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17 条记录 (耗时 0.023 秒)

    Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives
    1.
    发明授权
    Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives 失效
    4-羟基环戊-2-烯-1-酮衍生物的制备方法

    公开(公告)号：US4132726A

    公开(公告)日：1979-01-02

    申请号：US642800

    申请日：1975-12-22

    申请人： Seizi Kurozumi ,  Takeshi Toru ,  Toshio Tanaka ,  Shuzi Miura ,  Makiko Kobayashi ,  Sachio Ishimoto ,  Sadakazu Matsubara

    发明人： Seizi Kurozumi ,  Takeshi Toru ,  Toshio Tanaka ,  Shuzi Miura ,  Makiko Kobayashi ,  Sachio Ishimoto ,  Sadakazu Matsubara

    IPC分类号： C07C35/06 ,  C07C45/67 ,  C07D309/12 ,  C07F7/18 ,  C12P7/38 ,  C12P41/00

    CPC分类号： C07C49/707 ,  C07C35/06 ,  C07C45/676 ,  C07D309/12 ,  C07F7/1804 ,  C07F7/1856 ,  C12P41/004 ,  C12P7/38 ,  Y02P20/55

    摘要： Novel optically active compounds of 4-protected hydroxy-cyclopent-2-en-1-ones of the formula ##STR1## wherein R is a splittable protective group for an alcoholic hydroxyl group, and a process for preparing the 4-protected hydroxycyclopent-2-en-1-ones by oxidizing monohydroxy-protected derivatives of cyclopent-1-ene-3,5-diol expressed by the following formula ##STR2## wherein R is the same as defined above. Optically active 4-hydroxycyclopent-2-en-1-one which is an optically active isomer of the compound of formula (2); or optically active cyclopent-1-en-3,5-diol (R-isomer) and a novel diacyl derivative of the diol, a novel monoacylmonosilyl-derivative of the diol and a novel monoacylmonotetrahydropyranol-derivative of the diol, which are intermediates for the protective derivative of formula (1). Processes are also provided for preparing the protective derivatives of formula (1) by converting these intermediates by esterification, hydrolysis, enzymatic processes, etc. The optically active compounds of formula (2) are useful as precursors for the preparation of prostaglandin or its analogues.

    摘要翻译： 新型的具有式（2）的4-保护的羟基 - 环戊-2-烯-1-酮的光学活性化合物，其中R是醇羟基的可裂解的保护基，以及制备4-保护的 羟基环戊-2-烯-1-酮通过氧化由下式（1）表示的环戊-1-烯-3,5-二醇的单羟基保护衍生物，其中R与上述定义相同。 光学活性的4-羟基环戊-2-烯-1-酮，它是式（2）化合物的旋光异构体; 或光学活性的环戊-1-烯-3,5-二醇（R-异构体）和二醇的新型二酰基衍生物，二醇的新型单酰基单甲硅烷基衍生物和二醇的新型单酰基单四氢吡喃醇衍生物，其为 式（1）的保护性衍生物。 还提供了通过酯化，水解，酶法等转化这些中间体来制备式（1）的保护性衍生物的方法。式（2）的光学活性化合物可用作制备前列腺素或其类似物的前体。

    2-Organothio-2-cyclopentenones, organothio-cyclopentanes derived therefrom
    7.
    发明授权
    2-Organothio-2-cyclopentenones, organothio-cyclopentanes derived therefrom 失效
    2-有机硫代-2-环戊烯酮，衍生自其的有机硫代环戊烷

    公开(公告)号：US4180672A

    公开(公告)日：1979-12-25

    申请号：US775119

    申请日：1977-03-07

    申请人： Seizi Kurozumi ,  Takeshi Toru ,  Makiko Kobayashi ,  Yoshinobu Hashimoto

    发明人： Seizi Kurozumi ,  Takeshi Toru ,  Makiko Kobayashi ,  Yoshinobu Hashimoto

    IPC分类号： A61K31/557 ,  C07C405/00 ,  C07F7/18 ,  C07C177/00

    CPC分类号： C07F7/1856 ,  C07C323/52 ,  C07C405/0033 ,  C07C2101/08 ,  C07C2101/10

    摘要： Organothiocyclopentanes of the formula ##STR1## wherein E represents >C.dbd.O or ##STR2## in which Z' represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; X represents --S--, --CH.sub.2 --, --CH.dbd.; represents a single or double bond; R' represents a monovalent or divalent organic group containing 1 to 25 carbon atoms; R represents a monovalent organic group containing 1 to 25 carbon atoms; Z represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; and when both E and Z represent a hydroxyl group or a protected hydroxyl group, X represents --S--.Also, 2-organothio-2-cyclopentenones of the formula ##STR3## wherein R and Z are as defined above. The compounds of formula (I) are prepared by reacting 2,3-epoxy-cyclopentanone or its derivatives with mercaptans in the presence of basic compounds. The compounds of formula (II) are prepared by reacting the compounds of formula (I) with mercaptans or organocopper-lithium compounds, and optionally reducing the resulting products, and optionally protecting the hydroxyl group at their cyclopentane ring.The compounds of formula (I) have an action of inhibiting ulcer formation, and are useful intermediates for the compounds of formula (II). The compounds of formula (II) are monothia- or dithia-prostanoic acid derivatives, and exhibit various superior pharmacological actions.

    摘要翻译： 式（II）的有机硫代环戊烷，其中E表示> C = O或其中Z'表示氢原子，羟基或被保护的羟基的“IMAGE” X表示-S - ， - CH 2 - ， - CH = 代表单键或双键; R'表示含有1〜25个碳原子的一价或二价有机基团; R表示含有1〜25个碳原子的一价有机基团; Z表示氢原子，羟基或保护的羟基; 并且当E和Z都表示羟基或被保护的羟基时，X表示-S-。 另外，式（I）的2-有机硫代-2-环戊烯酮其中R和Z如上定义。 在碱性化合物的存在下，使2,3-环氧环戊酮或其衍生物与硫醇反应制备式（I）化合物。 式（II）化合物通过使式（I）化合物与硫醇或有机锂化合物反应，任选地还原所得产物和任选地保护其环戊烷环上的羟基来制备。 式（I）化合物具有抑制溃疡形成的作用，并且是式（II）化合物的有用的中间体。 式（II）化合物是单硫酸或二硫氨基 - 前列腺烷酸衍生物，具有各种优异的药理作用。

    Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof
    8.
    发明授权
    Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof 失效

    公开(公告)号：US4421914A

    公开(公告)日：1983-12-20

    申请号：US311329

    申请日：1981-10-14

    申请人： Noriaki Okamura ,  Takeshi Toru ,  Takeo Oba ,  Toshio Tanaka ,  Kiyoshi Bannai ,  Kenzo Watanabe ,  Seizi Kurozumi ,  Tatsuyuki Naruchi ,  Keiji Komoriya

    发明人： Noriaki Okamura ,  Takeshi Toru ,  Takeo Oba ,  Toshio Tanaka ,  Kiyoshi Bannai ,  Kenzo Watanabe ,  Seizi Kurozumi ,  Tatsuyuki Naruchi ,  Keiji Komoriya

    IPC分类号： C07D513/04 ,  C07D513/14 ,  A61K31/505

    CPC分类号： C07D513/04

    摘要： A compound selected from thiazolo[3,2-a]pyrimidines or their enolate derivatives represented by the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are identical or different, and each represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 3 to 10 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted cycloaliphatic group having 3 to 8 carbon atoms, a substituted or unsubstituted phenylalkyl group or a substituted or unsubstituted acyl group having 2 to 7 carbon atoms, provided that R.sup.1 and R.sup.2 are not simultaneously hydrogen atoms or substituted or unsubstituted acyl groups having 2 to 7 carbon atoms; and R.sup.1 and R.sup.2, when taken together, may form, with the nitrogen atom to which they are bonded, a 5- or 6-membered ring which may further contain one or more hetero atoms;and acid addition salts of these compounds.The thiazolo[3,2-a]pyrimidines may be prepared by a process comprising (a) reacting a malonic acid derivative of the following general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined with regard to formula (I), and R.sup.4 and R.sup.5 are identical or different and each represents an alkyl group having 1 to 6 carbon atoms,with 2-aminothiazoline under heat, if desired in the presence of an inert organic solvent, to induce cyclocondensation, or (b) performing said condensation reaction in the presence of an alkali metal alkoxide, if desired in the presence of an inert organic solvent, and neutralizing the resulting enolate with an acid; and if desired, reacting the reaction product of (a) or (b) with an acid.The present invention provides also several processes for preparing enolate derivatives thereof.The thiazolo[3,2-a]pyrimidines, their enolate derivatives and acid addition compounds thereof are useful for regulating the immune function of a warm-blooded animal.

    Thiaprostaglandin E.sub.1 derivatives, process for production thereof, and pharmaceutical use thereof
    10.
    发明授权
    Thiaprostaglandin E.sub.1 derivatives, process for production thereof, and pharmaceutical use thereof 失效
    Thiaprostaglandin E1衍生物，其制备方法及其药物用途

    公开(公告)号：US4466980A

    公开(公告)日：1984-08-21

    申请号：US316902

    申请日：1981-10-30

    申请人： Toshio Tanaka ,  Takeshi Toru ,  Takeo Oba ,  Noriaki Okamura ,  Kenzo Watanabe ,  Kiyoshi Bannai ,  Atsuo Hazato ,  Seizi Kurozumi ,  Fukuyoshi Kamimoto ,  Akira Ohtsu

    发明人： Toshio Tanaka ,  Takeshi Toru ,  Takeo Oba ,  Noriaki Okamura ,  Kenzo Watanabe ,  Kiyoshi Bannai ,  Atsuo Hazato ,  Seizi Kurozumi ,  Fukuyoshi Kamimoto ,  Akira Ohtsu

    IPC分类号： C07C405/00 ,  C07D309/12 ,  C07C177/00 ,  A61K31/557

    CPC分类号： C07C405/0033 ,  C07D309/12

    摘要： A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E.sub.1 derivatives of the formula (I). ##STR1## wherein A represents --CH.sub.2 -- or ##STR2## in which n is 0, 1 or 2, provided that only one A cut of three is ##STR3## R.sup.1 -R.sup.7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E.sub.1 derivatives, the enatiomers of said thiaprostaglandin E.sub.1 derivatives or their 15-epimers, and mixtures of these compounds.A 7-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by subjecting an .alpha.,.beta.-unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction. And, 4-thiaprostaglandin derivative and/or its optical isomer may also be prepared by the Michael addition reaction from a 2-allyl substituted cyclopentanone (VI) and a thiol (VIII).Some compounds ((I)-1) amongst the compounds of the formula (I) and/or their optical isomer are useful for controlling vascular actions such as angina pectoris, vasodilation etc.

    摘要翻译： 选自式（I）的7-（或6-或4-）赖氨酸前列腺素E1衍生物的新化合物。 （I）其中A表示-CH 2 - 或，其中n为0,1或2，条件是三个只有一个A切割是R 1 -R 7，G如说明书中所定义， 所述thiaprostaglandin E1衍生物的15-差向异构体，所述thiaprostaglandin E1衍生物或它们的15-差向异构体的对映体，以及这些化合物的混合物。 7-硫代前列腺素E1衍生物和/或其旋光异构体可以通过2-有机-2-环戊烯酮（II）与有机铜 - 锂化合物（III）反应来制备共轭反应。 6-硫代前列腺素E1衍生物和/或其旋光异构体可以通过使α，β-不饱和酮（IV）和硫醇（V）进行迈克尔加成反应来制备。 并且，也可以通过从2-烯丙基取代的环戊酮（VI）和硫醇（VIII）的迈克尔加成反应制备4-硫代前列腺素衍生物和/或其旋光异构体。 式（I）化合物和/或其旋光异构体中的一些化合物（（I）-1）可用于控制血管作用，例如心绞痛，血管舒张等。