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    • 1. 发明授权
    • Process for preparing 2-thio-2-substituted-alkanoic acid derivatives
    • 2-硫代-2-取代 - 链烷酸衍生物的制备方法
    • US4245108A
    • 1981-01-13
    • US934553
    • 1978-08-17
    • Kiyosi KondoDaiei TunemotoAkira NegishiMinoru Suda
    • Kiyosi KondoDaiei TunemotoAkira NegishiMinoru Suda
    • C07D333/24C07C149/40
    • C07D333/24C07C323/00
    • 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.
    • 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。
    • 6. 发明授权
    • Precursors for prostaglandin analogue and process for preparing the same
    • 前列腺素类似物的前体及其制备方法
    • US4169199A
    • 1979-09-25
    • US862328
    • 1977-12-20
    • Kiyosi KondoDaiei TunemotoYuriko Takahatake
    • Kiyosi KondoDaiei TunemotoYuriko Takahatake
    • C07C405/00C07D309/10
    • C07C405/0033
    • 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.
    • 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。
    • 9. 发明授权
    • Prostaglandin precursors
    • 前列腺素前体
    • US4212984A
    • 1980-07-15
    • US862329
    • 1977-12-20
    • Kiyosi KondoDaiei TunemotoTeruo Umemoto
    • Kiyosi KondoDaiei TunemotoTeruo Umemoto
    • C07C29/14C07C405/00C07F7/18C07C177/00
    • C07C321/00C07C405/0033C07F7/1856Y02P20/55
    • 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.
    • 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。
    • 10. 发明授权
    • Prostaglandin precursors and processes for preparing the same
    • 前列腺素前体及其制备方法
    • US4163106A
    • 1979-07-31
    • US772053
    • 1977-02-25
    • Kiyosi KondoDaiei Tunemoto
    • Kiyosi KondoDaiei Tunemoto
    • C07C405/00C07C177/00C07C147/14
    • C07C405/0033C07C67/00C07C2102/18
    • 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.
    • 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。