Process for the preparation of 5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone
    31.
    发明授权
    Process for the preparation of 5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone 有权
    制备5 - [(4-氯苯基)甲基] -2,2-二甲基环戊酮的方法

    公开(公告)号:US07166750B1

    公开(公告)日:2007-01-23

    申请号:US10332471

    申请日:2000-08-11

    摘要: 5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone is produced by reacting 1-[(4-chlorophenyl)methyl]-3-methyl-2-oxocyclopentanecarboxylic acid methyl ester or 1-[(4-chlorophenyl)methyl]-3-methyl-2-oxocyclopentanecarboxylic acid ethyl ester with sodium hydride and methyl halide, then hydrolyzing the obtained 1-[(4-chlorophenyl)methyl]-3,3-dimethyl-2-oxocyclopentanecarboxylic acid methyl ester or 1-[(4-chlorophenyl)methyl]-3,3-dimethyl-2-oxocyclopentanecarboxylic acid ethyl ester. The process provides 5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone, an important intermediate of an agricultural or horticultural fungicide, e.g., Metconazole.

    摘要翻译: 5 - [(4-氯苯基)甲基] -2,2-二甲基环戊酮通过使1 - [(4-氯苯基)甲基] -3-甲基-2-氧代环戊烷甲酸甲酯或1 - [(4-氯苯基) 甲基] -3-甲基-2-氧代环戊烷甲酸乙酯与氢化钠和甲基卤反应,然后水解所得的1 - [(4-氯苯基)甲基] -3,3-二甲基-2-氧代环戊烷甲酸甲酯或1- [(4-氯苯基)甲基] -3,3-二甲基-2-氧代环戊烷甲酸乙酯。 该方法提供了5 - [(4-氯苯基)甲基] -2,2-二甲基环戊酮,农业或园艺杀真菌剂如甲基康唑的重要中间体。

    Process for preparation of azolylmethylcycloalkanol derivatives
    32.
    发明授权
    Process for preparation of azolylmethylcycloalkanol derivatives 失效
    唑基甲基环烷醇衍生物的制备方法

    公开(公告)号:US5466816A

    公开(公告)日:1995-11-14

    申请号:US337275

    申请日:1994-11-10

    摘要: A process for preparing a derivative of azolylmethylcycloalkanol of the following formula (I) comprising, providing a solid-liquid two-phase mixture of a cycloalkanone derivative of formula (II), an azole compound of formula (III), a metal oxide of formula (IV), and an organic solvent, and adding a sulfonium compound of formula (V) to said solid-liquid two-phase mixture under heating while stirring, ##STR1## wherein R.sup.1 and R.sup.2 individually represent a hydrogen atom or an alkyl group; X is a halogen atom, an alkyl group, a haloalkyl group, a phenyl group, a cyano group, or a nitro group; m is an integer of 0 to 5 (when m is 2 or larger, Xs may be either the same or different); n is an integer of 0 to 2; A represents a nitrogen atom or a group CH; M.sup.1 represents an alkali metal atom or an alkaline earth metal atom; M.sup.2 represents an alkaline earth metal atom, a zinc atom, or two alkali metal atoms; Y represents a halogen atom or a C.sub.1 -C.sub.4 alkoxysulfonyloxy group; and p denotes an integer of 0 or 1.

    摘要翻译: 一种制备下式(I)的唑基甲基环烷醇衍生物的方法,包括:提供式(II)的环烷酮衍生物,式(III)的唑类化合物,式(III)的唑类化合物,式 (IV)和有机溶剂,并在搅拌下在加热下向所述固液两相混合物中加入式(Ⅴ)的锍化合物,(II)+(III)+ M 2 O (I)其中R 1和R 2各自表示氢原子或烷基; X是卤素原子,烷基,卤代烷基,苯基,氰基或硝基; m为0〜5的整数(当m为2以上时,X可以相同或不同); n为0〜2的整数, A表示氮原子或基团CH; M1表示碱金属原子或碱土金属原子; M2表示碱土金属原子,锌原子或两个碱金属原子; Y表示卤素原子或C1-C4烷氧基磺酰氧基; p表示0或1的整数。

    Azole derivative and azole mycocide
    34.
    发明授权
    Azole derivative and azole mycocide 失效
    唑类衍生物和唑类杀真菌剂

    公开(公告)号:US5240955A

    公开(公告)日:1993-08-31

    申请号:US928954

    申请日:1992-08-13

    申请人: Satoru Kumazawa

    发明人: Satoru Kumazawa

    IPC分类号: C07D249/08 C07D521/00

    摘要: Disclosed herein are azole derivatives or the salts thereof which are represented by the general formula (I): ##STR1## wherein X represents a halogen atom, an alkyl group having 1 to 5 carbon atoms, a haloalkyl group, a phenyl group, a cyano group, or a nitro group, Xs being either the same or different from each other; n represents an integer of 1 to 5; A represents a nitrogen atom or CH; and one of R.sub.1 and R.sub.2 represents an alkyl group having 1 to 5 carbon atoms and the other a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, with the proviso that when n is 1 or 2, X does not represent a halogen atom, an alkyl group having 1 to 5 carbon atoms or a phenyl group, and mycocides comprising an effective amount of azole derivative or medically or veterinarily acceptable salt thereof, said azole derivative being represented by the general formula (II): ##STR2## wherein X represents a halogen atom, an alkyl group having 1 to 5 carbon atoms, a haloalkyl group, a phenyl group, a cyano group, or a nitro group, Xs being either the same or different from each other; n represents an integer of 0 to 5; A represents a nitrogen atom or CH; and R.sub.1 and R.sub.2 respectively represent a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, and a diluent or a carrier which is medically or veterinarily acceptable.

    摘要翻译: 本文公开的是由通式(I)表示的唑衍生物或其盐:其中X表示卤素原子,具有1至5个碳原子的烷基,卤代烷基,苯基 ,氰基或硝基,Xs彼此相同或不同; n表示1〜5的整数, A表示氮原子或CH; R1和R2之一表示碳原子数为1〜5的烷基,另一个为氢原子或碳原子数为1〜5的烷基,条件是当n为1或2时,X不表示卤素 原子,具有1〜5个碳原子的烷基或苯基,以及包含有效量的唑衍生物或其医学上或兽医学上可接受的盐的霉菌,所述唑衍生物由通式(II)表示: II)其中X表示卤素原子,具有1至5个碳原子的烷基,卤代烷基,苯基,氰基或硝基,X可以相同或不同; n表示0〜5的整数, A表示氮原子或CH; R 1和R 2分别表示氢原子或碳原子数1〜5的烷基,以及在医学上或兽医学上可接受的稀释剂或载体。

    Alkyl 3-(substituted or unsubstituted
benzylidene)-1-alkyl-2-oxocyclopentanecarboxylate derivatives, process
for preparing the same
    35.
    发明授权
    Alkyl 3-(substituted or unsubstituted benzylidene)-1-alkyl-2-oxocyclopentanecarboxylate derivatives, process for preparing the same 失效
    烷基3-(取代或未取代的亚苄基)-1-烷基-2-氧代环戊烷羧酸酯衍生物,其制备方法

    公开(公告)号:US5519160A

    公开(公告)日:1996-05-21

    申请号:US340150

    申请日:1994-11-15

    CPC分类号: C07C69/757 A01N37/42

    摘要: Derivatives of alkyl 3-(substituted or unsubstituted benzylidene)-1-alkyl-2-oxocylopentanecarboxylate of the following formula (I), ##STR1## wherein R.sup.1 and R.sup.2 individually represent a lower alkyl group; X is a halogen atom, a cyano group, an alkyl group, a haloalkyl group, a phenyl group, or a nitro group; and m is an integer of 0 to 5; provided when m is 2 or larger, Xs may be either the same or different. The compounds are useful themselves as an effective ingredient of antifungal compositions, and can be used for intermediates of agriculture chemicals and medicines.

    摘要翻译: 下式(I)的烷基3-(取代或未取代的亚苄基)-1-烷基-2-氧代戊烷羧酸酯的衍生物,其中R 1和R 2各自表示低级烷基; X是卤素原子,氰基,烷基,卤代烷基,苯基或硝基; m为0〜5的整数。 当m为2或更大时,X可以相同或不同。 这些化合物本身可用作抗真菌组合物的有效成分,可用于农药和药物的中间体。

    Process for optical resolution of 1,2-diol derivatives
    36.
    发明授权
    Process for optical resolution of 1,2-diol derivatives 失效
    1,2-二醇衍生物的光学拆分方法

    公开(公告)号:US5493063A

    公开(公告)日:1996-02-20

    申请号:US345463

    申请日:1994-11-21

    CPC分类号: C12P7/62 C12P41/004

    摘要: This invention provides a process for producing an optically active 1,2-diol derivative by optical resolution. The optically active 1,2-diol derivative of the formula (I) which is capable of utilizing as an intermediate of fungicidal optically-active azole derivatives can be produced by esterifying a 1,2-diol derivative of the formula (I) as a substrate with a carboxylic acid derivative of the formula (II) as a reagent in the presence of a lipase as a catalyst. ##STR1## wherein R.sup.1 is C1-C5 alkyl group, C3-C7 cycloalkyl group or C1-C5 haloalkyl group, R.sup.2 is C1-C3 alkyl group substituted by a phenyl group which may have one or two halogen atoms and/or C1-C4 alkyl groups, C2-C3 alkenyl group substituted by a phenyl group which may have one or two halogen atoms and/or C1-C4 alkyl groups, or C1-C3 alkyl group substituted by a phenoxy group which may have one or two halogen atoms and/or C1-C4 alkyl groups, R.sup.3 is C1-C10 alkyl group or aryl group, and R.sup.4 is hydrogen atom, C1-C5 alkyl group, C2-C4 alkenyl group or COR.sub.3.

    摘要翻译: 本发明提供了通过光学拆分制备光学活性1,2-二醇衍生物的方法。 能够用作杀真菌的光学活性唑衍生物的中间体的式(I)的光学活性1,2-二醇衍生物可以通过将式(I)的1,2-二醇衍生物酯化为 在作为催化剂的脂肪酶存在下,用式(II)的羧酸衍生物作为试剂的底物。 (I)R 3 COOR 4(II)其中R 1是C 1 -C 5烷基,C 3 -C 7环烷基或C 1 -C 5卤代烷基,R 2是被可以具有一个或两个卤素的苯基取代的C 1 -C 3烷基 原子和/或C 1 -C 4烷基,被可具有一个或两个卤素原子和/或C 1 -C 4烷基的苯基取代的C 2 -C 3烯基或被苯氧基取代的C 1 -C 3烷基, 具有一个或两个卤素原子和/或C 1 -C 4烷基,R 3是C 1 -C 10烷基或芳基,R 4是氢原子,C 1 -C 5烷基,C 2 -C 4烯基或COR 3。

    Process for separating optically active 1-hydroxy-cyclopentane methanol
derivatives using lipase from candida or pseudomonas
    38.
    发明授权
    Process for separating optically active 1-hydroxy-cyclopentane methanol derivatives using lipase from candida or pseudomonas 失效
    使用来自念珠菌或假单胞菌的脂肪酶分离光学活性的1-羟基 - 环戊烷甲醇衍生物的方法

    公开(公告)号:US5494821A

    公开(公告)日:1996-02-27

    申请号:US322725

    申请日:1994-10-13

    摘要: In the present invention, an optically active cis type 1,2-diol derivative of the following formula (I) is produced by reacting a cis type 1,2-diol derivative of the formula (I) with a carboxylic acid derivative of the formula (II) in the presence of a lipase: ##STR1## wherein R.sup.1 and R.sup.2 independently represent hydrogen atom or an alkyl group, X represents a halogen atom, a nitro group, a cyano group, an alkyl group, a haloalkyl group, or a phenyl group, and n represents an integer of from 0 to 5; R.sup.3 represents a C.sub.1 -C.sub.10 alkyl group or an aryl group, and R.sup.4 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, a C.sub.2 -C.sub.4 alkenyl group, or COR.sub.3.The cis type means that the bond between the cyclopentane ring and the hydroxy group and the bond between the cyclopentane ring and the benzyl group reside in the same direction as that portrayed on the paper.The optically active cis type 1,2-diol derivative is used as an intermediate for producing an optically active cis type azole derivative of the formula (VII).

    摘要翻译: 在本发明中,通式(I)的顺式1,2-二醇衍生物与式(I)的顺式1,2-二醇衍生物与式 (II)在存在脂肪酶时:(I)R 3 COOR 4(II)氢原子或烷基,X表示卤素原子,硝基,氰基,烷基,卤代烷基 基团或苯基,n表示0〜5的整数, R3表示C1-C10烷基或芳基,R4表示氢原子,C1-C5烷基,C2-C4烯基或COR3。 顺式是指环戊烷环与羟基之间的键和环戊烷环与苄基之间的键位于与纸上描绘的方向相同的方向。 光学活性顺式1,2-二醇衍生物用作制备式(Ⅶ)的光学活性顺式唑衍生物的中间体。