Process for the producing of alkylcyclopentanone derivatives
    11.
    发明授权
    Process for the producing of alkylcyclopentanone derivatives 失效
    制备烷基环戊酮衍生物的方法

    公开(公告)号:US5681979A

    公开(公告)日:1997-10-28

    申请号:US609374

    申请日:1996-03-01

    CPC分类号: C07C69/757

    摘要: The present invention provides a process for producing alkylcyclopentanone derivatives of formula (1) by reacting alkyl cyclopentanone derivatives of formula (2) and alkyl halides of formula (3) in an organic solvent in the presence of molecular sieves and an alkaline metal hydroxide: ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl group; R.sup.2 is hydrogen atom or C.sub.1 -C.sub.5 alkyl group; R.sup.3 is C.sub.1 -C.sub.5 alkyl group; Y is halogen atom, C.sub.1 -C.sub.5 alkyl group, C.sub.1 -C.sub.5 haloalkyl group, phenyl group, cyano group or nitro group; n is an integer from 0 to 5; when n is 2 or greater, Y's may be identical or different; R.sup.3 in formula (3) is the same as R.sup.3 in formula (1); and a process for preparing alkylcyclopentanone derivatives of formula (5) by reacting cyclopentanone derivatives of formula (4) and alkyl halides of formula (6) in an organic solvent in the presence of molecular sieves and an alkaline metal hydroxide: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl group; R.sup.4 is hydrogen atom or C.sub.1 -C.sub.5 alkyl group; R.sup.5 is C.sub.1 -C.sub.5 alkyl group; R.sup.k is either R.sup.4 or R.sup.5 ; Y is halogen atom, C.sub.1 -C.sub.5 alkyl group, C.sub.1 -C.sub.5 haloalkyl group, phenyl group, cyano group or nitro group; n is an integer from 0 to 5; when n is 2 or greater, Y's may be identical or different.

    摘要翻译: 本发明提供了在分子筛和碱金属氢氧化物的存在下,通过使式(2)的烷基环戊酮衍生物与式(3)的烷基卤衍生物在有机溶剂中反应制备式(1)的烷基环戊酮衍生物的方法: (1)图像(2)R3X(3)其中R1是C1-C4烷基; R2是氢原子或C1-C5烷基; R3是C1-C5烷基; Y是卤素原子,C1-C5烷基,C1-C5卤代烷基,苯基,氰基或硝基; n为0〜5的整数, 当n为2以上时,Y可以相同或不同; 式(3)中的R 3与式(1)中的R 3相同; (4)的环戊酮衍生物和式(6)的烷基卤在有机溶剂中在分子筛和碱金属氢氧化物存在下制备式(5)的烷基环戊酮衍生物的方法: (5)RkX(6)其中R1是C1-C4烷基; R4是氢原子或C1-C5烷基; R5是C1-C5烷基; Rk是R4或R5; Y是卤素原子,C1-C5烷基,C1-C5卤代烷基,苯基,氰基或硝基; n为0〜5的整数, 当n为2以上时,Y可以相同也可以不同。

    Process for production of (azolylmethyl)-(biphenylmethyl)cyclopentanol
derivatives
    12.
    发明授权
    Process for production of (azolylmethyl)-(biphenylmethyl)cyclopentanol derivatives 失效
    (唑基甲基) - (联苯甲基)环戊醇衍生物的制备方法

    公开(公告)号:US5468869A

    公开(公告)日:1995-11-21

    申请号:US124763

    申请日:1993-09-22

    摘要: This invention provides a simple process for production of an (azolylmethyl)(biphenylmethyl)cyclopentanol derivative represented by the following formula (I) in a good yield. This process comprises, as described in the following reaction formula, reacting an (azolylmethyl)(halogenophenylmethyl)cyclopentanol derivative represented by the following formula (II) with a benzene derivative represented by the following formula (III) by light irradiation. ##STR1## wherein X denotes a halogen atom, R.sup.1 and R.sup.2 denote independently a hydrogen atom or a C1-C5 alkyl group, R.sup.3 denotes a C1-C5 alkyl group, n means an integer of 0-2, and A represents CH or N.

    摘要翻译: 本发明提供以良好的产率制备由下式(I)表示的(唑基甲基)(联苯甲基)环戊醇衍生物的简单方法。 该方法如下述反应式所示,通过光照射使由下式(II)表示的(唑基甲基)(卤代苯基甲基)环戊醇衍生物与下式(III)表示的苯衍生物反应。 其中X表示卤素原子,R1和R2分别独立地表示氢原子或C1-C5烷基,R3表示C1-C5烷基,n表示0〜2的整数,A表示 CH或N.

    Azole mycocide and method of treating mycosis
    13.
    发明授权
    Azole mycocide and method of treating mycosis 失效
    唑类霉菌和治疗真菌病的方法

    公开(公告)号:US5162356A

    公开(公告)日:1992-11-10

    申请号:US666488

    申请日:1991-03-06

    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。

    Process for the preparation of 5-[(4-chlorophenyl)methyl]-2,2-dimethylcyclopentanone
    17.
    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
    18.
    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
    20.
    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。