Method for producing optically active 2-cyclopenten-4-one-1-ol esters,
2-cyclopenteno-4-one-1-ol ester and complexes thereof with optically
active 1,6-diphenyl-2,4-hexadiyne-1,6-diol
    62.
    发明授权
    Method for producing optically active 2-cyclopenten-4-one-1-ol esters, 2-cyclopenteno-4-one-1-ol ester and complexes thereof with optically active 1,6-diphenyl-2,4-hexadiyne-1,6-diol 失效
    光学活性的2-环戊烯-4-酮-1-醇酯,2-环戊烯-4-酮-1-醇酯及其与光学活性的1,6-二苯基-2,4-己二炔-1的配合物的制备方法, 6-二醇

    公开(公告)号:US5041620A

    公开(公告)日:1991-08-20

    申请号:US892103

    申请日:1986-08-04

    摘要: A method for producing an optically active 2-cyclopenten-4-one-1-ol ester useful as an intermediate for medicines, agricultural chemicals and represented by the general formula (I), ##STR1## wherein R represents a saturated or unsaturated aliphatic hydrocarbon residue which may or may not be substituted with a halogen atom, and a mark * represents an asymmetric carbon,which comprises bringing a 2-cyclopenten-4-one-1-ol ester represented by the general formula ##STR2## wherein R represents a saturated or unsaturated aliphatic hydrocarbon residue which may or may not be substituted with a halogen atom, into contact with an optically active 1,6-diphenyl-2,4-hexadiyne-1,6-diol derivative represented by the general formula (II), ##STR3## wherein R' represents a halogenated phenyl, lower alkylphenyl, naphthyl or tertiary lower alkyl group, and a mark * represents an asymmetric carbon,in an organic solvent to obtain an optically active cyclopentenone ester complex which is a bound product of the optically active 2-cyclopenten-4-one-1-ol ester represented by the foregoing general formula (I) with the optically active 1,6-diphenyl-2,4-hexadiyne-1,6-diol derivative represented by the foregoing general formula (II), and then decomposing the resulting optically active cyclopentenone ester complex.

    摘要翻译: 可用作药物,农药中间体的光学活性2-环戊烯-4-酮-1-醇酯的方法,由通式(I)表示,其中R表示饱和或 不饱和脂肪族烃残基,其可以被卤素原子取代,也可以不被卤原子取代,标记*表示不对称碳,该方法包括使由通式表示的2-环戊烯-4-酮-1-醇酯 R表示可以或可以不被卤素原子取代的饱和或不饱和脂肪族烃残基,与通式(1)表示的光学活性1,6-二苯基-2,4-己二炔-1,6-二醇衍生物接触, (II),其中R'表示卤代苯基,低级烷基苯基,萘基或叔低级烷基,标记*表示不对称碳,在有机溶剂中得到光学活性环戊烯酮酯络合物,其中 是一个有限的亲 由上述通式(I)表示的光学活性2-环戊烯-4-酮-1-醇酯与光学活性1,6-二苯基-2,4-己二炔-1,6-二醇衍生物的管道,由 前述通式(II),然后分解得到的光学活性环戊烯酮酯络合物。

    Optically active benzene derivatives and process for preparation thereof
    63.
    发明授权
    Optically active benzene derivatives and process for preparation thereof 失效
    光活性苯衍生物及其制备方法

    公开(公告)号:US4985590A

    公开(公告)日:1991-01-15

    申请号:US182461

    申请日:1988-04-18

    IPC分类号: C07C43/178 C12P7/22 C12P41/00

    摘要: Disclosed are novel optically active benzene derivatives represented by the formula (I): ##STR1## wherein R represents an alkyl or alkoxyalkyl group having 1 to 20 carbon atoms, which group may contain a halogen; Z represents a hydrogen atom or a halogen atom; l and n each represents a number of 0 or 1; and * indicates asymmetric carbon atom, anda process for preparing the above optically active benzene derivative which comprises debenzylating an optically active benzyl derivative represented by the formula (II): ##STR2## wherein, R, Z, l, n and * have the same meanings as defined above, and A represents a hydrogen atom, a lower alkyl group, a lower alkoxyl group or a halogen atom.

    Production of cyclopentenones by enzyme resolution
    64.
    发明授权
    Production of cyclopentenones by enzyme resolution 失效
    通过酶分解制备环戊烯酮

    公开(公告)号:US4957867A

    公开(公告)日:1990-09-18

    申请号:US055362

    申请日:1987-05-29

    IPC分类号: C12P7/42 C12P7/62

    CPC分类号: C12P7/42 C12P7/62

    摘要: A process for preparing an optically active cyclopentenone of the formula: ##STR1## wherein R is a hydrogen atom or a lower alkyl group and n is an integer of 4 to 8, which comprises contacting a dl-cyclopentenone ester of the formula: ##STR2## wherein R and n are each as defined above and R' is a lower alkyl group optionally substituted with halogen on an enzyme having a capability of hydrolyzing selectively either one of the d- or l-form isomer in the dl-cyclopentenone ester (II) in an aqueous medium for asymmetric hydrolysis.

    摘要翻译: 一种制备下式的光学活性环戊烯酮的方法:其中R是氢原子或低级烷基,n是4至8的整数,其包括使下式的dl-环戊烯酮与式 (II)其中R和n各自如上所定义,R'是任选被卤素取代的低级烷基,该酶具有选择性地水解d-或l-型异构体中的任一种的能力 dl-环戊烯酮酯(II)在不溶性水解的水性介质中。

    Process for preparing optically active 4-hydroxy-2-cyclopentenones
    65.
    发明授权
    Process for preparing optically active 4-hydroxy-2-cyclopentenones 失效
    光学活性4-羟基-2-环戊烯酮的制备方法

    公开(公告)号:US4714782A

    公开(公告)日:1987-12-22

    申请号:US700890

    申请日:1985-02-12

    摘要: A process for preparing an optically active 2-substituted or unsubstituted-4-hydroxy-2-cyclopentenone of the formula: ##STR1## wherein R is a hydrogen atom, an allyl group or a propargyl group, which comprises reacting the corresponding 2-substituted or unsubstituted-4-hydroxy-2-cyclopentenone of the formula: ##STR2## wherein R is defined above with a lactone chosen from (1R,5S)-6,6-dimethyl-4-hydroxy-3-oxabicyc lo[3.1.0]hexan-2-one or (1S,5R)-6,6-dimethyl-4-hydroxy-3-oxabicyclo[3.1.0]hexan-2-one in a molar ratio of 1.5 - 2:1 in the presence of p-toluenesulfonic acid or benzenesulfonic acid in the coexistence of an organic solvent under elimination of water as an azeotropic mixture with the organic solvent to obtain a reaction mixture comprising (1R,5S)-6,6-dimethyl-3-oxa-4(R)-[1(R)-4-oxo-2-substituted or unsubstituted-2-cyclopentenyloxy]bicyclo[3.1.0]hexan-2-one or (1S,5R)-6,6-dimethyl-3-oxa-4(S)-[1(S)-4-oxo-2-substituted or unsubstituted-2-cyclopentenyloxy]bicyclo[3.1.0]hexan-2-one of the formula: ##STR3## wherein R is as defined above, of which either one isomer is contained in a considerably larger amount than the other isomer, separating the isom er having the larger content from the reaction mix ture and hydrolyzing the separated isomer to give the optically active 2-substituted or unsubstituted-4-hydrox y-2-cyclopentenone.

    摘要翻译: 制备下式的光学活性2-取代或未取代的4-羟基-2-环戊烯酮的方法:其中R是氢原子,烯丙基或炔丙基,其包括使相应的2-取代的 或下式所示的未取代的4-羟基-2-环戊烯酮:其中R定义如上,其中内酯选自(1R,5S)-6,6-二甲基-4-羟基-3-氧杂双环[3.1。 0]己-2-酮或(1S,5R)-6,6-二甲基-4-羟基-3-氧杂双环[3.1.0]己烷-2-酮,其摩尔比为1.5-2:1 的对甲苯磺酸或苯磺酸在与有机溶剂的共沸混合物中除去水作为有机溶剂共存,得到包含(1R,5S)-6,6-二甲基-3-氧杂-4 (R) - [1(R)-4-氧代-2-取代或未取代的-2-环戊烯氧基]双环[3.1.0]己-2-酮或(1S,5R)-6,6-二甲基-3- 氧杂-4(S) - [1(S)-4-氧代-2-取代或未取代的-2-环戊烯氧基]双环[3.1.0]己-2-酮 其中R如上所定义,其中一种异构体的含量比其他异构体大得多,从反应混合物中分离具有较大含量的等分子并水解分离的异构体,得到 光学活性的2-取代或未取代的-4-羟基-2-环戊烯酮。

    Process for preparing 4-hydroxy-2-cyclopentenones
    67.
    发明授权
    Process for preparing 4-hydroxy-2-cyclopentenones 失效
    制备4-羟基-2-环戊烯酮的方法

    公开(公告)号:US4608442A

    公开(公告)日:1986-08-26

    申请号:US629488

    申请日:1984-07-10

    CPC分类号: C07C45/673

    摘要: A process for producing a compound of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, an alkyl group or an alkenyl group and R.sub.2 is an alkyl group, an alkenyl group or an alkynyl group, which comprises treating a compound of the formula: ##STR2## wherein R.sub.1 and R.sub.2 are each as defined above and R is a hydrogen atom or a lower alkyl group in the presence of an acidic substance and water.

    摘要翻译: 一种制备下式的化合物的方法:其中R1是氢原子,烷基或烯基,R2是烷基,烯基或炔基,其包括处理化合物 其中R1和R2各自如上所定义,R是氢原子或低级烷基,其在酸性物质和水的存在下进行。

    Method for producing an optically active
2,2-dimethylcyclopropanecarboxylic acid
    68.
    发明授权
    Method for producing an optically active 2,2-dimethylcyclopropanecarboxylic acid 失效
    光学活性2,2-二甲基环丙烷羧酸的制造方法

    公开(公告)号:US4542235A

    公开(公告)日:1985-09-17

    申请号:US482259

    申请日:1983-04-05

    IPC分类号: C07C51/487 C07C61/04

    CPC分类号: C07C51/487

    摘要: A method for producing an optically active 2,2-dimethylcyclopropanecarboxylic acid useful as an intermediate for dehydropeptidase I inhibitors, medicines and agricultural chemicals, which comprises reacting an optically active diphenylethylamine represented by the formula, ##STR1## wherein R.sub.1 and R.sub.2 are each a hydrogen atom or a lower alkyl group, with 2,2-dimethylcyclopropanecarboxylic acid in a solvent to achieve the optical purification of said acid.

    摘要翻译: 一种用作脱水肽酶I抑制剂,药物和农药的中间体的光学活性2,2-二甲基环丙烷羧酸的制备方法,其包括使下式表示的光学活性二苯乙胺,其中R1和R2各自为氢 原子或低级烷基,与2,2-二甲基环丙烷羧酸在溶剂中实现所述酸的光学纯化。

    Process for preparing 2-cyclopentenone esters
    69.
    发明授权
    Process for preparing 2-cyclopentenone esters 失效
    制备2-环戊烯酮酯的方法

    公开(公告)号:US4535182A

    公开(公告)日:1985-08-13

    申请号:US523602

    申请日:1983-08-16

    摘要: 2-Cyclopentenone esters of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or lower alkenyl, R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, or cycloalkyl, cycloalkenyl or substituted or unsubstituted aryl and R.sup.3 is hydrogen or lower alkyl are prepared in high yields by reacting the corresponding racemic or optically active 4-cyclopentenone of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above and R.sup.3 is hydrogen or acyl with at least one lower aliphatic carboxylic acid and/or metal or amine salts thereof.

    摘要翻译: 2-环戊烯酮,其分子式如下:其中R1是氢,低级烷基或低级烯基,R2是低级烷基,低级烯基,低级炔基或环烷基,环烯基或取代或未取代的芳基,R3是氢或 通过使下式的相应的外消旋或光学活性的4-环戊烯酮与其中R 1和R 2各自如上定义并且R 3是氢或酰基与至少一个低级脂族羧酸(II)反应制得低级烷基, 酸和/或其金属盐或胺盐。

    Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric
acid)-cyclohexane).alpha.-methyl substituted
    70.
    发明授权
    Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric acid)-cyclohexane).alpha.-methyl substituted 失效
    4-(1,1-双 - (苯氧基 - 丙酸) - 环己烷)(60-甲基取代的)的二杂环酯

    公开(公告)号:US4092324A

    公开(公告)日:1978-05-30

    申请号:US716666

    申请日:1976-08-23

    摘要: Bisphenoxy carboxylic acid derivatives useful as an antiarteriosclerosis agent with good absorbability and low toxicity, which are novel compounds represented by the general formula, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atoms or lower alkyl groups and A preresents ##STR2## (wherein in case R.sub.3 is a hydrogen atom, R.sub.4 represents an amino-lower-alkyl group, an N-lower-alkylaminoalkyl group, a heterocyclic group, or a heterocyclic group-substituted alkyl group; or R.sub.3 and R.sub.4 may join through an intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent) or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a hydroxyalkyl group or a derivative thereof, and R.sub.6 represents a hydroxyalkyl group or a heterocyclic group; or R.sub.5 and R.sub.6 may join to form a cyclic group, or may join through another intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent).

    摘要翻译: 作为具有良好吸收性和低毒性的抗动脉硬化剂的双苯氧基羧酸衍生物,它们是由通式表示的新化合物,其中R 1和R 2表示氢原子或低级烷基,并且A表示( 其中,在R 3为氢原子的情况下,R 4表示氨基 - 低级烷基,N-低级烷基氨基烷基,杂环基或杂环基取代的烷基;或者,R 3和R 4可以通过中间杂原子 原子形成杂环基,如果所述杂原子是氮原子,则该氮原子可以具有作为取代基的低级烷基)或者其中R5表示氢原子,羟烷基或其衍生物,和 R6表示羟基烷基或杂环基;或者R5和R6可以连接形成环状基团,或者可以通过另一个中间杂原子连接形成杂环基,如果所述杂原子是氮原子 ,该氮原子可以具有低级烷基作为取代基)。