摘要： A novel optically active erythro-1-alkanoyloxy-2,4-O-isopropylidene-2,4-dihydroxy-5-substituted pentane expressed by the formula ##STR1## wherein R.sup.1 represents a halogen atom or cyano group and R.sup.2 represents an alkyl group of 1 to 6 carbon atoms, and a process for producing the above compound are provided, the compound being preferably usable as an intermediate for preparing a HMG-CoA reductase inhibitor and the process being practiced under mild conditions and with a high yield.
摘要翻译： 由式（1）表示的新型光学活性的赤式-1-烷酰氧基-2,4-O-异亚丙基-2,4-二羟基-5-取代戊烷，其中R 1表示卤素原子或氰基，R 2表示 提供1〜6个碳原子的烷基和上述化合物的制造方法，该化合物优选用作制备HMG-CoA还原酶抑制剂的中间体，该方法在温和条件下以高产率进行 。
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3.发明授权Method for producing optically active 3-substituted-2-norbornanones and their intermediates 失效光学活性3-取代-2-降冰片烯酮及其中间体的制备方法
公开(公告)号：US5266728A
公开(公告)日：1993-11-30
申请号：US931993
申请日：1992-08-19
IPC分类号： C07C45/29 , C07C45/68 , C07C49/433 , C07C49/653 , C07C49/657 , C07C61/13 , C07C61/29 , C07C62/06 , C07D207/40 , C07D207/408
CPC分类号： C07D207/408 , C07C45/29 , C07C45/68 , C07C49/433 , C07C49/653 , C07C49/657 , C07C61/13 , C07C61/29 , C07C62/06 , C07C2102/42
摘要： The present invention provides a method for producing optically active 3-substituted-2-norbornanones which are useful as starting materials for several kinds of physiologically active materials, and to their intermediates, optically active 2-hydroxy-2-norbornanecarboxylic acid and to a method for producing these intermediates.
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4.发明授权Optically active trans-2-aryl-1-cyclohexanol derivatives and a process for producing the compounds 失效光学活性的反式-2-芳基-1-环己醇衍生物及其制备方法
公开(公告)号：US5395766A
公开(公告)日：1995-03-07
申请号：US968311
申请日：1992-10-29
IPC分类号： C07D309/12 , C07C37/56 , C07C39/17 , C07C41/26 , C07C43/23 , C07C43/253 , C07C67/03 , C07C69/013 , C07C69/03 , C07D453/02 , C07F7/18 , C12P41/00 , C07D315/00 , C07C41/00 , C07C69/00
CPC分类号： C07C43/23 , C07C69/013 , C07D453/02 , C07C2101/14
摘要： The present invention provides an optically active trans-2-aryl-1-cyclohexanol derivative represented by the following general formula (I). ##STR1## The compounds can be obtained by transesterifiation reaction of the following compound (II) as a starting material with lipase. ##STR2## The optically active trans-2-aryl-1-cyclohexanol derivative can be used as an asymmetric source of asymmetric Diels-Alder reaction or a starting material of physiological active materials.
摘要翻译： 本发明提供由以下通式（I）表示的光学活性的反式-2-芳基-1-环己醇衍生物。 以下化合物（II）作为原料与脂肪酶的反应反应。 （II）光学活性的反式-2-芳基-1-环己醇衍生物可用作不对称狄尔斯 - 阿尔德反应的不对称来源或生理活性物质的原料。
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5.发明授权Optically active 1-5-disubstituted-2,4-o-isopropylidene-2,4-dihydroxypentane and a process for producing the same 失效光学活性的1-5-二取代-2,4-O-异亚丙基-2,4-二羟基戊烷及其制备方法
公开(公告)号：US5329018A
公开(公告)日：1994-07-12
申请号：US70985
申请日：1993-06-04
IPC分类号： C07D319/06 , C12P7/62 , C12P17/06 , C12P41/00
CPC分类号： C07D319/06 , C12P17/06 , C12P41/004 , C12P7/62
摘要： A novel optically active erythro-1-alkanoyloxy-2,4-O-isopropylidene-2,4-dihydroxy-5-substituted pentane expressed by the formula ##STR1## wherein R.sup.1 represents a halogen atom or cyano group and R.sup.2 represents an alkyl group of 1 to 6 carbon atoms, and a process for producing the above compound are provided, the compound being preferably usable as an intermediate for preparing a HMG-CoA reductase inhibitor and the process being practiced under mild conditions and with a high yield.
摘要翻译： 由式（1）表示的新型光学活性的赤式-1-烷酰氧基-2,4-O-异亚丙基-2,4-二羟基-5-取代戊烷，其中R 1表示卤素原子或氰基，R 2表示 提供1〜6个碳原子的烷基和上述化合物的制造方法，该化合物优选用作制备HMG-CoA还原酶抑制剂的中间体，该方法在温和条件下以高产率进行 。
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6.发明授权Process for producing optically active 3-aminobutanoic acid and the ester intermediates 失效光学活性3-氨基丁酸和酯中间体的制备方法
公开(公告)号：US5518903A
公开(公告)日：1996-05-21
申请号：US289031
申请日：1994-08-11
CPC分类号： C12P41/005 , C12P13/04
摘要： The present invention provides a process for producing optically active 3-aminobutanoic acid characterized in that it comprises an asymmetrically hydrolyzing racemic ester of 3-substituted aminobutanoic acid in the presence of a hydrolase, obtaining an optically active ester of 3-substituted aminobutanoic acid and an optically active 3-substituted aminobutanoic acid of an enantiomer of the ester, and treating the above ester represented by the formula (II): ##STR1## to remove the protecting group. In addition, the new ester intermediates represented by the above formula (II) are provided.
摘要翻译： 本发明提供了一种光学活性3-氨基丁酸的制备方法，其特征在于，在水解酶存在下，其包含不对称水解的3-取代氨基丁酸的外消旋酯，得到3-取代氨基丁酸的光学活性酯和 光学活性的3-取代的氨基丁酸的酯的对映异构体，并处理由式（II）表示的上述酯：除去保护基。 此外，提供由上述式（II）表示的新的酯中间体。
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公开(公告)号：US5604120A
公开(公告)日：1997-02-18
申请号：US517792
申请日：1995-08-22
IPC分类号： C12N11/08 , C07C35/30 , C07C69/24 , C07C69/614 , C07C69/74 , C07C69/76 , C12N11/10 , C12P7/02 , C12P41/00 , C12R1/72 , C12P7/62
CPC分类号： C12P7/02 , C12P41/004
摘要： The present invention provides a method for producing optically active endo-2-norborneols, represented by the following formula: ##STR1## and the antipodes, it comprises asymmetrically hydrolysing racemic endo-2-acyloxynorbornane or endo-2-acyloxynorbornane, whose (R)-compound is in excess, having an optical purity of 50-95% ee with lipase derived from Candida genus. The optically active endo-2-norborneol useful for synthesizing intermediates of pharmaceutical preparations in large quantities.
摘要翻译： 本发明提供了一种由下式表示的光学活性的内-2-降冰片烯的方法：＆lt; IMAGE＆gt;和对映体，包括不对称水解的外消旋内-2-酰氧基降冰片烷或内-2-酰氧基降冰片烷，其（R） 化合物过量，具有50-95％ee的光学纯度，并且衍生自念珠菌属的脂肪酶。 用于大量合成药物制剂中间体的光学活性内-2-羟基吲哚类。
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公开(公告)号：US5623078A
公开(公告)日：1997-04-22
申请号：US666742
申请日：1996-06-20
IPC分类号： C07D209/52 , C07D209/02
CPC分类号： C07D209/02
摘要： A production process with good efficiency, and applicable to production of a synthetic intermediate of a new quinolone anti-fungus agent CP-99219, is provided.A production process of an intermediate of a new quinolone compound expressed by the formula (IV) ##STR1## wherein R.sup.3 represents a benzyl group, a diphenylmethyl group, etc. and R.sup.4 represents a linear or branched alkyl group of 1 to 8C, a cycloalkyl group, etc.which process employs as a starting substance, a cyclopropanetricarboxylic acid triester expressed by the formula (I) ##STR2## wherein R.sup.1 and R.sup.2 represent a linear or branched alkyl group, a cycloalkyl group, an aryl group or an aralkyl group,and passes through seven steps.
摘要翻译： 提供了一种效率高，适用于生产新型喹诺酮类抗真菌剂CP-99219的合成中间体的生产方法。 由式（IV）表示的新型喹诺酮化合物的中间体（IV）的制备方法，其中R 3表示苄基，二苯基甲基等，R 4表示1〜8的直链或支链烷基 ，该方法用作起始物质的环烷基等，由式（I）表示的环丙烷三羧酸三酯，支化烷基，环烷基，芳基或芳烷基，并通过七个步骤。
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9.发明授权Method for producing optically active 3-hydroxyhexanoic acids using porcine pancreatic lipase 失效使用猪胰脂肪酶制备光学活性3-羟基己酸的方法
公开(公告)号：US5643793A
公开(公告)日：1997-07-01
申请号：US542067
申请日：1995-10-12
申请人： Hitoshi Yano , Naoyuki Yoshida , Teruyo Sugiura
发明人： Hitoshi Yano , Naoyuki Yoshida , Teruyo Sugiura
CPC分类号： C12P7/42 , C12P41/005
摘要： A method for producing an optically active 3-hydroxy-hexanoic acid represented by formula (1) and the enantimer by asymmetrically hydrolyzing a racemic ester of 3-hydroxyhexanoic acid in the presence of a lipase derived from porcine pancreas. ##STR1##
摘要翻译： 在由来自猪胰腺的脂肪酶存在下，通过不对称地水解3-羟基己酸的外消旋酯，制备由式（1）表示的光学活性3-羟基己酸和对映异构体的方法。 （1）
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公开(公告)号：US5128252A
公开(公告)日：1992-07-07
申请号：US690256
申请日：1991-04-25
IPC分类号： C12P41/00
CPC分类号： C12P41/004
摘要： The invention provides an optically active compound which is R- or S- ester having the general formula: ##STR1## wherein R.sup.1 is hydrogen or acyl of 2-20 carbon atoms, R.sup.2 is alkyl, alkenyl or alkynyl of 3-40 carbon atoms, and the carbon indicated by * is an asymmetric carbon atom.
摘要翻译： 本发明提供了具有以下通式的R-或S-酯的光学活性化合物：其中R1是氢或2-20个碳原子的酰基，R2是3-40的烷基，烯基或炔基 碳原子，由*表示的碳是不对称碳原子。
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