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    2-Nitroethylcyclopentane compounds and process for preparing the same
    1.
    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

    申请人： Kiyosi Kondo ,  Daiei Tunemoto ,  Teruo Umemoto

    发明人： Kiyosi Kondo ,  Daiei Tunemoto ,  Teruo Umemoto

    IPC分类号： C07C45/51 ,  C07C45/67 ,  C07C405/00 ,  C07C49/46

    CPC分类号： C07C405/0041 ,  C07C45/511 ,  C07C45/673 ,  Y02P20/55

    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， 。

    Prostaglandin precursors
    2.
    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

    申请人： Kiyosi Kondo ,  Daiei Tunemoto ,  Teruo Umemoto

    发明人： Kiyosi Kondo ,  Daiei Tunemoto ,  Teruo Umemoto

    IPC分类号： C07C29/14 ,  C07C405/00 ,  C07F7/18 ,  C07C177/00

    CPC分类号： C07C321/00 ,  C07C405/0033 ,  C07F7/1856 ,  Y02P20/55

    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。

    Prostaglandin precursors and processes for preparing the same
    3.
    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

    申请人： Kiyosi Kondo ,  Daiei Tunemoto

    发明人： Kiyosi Kondo ,  Daiei Tunemoto

    IPC分类号： C07C405/00 ,  C07C177/00 ,  C07C147/14

    CPC分类号： C07C405/0033 ,  C07C67/00 ,  C07C2102/18

    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。

    Process for producing allyl alcohol derivatives useful in prostaglandin synthesis
    4.
    发明授权
    Process for producing allyl alcohol derivatives useful in prostaglandin synthesis 失效
    制备用于前列腺素合成的烯丙醇衍生物的方法

    公开(公告)号：US4094886A

    公开(公告)日：1978-06-13

    申请号：US767165

    申请日：1977-02-09

    申请人： Kiyosi Kondo ,  Daiei Tunemoto

    发明人： Kiyosi Kondo ,  Daiei Tunemoto

    IPC分类号： C07C405/00 ,  C07D307/935 ,  C07D307/937 ,  C07D309/12 ,  C07F7/18 ,  C07D307/93

    CPC分类号： C07D307/935 ,  C07C321/00 ,  C07C405/00 ,  C07D309/12 ,  C07F7/1852

    摘要： A novel process for producing allyl alcohol derivatives having the formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; and R.sup.2 represents an alkyl group which can have an inert substituent; and X represents a hydrogen atom, a hydroxy, an alkoxy, a tetrahydropyranyloxy or a silyloxy group; which are useful intermediates for the syntheses of prostaglandins and analogous compounds is disclosed. In the process, the allyl alcohol derivatives are produced starting from .beta.-keto-esters and azides through a series of reactions.

    摘要翻译： 一种制备式（XI）的烯丙醇衍生物的新方法，其中R1表示氢原子或低级烷基; 并且R 2表示可具有惰性取代基的烷基; X表示氢原子，羟基，烷氧基，四氢吡喃基氧基或甲硅烷氧基; 其是用于合成前列腺素和类似化合物的有用的中间体。 在此过程中，烯丙醇衍生物通过一系列反应从β-酮酯和叠氮化物开始制备。

    Method for preparing 5-mercapto-1,2,3-thiadiazole salts
    5.
    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

    申请人： Kunikazu Sakai ,  Daiei Tunemoto ,  Takeo Kobori ,  Kiyosi Kondo

    发明人： Kunikazu Sakai ,  Daiei Tunemoto ,  Takeo Kobori ,  Kiyosi Kondo

    IPC分类号： C07D249/04 ,  C07D249/06 ,  C07D285/06

    CPC分类号： C07D285/06 ,  C07D249/04 ,  C07D249/06

    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。

    1-Hydrocarbyl-pyrrole-2-acetic acid derivatives and their production
    7.
    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

    申请人： Kiyosi Kondo ,  Minoru Suda ,  Daiei Tunemoto

    发明人： Kiyosi Kondo ,  Minoru Suda ,  Daiei Tunemoto

    IPC分类号： C07D207/32 ,  C07D207/33 ,  C07D207/337 ,  C07D207/34

    CPC分类号： C07D207/33 ,  C07D207/337 ,  C07D207/34

    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。

    Precursors for prostaglandin analogue and process for preparing the same
    8.
    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

    申请人： Kiyosi Kondo ,  Daiei Tunemoto ,  Yuriko Takahatake

    发明人： Kiyosi Kondo ,  Daiei Tunemoto ,  Yuriko Takahatake

    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。

    Process for preparing 2-thio-2-substituted-alkanoic acid derivatives
    10.
    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

    申请人： Kiyosi Kondo ,  Daiei Tunemoto ,  Akira Negishi ,  Minoru Suda

    发明人： Kiyosi Kondo ,  Daiei Tunemoto ,  Akira Negishi ,  Minoru Suda

    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。