Method for preparing 5-mercapto-1,2,3-thiadiazole salts
    1.
    发明授权
    Method for preparing 5-mercapto-1,2,3-thiadiazole salts 失效
    5-巯基-1,2,3-噻二唑盐的制备方法

    公开(公告)号:US4540794A

    公开(公告)日:1985-09-10

    申请号:US532922

    申请日:1983-09-16

    摘要: A method for preparing a 5-mercapto-1,2,3-thiadiazole salt represented by the general formula (I) is disclosed: ##STR1## the method comprises the steps of: providing a sulfonylhydrazone derivative represented by the general formula (II): ##STR2## providing a sulfide represented by the general formula (III):M--S--M' (III)(wherein R is an aryl group, X is a chlorine or bromine atom, M is an alkali metal atom and M' is a hydrogen atom or an alkali metal atom);combining the sulfonylhydrazone derivative represented by the general formula (II) and the sulfide represented by the general formula (III) and allowing a reaction to occur; andobtaining the 5-mercapto-1,2,3-thiadiazole salt represented by the general formula (I).

    摘要翻译: 公开了制备由通式(I)表示的5-巯基-1,2,3-噻二唑盐的方法:(I)该方法包括以下步骤:提供由通式(I)表示的磺酰腙衍生物 (II):提供由通式(III)表示的硫化物的化合物(II):MS-M'(III)(其中R是芳基,X是氯或溴原子,M是碱金属 原子和M'是氢原子或碱金属原子); 将由通式(II)表示的磺酰腙衍生物与由通式(III)表示的硫化物组合并进行反应; 得到通式(I)表示的5-巯基-1,2,3-噻二唑盐。

    2-Nitroethylcyclopentane compounds and process for preparing the same
    2.
    发明授权
    2-Nitroethylcyclopentane compounds and process for preparing the same 失效
    2-硝基乙基环戊烷化合物及其制备方法

    公开(公告)号:US4163758A

    公开(公告)日:1979-08-07

    申请号:US939937

    申请日:1978-09-06

    摘要: 2-Nitroethylcyclopentane compounds represented by the formula (I) ##STR1## wherein X represents a ##STR2## R and R.sup.1 each represents a hydrogen atom or a protective group for a hydroxy group, R.sup.2 represents an unsubstituted or substituted alkyl group having 1 to 8 carbon atoms and R.sup.5 represents a hydrogen atom or an alkyl group havng 1 to 4 carbon atoms, which are useful as intermediates for the synthesis of prostaglandin compounds, and a process for preparing the 2-nitroethylcyclopentane compounds of the formula (I).

    摘要翻译: 由式(I)表示的2-硝基乙基环戊烷化合物其中X表示R 1和R 1各自表示氢原子或羟基的保护基,R 2表示未取代或取代的烷基,其具有 1〜8个碳原子,R 5表示氢原子或1〜4个碳原子的烷基,可用作合成前列腺素化合物的中间体,以及制备式(I)的2-硝基乙基环戊烷化合物的方法, 。

    Precursors for prostaglandin analogue and process for preparing the same
    3.
    发明授权
    Precursors for prostaglandin analogue and process for preparing the same 失效
    前列腺素类似物的前体及其制备方法

    公开(公告)号:US4169199A

    公开(公告)日:1979-09-25

    申请号:US862328

    申请日:1977-12-20

    IPC分类号: C07C405/00 C07D309/10

    CPC分类号: C07C405/0033

    摘要: Bicyclolactone compounds represented by the formula (I) ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 4 carbon atoms, R.sup.2 represents a substituted or unsubstituted alkyl group having 1 to 8 carbon atoms and R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms;.gamma.-lactone sulfide or sulfoxide compounds represented by the formula (II) ##STR2## wherein R.sup.2 and R.sup.3 are as defined above, R.sup.4 represents a hydrogen atom or a --COOR.sup.1 group wherein R.sup.1 is as defined above, R.sup.5 represents a hydrogen atom or a --CH.sub.2 --Y--(CH.sub.2).sub.n --COOR.sup.6 group wherein Y represents a --CH.sub.2 CH.sub.2 -- group or a --CH.dbd.CH-- group, R.sup.6 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms and n is an integer of 0 to 6, R.sup.7 represents an alkyl group having 1 to 4 carbon atoms or an aryl group and m is 0 or 1, useful as precursors for prostaglandin analogues; and process for preparing the same.

    摘要翻译: 由式(I)表示的双环内酯化合物其中R 1表示具有1至4个碳原子的烷基,R 2表示取代或未取代的碳原子数1〜8的烷基,R 3表示氢原子或 具有1至4个碳原子的烷基; (II)表示的γ-LACTON硫化物或硫化物化合物其中R 2和R 3如上所定义,R 4表示氢原子或-COOR 1基团,其中R 1如上所定义,R 5表示氢 原子或-CH 2 -Y-(CH 2)n -COOR 6基团,其中Y表示-CH 2 CH 2 - 基或-CH = CH-基,R 6表示氢原子或具有1至4个碳原子的烷基,n为 0〜6的整数,R7表示碳原子数为1〜4的烷基或芳基,m为0或1,可用作前列腺素类似物的前体; 及其制备方法。

    1-Hydrocarbyl-pyrrole-2-acetic acid derivatives and their production
    5.
    发明授权
    1-Hydrocarbyl-pyrrole-2-acetic acid derivatives and their production 失效
    1-烃基 - 吡咯-2-乙酸衍生物及其制备

    公开(公告)号:US4238396A

    公开(公告)日:1980-12-09

    申请号:US963673

    申请日:1978-11-27

    摘要: 5-Cyano-1-hydrocarbylpyrrole-2-acetic acid is converted to 5-acyl-1-hydrocarbylpyrrole-2-acetic acid by reaction with a Grignard reagent followed by hydrolysis. The cyano compound, novel per se, is produced by reacting 1-hydrocarbyl-2-(2',2',2'-trihalo-1'-hydroxyethyl)pyrrole with a cyanating reagent under basic conditions. The latter pyrrole is in turn formed by reacting 1-hydrocarbylpyrrole with trihaloacetaldehyde such as chloral, preferably in the presence of added organic acid catalyst.

    摘要翻译: 5-氰基-1-烃基吡咯-2-乙酸通过与格氏试剂反应然后水解转化为5-酰基-1-烃基吡咯-2-乙酸。 氰基化合物本身是通过在碱性条件下使1-烃基-2-(2',2',2'-三卤代-1'-羟乙基)吡咯与氰化试剂反应制备的。 后者的吡咯又通过1-烃基吡咯与三卤代乙醛如氯醛反应形成,优选在加入的有机酸催化剂存在下形成。

    Process for preparing 2-thio-2-substituted-alkanoic acid derivatives
    7.
    发明授权
    Process for preparing 2-thio-2-substituted-alkanoic acid derivatives 失效
    2-硫代-2-取代 - 链烷酸衍生物的制备方法

    公开(公告)号:US4245108A

    公开(公告)日:1981-01-13

    申请号:US934553

    申请日:1978-08-17

    IPC分类号: C07D333/24 C07C149/40

    CPC分类号: C07D333/24 C07C323/00

    摘要: A process for preparing a 2-thio-2-substituted-alkanoic acid derivative represented by the formula (I) ##STR1## wherein A, R, R.sup.3 and R.sup.4 are as defined hereinafter, which comprises condensing an aldehyde compound of the formula (V)A--CHO (V)wherein A is as defined hereinafter, with a haloform of the formula CHX.sub.3 wherein X is as defined hereinafter and a mercaptan compound of the formula (IV)R.sup.3 SH (IV)wherein R.sup.3 is as defined hereinafter, in the presence of a base to produce a 2-(arylthio or alkylthio)-2-substituted-acetic acid of the formula (III) ##STR2## wherein A and R.sup.3 are as defined hereinafter, and reacting the resulting 2-(arylthio or alkylthio)-2-substituted-acetic acid of the formula (III) with an alkylating agent represented by the formula (II)RZ (II)wherein R and Z are as defined hereinafter, in the presence of at least 2 mols of a base per mol of the 2-(arylthio or alkylthio)-2-substituted-acetic acid, to form the compound of the formula (I) wherein R.sup.4 represents a hydrogen atom and, optionally, converting the resulting compound to the compound of the formula (I) wherein R.sup.4 represents an alkyl group by esterification.

    摘要翻译: 一种制备由式(I)表示的2-硫代-2-取代的链烷酸衍生物的方法,其中A,R,R 3和R 4如下文所定义,其中包括将 式(Ⅴ)A-CHO(Ⅴ)其中A如下文定义,与式CHX 3的卤代甲基,其中X如下文所定义,和式(Ⅳ)的硫醇化合物,其中R 3如下文所定义 在碱的存在下,制备式(Ⅲ)的2-(芳硫基或烷硫基)-2-取代的乙酸,其中A和R3如下文所定义,并使所得的2 式(III)的(芳硫基或烷硫基)-2-取代的乙酸与式(II)表示的烷基化剂RZ(II)其中R和Z如下文所定义,在至少2 每摩尔2-(芳硫基或烷硫基)-2-取代 - 乙酸的碱的摩尔数,形成式(I)的化合物,其中R 4表示 氢原子,并且任选地将所得化合物转化为其中R 4表示烷基的式(I)化合物。

    Prostaglandin precursors
    8.
    发明授权
    Prostaglandin precursors 失效
    前列腺素前体

    公开(公告)号:US4212984A

    公开(公告)日:1980-07-15

    申请号:US862329

    申请日:1977-12-20

    摘要: 4-Oxy-6-alkenyl-bicyclo[3.1.0]hexan-2-one compounds represented by the formula (I) ##STR1## wherein R represents a hydrogen atom or a protective group for a hydroxy group, R.sup.1 represents an alkyl group having 1 to 4 carbon atoms or an aryl group, R.sup.2 represents a substituted or unsubstituted alkyl group having 1 to 8 carbon atoms and R.sup.3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms;4-oxycyclopentanone compounds represented by the formula (II) ##STR2## wherein R, R.sup.2 and R.sup.3 are as defined above, R.sup.4 represents a hydroxymethyl group, a methylene group (.dbd.CH.sub.2) or a --COOR.sup.1 group wherein R.sup.1 is as defined above, and R.sup.5 represents an alkyl group having 1 to 4 carbon atoms or an aryl group, useful as prostaglandin precursors; and processes for preparing the same.

    摘要翻译: 由式(I)表示的4-氧基-6-烯基 - 双环[3.1.0]己-2-酮化合物其中R表示氢原子或羟基保护基,R 1表示 具有1〜4个碳原子的烷基或芳基,R 2表示取代或未取代的碳原子数1〜8的烷基,R 3表示氢原子或碳原子数1〜4的烷基。 由式(II)表示的4-羟基环戊酮化合物其中R,R 2和R 3如上所定义,R 4表示羟甲基,亚甲基(= CH 2)或-COOR 1基团,其中R 1为 R5代表具有1-4个碳原子的烷基或芳基,可用作前列腺素前体; 及其制备方法。

    Process for preparing 1,2-disubstituted-trans-olefins
    9.
    发明授权
    Process for preparing 1,2-disubstituted-trans-olefins 失效
    1,2-二取代 - 反式 - 烯烃的制备方法

    公开(公告)号:US3988380A

    公开(公告)日:1976-10-26

    申请号:US529083

    申请日:1974-12-03

    摘要: A new process for preparing 1,2-disubstituted-trans-olefins selectively by reacting specific 2-alkenyl phosphonic acid derivatives with metal hydrides, and a new process for producing the specific 2-alkenylphosphonic acid derivatives. The 1,2-disubstituted-trans-olefins are useful as precursors for synthesis of insect pheromones.

    摘要翻译: 通过使特定的2-烯基膦酸衍生物与金属氢化物反应选择性地制备1,2-二取代的 - 反式烯烃的新方法,以及用于制备特定的2-链烯基膦酸衍生物的新方法。 1,2-二取代的 - 反式 - 烯烃可用作合成昆虫信息素的前体。

    Prostaglandin precursors and processes for preparing the same
    10.
    发明授权
    Prostaglandin precursors and processes for preparing the same 失效
    前列腺素前体及其制备方法

    公开(公告)号:US4163106A

    公开(公告)日:1979-07-31

    申请号:US772053

    申请日:1977-02-25

    摘要: 6-Alkenyl-bicyclo[3.1.0]hexanone compounds represented by the formula (I) ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 4 carbon atoms or an aryl group, and R.sup.2 represents a substituted or unsubstituted alkyl group having 1 to 8 carbon atoms;Cyclopentanone compounds represented by the formula (II) ##STR2## wherein R.sup.2 is as defined above, R.sup.3 represents a hydrogen atom or a --COOR.sup.1 group wherein R.sup.1 is as defined above, R.sup.4 represents a hydrogen atom or a --CH.sub.2 --Y--(CH.sub.2).sub.n --COOR.sup.6 wherein Y represents a --CH.sub.2 CH.sub.2 -- group or a --CH.dbd.CH-- group, R.sup.6 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, and n is an integer of 0 to 6, R.sup.5 represents a --S--R.sup.7 group or a --SO--R.sup.7 group wherein R.sup.7 represents an alkyl group having 1 to 4 carbon atoms or an aryl group, with the proviso that R.sup.3 and R.sup.4 cannot be hydrogen atoms at the same time, useful as prostaglandin precursors; andProcesses for preparing the same.

    摘要翻译: 由式(I)表示的6-烯基 - 双环[3.1.0]己酮化合物其中R 1表示具有1至4个碳原子的烷基或芳基,R 2表示取代或未取代的烷基 具有1至8个碳原子的基团; 式(II)表示的环戊烷酮化合物其中R 2如上所定义,R 3表示氢原子或-COOR 1基团,其中R 1如上所定义,R 4表示氢原子或-CH 2 -Y - (CH 2)n -COOR 6其中Y表示-CH 2 CH 2 - 基或-CH = CH-基,R 6表示氢原子或碳原子数1〜4的烷基,n表示0〜6的整数, R5表示-S-R7基或-SO-R7基,其中R7表示具有1-4个碳原子的烷基或芳基,条件是R3和R4不能同时为氢原子,可用作 前列腺素前体; 及其制备方法。