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1. 发明授权

US5329035A Process for producing 2,3-disubstituted-4-substituted cyclopentanones, enantiomorphs, or mixtures thereof 失效
标题翻译： 2,3-二取代-4-取代的环戊酮，对映体或其混合物的制备方法
公开(公告)号：US5329035A
公开(公告)日：1994-07-12
申请号：US38066
申请日：1993-03-29
申请人： Ryoji Noyori , Masaaki Suzuki , Toshio Tanaka , Seizi Kurozumi
发明人： Ryoji Noyori , Masaaki Suzuki , Toshio Tanaka , Seizi Kurozumi
IPC分类号： C07C405/00 , C07F7/18
CPC分类号： C07C405/0025 , C07C405/00 , C07F7/1856
摘要： A process for producing a 2,3-disubstituted-4-substituted cyclopentanone, an enantiomorph thereof, or a mixture of these in an arbitrary ratio.The process comprises (A) subjecting a 4-substituted-2-cyclopentenone, an enantiomorph thereof, or a mixture of these in an arbitrary ratio, and an organocopper compound to conjugate addition-reaction, and thereafter (B) reacting the resulting enolate intermediate with a halide in the presence of a phenyl organotin compound.
摘要翻译：制备2,3-二取代-4-取代的环戊酮，其对映体或它们的混合物的任意比例的方法。该方法包括（A）将4-取代-2-环戊烯酮，其对映体或它们的任意比例的混合物与有机聚合物化合物进行共轭加成反应，然后（B）使得到的烯醇化物中间体在苯基有机锡化合物存在下用卤化物。

2. 发明授权

US5159102A 7-thiaprostaglandins E, and process for producing same 失效
标题翻译： 7-硫代前列腺素E及其制备方法
公开(公告)号：US5159102A
公开(公告)日：1992-10-27
申请号：US526682
申请日：1990-05-22
申请人： Toshio Tanaka , Kiyoshi Bannai , Atsuo Hazato , Seizi Kurozumi
发明人： Toshio Tanaka , Kiyoshi Bannai , Atsuo Hazato , Seizi Kurozumi
IPC分类号： C07C405/00
CPC分类号： C07C405/0033
摘要： 7-thiaprostaglandins E.sub.1 which are compounds represented by the following formula [I] or their enantiomers or mixtures thereof in any ratio: ##STR1## where R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a C.sub.2 -C.sub.20 alkenyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted C.sub.3 -C.sub.10 cycloalkyl group, a substituted or unsubstituted phenyl (C.sub.1 -C.sub.2) alkyl group, or one equivalent cation; R.sup.2 and R.sup.3, which may be the same or different, represent a hydrogen atom, a tri (C.sub.1 -C.sub.7) hydrocarbon silyl group, or a group forming an acetal linkage together with an oxygen atom of a hydroxyl group; R.sup.4 represents a hydrogen atom, a methyl group or a vinyl group; R.sup.5 represents a linear or branched C.sub.3 -C.sub.8 alkyl group, a linear or branched C.sub.3 -C.sub.8 alkenyl group, a linear or branched C.sub.2 -C.sub.8 alkynyl group, a phenyl group which may be substituted, a phenoxy group which may be substituted, a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted, or a linear or branched C.sub.1 -C.sub.5 alkyl group which may be substituted with a C.sub.1 -C.sub.6 alkoxy group, a phenyl group which may be substituted, a phenoxy group which may be substituted or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted; X represents an ethylene group, a vinylene group or an ethylene group; n represents 0 or 1; the expression represents an ethylene group or a vinylene group, provided that when n is o and x is an ethylene group, R.sup.5 is not a linear or branched C.sub.3 -C.sub.8 alkyl group or a C.sub.3 -C.sub.10 cycloalkyl group which may be substituted.Such compounds are especially useful for the treatment and prevention of digestive organ diseases such as a duodenal ulcer or a gastric ulcer.
摘要翻译：作为由下式[I]表示的化合物或其对映异构体或其混合物的7-硫代前列腺素E1为任意比例：其中R 1表示氢原子，C 1 -C 10烷基，C 2 -C 20链烯基取代或未取代的苯基，取代或未取代的C3-C10环烷基，取代或未取代的苯基（C1-C2）烷基或一个当量的阳离子; R2和R3可以相同或不同，表示氢原子，三（C1-C7）烃甲硅烷基或与羟基的氧原子一起形成缩醛键的基团; R4表示氢原子，甲基或乙烯基; R 5表示直链或支链C 3 -C 8烷基，直链或支链C 3 -C 8烯基，直链或支链C 2 -C 8炔基，可被取代的苯基，可被取代的苯氧基，C3 可以被取代的C 10环烷基，或可以被C 1 -C 6烷氧基取代的直链或支链C 1 -C 5烷基，可被取代的苯基，可被取代的苯氧基或C 3 -C 6烷氧基，可被取代的C 10环烷基; X表示亚乙基，亚乙烯基或亚乙基; n表示0或1; 该表达式表示亚乙基或亚乙烯基，条件是当n是o且x是亚乙基时，R 5不是直链或支链C 3 -C 8烷基或可被取代的C 3 -C 10环烷基。这些化合物特别可用于治疗和预防消化器官疾病如十二指肠溃疡或胃溃疡。

3. 发明授权

US5116869A 2-substituted-2-cyclopentenones 失效
标题翻译： 2-取代的2-环丙基
公开(公告)号：US5116869A
公开(公告)日：1992-05-26
申请号：US759785
申请日：1991-09-03
申请人： Satoshi Sugiura , Atsuo Hazato , Toru Minoshima , Yoshinori Kato , Yasuko Koshihara , Seizi Kurozumi
发明人： Satoshi Sugiura , Atsuo Hazato , Toru Minoshima , Yoshinori Kato , Yasuko Koshihara , Seizi Kurozumi
IPC分类号： C07C317/24 , C07C323/22 , C07C405/00 , C07D303/32 , C07D303/40
CPC分类号： C07C317/24 , C07C323/22 , C07C405/00 , C07C405/0033 , C07D303/32 , C07D303/40 , C07C2101/10
摘要： 2-Substituted-2-cyclopentenones represented by the formula (I): ##STR1## wherein A is a hydroxyl group or ##STR2## and B is a hydrogen atom or A and B are bonded together to form one bonding arm;R.sup.1 represents a substituted or unsubstituted hydrocarbon group having 1 to 10 carbon atoms;R.sup.2 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms;R.sup.3 represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 10 carbon atoms; wherein,when R.sup.3 is a single bond bonded to the cyclopentene skeleton, X represents a hydrogen atom, a hydroxyl group or a protected hydroxyl group; andwhen R.sup.3 is a double bond bonded to the pentene skeleton, X represents a bonding arm constituting a part of said double bond; andm and n independently represent 0, 1 or 2.

4. 发明授权

US4978775A Process for producing bicyclo[3.3.0]octanes 失效
标题翻译：制备双环[3.3.0]辛烷的方法
公开(公告)号：US4978775A
公开(公告)日：1990-12-18
申请号：US890690
申请日：1986-07-16
申请人： Shiro Ikegami , Yasuhiro Torizawa , Seizi Kurozumi
发明人： Shiro Ikegami , Yasuhiro Torizawa , Seizi Kurozumi
IPC分类号： C07F7/18 , C07C51/377 , C07C67/00 , C07C401/00 , C07C405/00
CPC分类号： C07C405/0083 , C07C51/377 , Y02P20/55
摘要： This invention provides a process for producing bicyclo[3.3.0]octanes expressed by the following formula [II] ##STR1## wherein R.sub.11 represents H, a one-equivalent cation or R.sub.1, R.sub..omega.' , represents R.sub..omega.' , and R.sub.21 represents H or R.sub.2,from a thiol compound expressed by the following formula [I], ##STR2## wherein R.sub.1 represents a C.sub.1-10 alkyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted alicyclic group, a substituted or unsubstituted phenyl (C.sub.1-2)alkyl group or a tri(C.sub.1-7 hydrocarbyl)silyl group, Ar represents a substituted or unsubstituted aryl group, R.sub..omega. represents a substituted or unsubstituted C.sub.1-13 alkyl group or a substituted or unsubstituted C.sub.2-13 alkenyl group, and R.sub.2 represents a hydroxyl-protecting group.This process enables to obtain isocarbacyclines or synthetic intermediates therefor with industrial advantages.
摘要翻译： PCT No.PCT / JP85 / 00636 Sec。 371日期：1986年7月16日 102（e）日期1986年7月16日PCT提交1985年11月14日PCT公布。公开号WO86 / 02923 日本公开日1986年5月22日。本发明提供一种由下式[II]表示的双环[3.3.0]辛烷的方法。其中R11表示H，单当量阳离子或R 1，R“ ，由下式[I]表示的硫醇化合物表示R omega'，R 21表示H或R 2，其中R 1表示C 1-10烷基，取代或未取代的苯基，取代或未取代的脂环基，取代或未取代的苯基（C1-2）烷基或三（C1-7烃基）甲硅烷基，Ar表示取代或未取代的芳基，R表示取代或未取代的C1-13烷基或取代或未取代的C 2-3烯基，R 2表示羟基保护基。该方法能够获得具有工业优势的异卡途菌素或其合成中间体。

5. 发明授权

US4472428A Halogenated prostacyclins pharmaceutical use thereof and hydroxy intermediates therefore 失效
标题翻译：因此，其卤化前列环素及其羟基中间体
公开(公告)号：US4472428A
公开(公告)日：1984-09-18
申请号：US327741
申请日：1981-12-04
申请人： Takeshi Toru , Kiyoshi Bannai , Takeo Oba , Toshio Tanaka , Noriaki Okamura , Kenzo Wantanabe , Seizi Kurozumi , Akira Ohtsu , Tatsuyuki Naruchi
发明人： Takeshi Toru , Kiyoshi Bannai , Takeo Oba , Toshio Tanaka , Noriaki Okamura , Kenzo Wantanabe , Seizi Kurozumi , Akira Ohtsu , Tatsuyuki Naruchi
IPC分类号： C07D307/937 , A61K31/557 , C07D307/935
CPC分类号： C07D307/937
摘要： Novel 5- or 7-monohalogenated or 5,7-dihalogenated .sup.6 -PGI.sub.1 and 5- or 7-monohalogenated or dihalogenated PGI.sub.2 (except 5-monofluorinated PGI.sub.2). The novel halogenated prostacyclins are useful for controlling vascular actions and also in organ transplantation, extra-corporeal circulation and the like. The present invention also provides processes for preparing the novel halogenated prostacyclins.
摘要翻译： 5-或7-单卤代或5,7-二卤代6-PGI1和5-或7-单卤代或二卤代PGI2（5-单氟化PGI2除外）。新型卤代前列环素可用于控制血管作用，还可用于器官移植，体外循环等。本发明还提供了制备新型卤代前列环素的方法。

6. 发明授权

US4132726A Process for the preparation of 4-hydroxycyclopent-2-en-1-one derivatives 失效
标题翻译： 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。

7. 发明授权

US5283349A 2,6,7-trisubstituted-3-methylenebicyclo(3.3.0)-octanes, and process for production thereof 失效
标题翻译： 2,6,7-三取代-3-亚甲基双环（3.3.0） - 辛烷，及其制备方法
公开(公告)号：US5283349A
公开(公告)日：1994-02-01
申请号：US905976
申请日：1986-09-11
申请人： Toshio Tanaka , Kiyoshi Bannai , Seizi Kurozumi
发明人： Toshio Tanaka , Kiyoshi Bannai , Seizi Kurozumi
IPC分类号： C07C405/00 , C07D303/14 , C07D303/16 , C07F7/18 , C07F9/117 , C07F7/08
CPC分类号： C07D303/14 , C07C405/0083 , C07D303/16 , C07F7/1856 , C07F9/117
摘要： A 2,6,7-trisubstituted-3-methylenebicyclo-[3.3.0]octane of formula (I) or an enantiomer thereof, or a mixture of these in an arbitrary ratio. The compound is a key intermediate for preparation of isocarbacyclins which are useful as medicines for the circulatory system such as an antithrombotic agent, an antilipidemic agent, a hypotensive agent or an antiarterosclerotic agent.
摘要翻译：式（I）的2,6,7-三取代-3-亚甲基双环（3.3.0）辛烷或其对映异构体，或它们的任意比例的混合物。该化合物是制备用于循环系统的药物的异卡巴菌素的关键中间体，例如抗血栓形成剂，抗血脂剂，降血压药或抗动物硬化剂。

8. 发明授权

US4841091A Process for producing 16-substituted prostaglandin es. 失效
标题翻译：生产16-取代的前列腺素的方法。
公开(公告)号：US4841091A
公开(公告)日：1989-06-20
申请号：US913889
申请日：1986-09-29
申请人： Toshio Tanaka , Atsuo Hazato , Seizi Kurozumi , Masahiro Koga
发明人： Toshio Tanaka , Atsuo Hazato , Seizi Kurozumi , Masahiro Koga
IPC分类号： C07C405/00
CPC分类号： C07C405/0033 , C07C405/00
摘要： A novel process for manufacturing 16-substituted .DELTA..sup.7 -prostaglandin Es, which include compounds expressed by the following formula (I), their enanantiomers, or their mixtures of arbitray mixing ratio, ##STR1## wherein R.sup.1 indicates COOR.sup.2, CH.sub.2 OR.sup.3, in which R.sup.2 indicates a hydrogen atom, a dubstituted or unsubstituted C.sub.1 -C.sub.10 alkyl group, a substituted or unsubstituted C.sub.3 -C.sub.10 cycloalkyl group, or a substituted or unsubstituted phenyl group, and R.sup.3 indicates a hydrogen atom, a tri(C.sub.1 -C.sub.7) hydrocarbon silyl group, a group which forms an acetal bond together with the oxygen atom of a hydroxyl group, or a C.sub.2 -C.sub.7 acyl group; R.sup.4 and R.sup.5 are identical or different, each representing a hydrogen atom, a tri(C.sub.1 -C.sub.7 ) hydrocarbon silyl group, or a group which forms an acetal bond together with the oxygen atom of a hydroxyl group; R.sup.6 indicates a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, or a vinyl group; R.sup.7 indicates a linear or branched C.sub.3 -C.sub.8 alkyl group, an alkyenyl group, or an alkynyl group, which may contain an oxygen atom; a phenyl group, a phenoxy group, or a C.sub.3 -C.sub.10 cycloalkyl group, which may be substituted; or a linear or branched C.sub.1 -C.sub.5 alkyl group which is substituted by a C.sub.1 -C.sub.6 alkoxy group, a phenyl group a phenoxy group, or a C.sub.3 -C.sub.10 cycloalkyl group, which may be substituted; and Y indicates CH.sub.2 X or XCH.sub.2, in which X represents an ethylene group, a cis -or trans-vinylene group, or an ethynylene group.
摘要翻译： PCT No.PCT / JP86 / 00034 Sec。 371日期1986年9月29日第 102（e）1986年9月29日PCT PCT公布1986年1月28日PCT公布。出版物WO86 / 04330 日期：1986年7月31日。一种用于制备16取代的DELTA 7-前列腺素Es的新方法，其包括由下式（I）表示的化合物，其对映异构体或其混合比的混合物，其中R1表示COOR2，CH2OR3，其中R2表示氢原子，取代或未取代的C1-C10烷基，取代或未取代的C3-C10环烷基或取代或未取代的苯基，R3表示氢原子，三（C 1 -C 7）烃甲硅烷基，与羟基的氧原子一起形成缩醛键的基团或C 2 -C 7酰基; R4和R5相同或不同，各自表示氢原子，三（C1-C7）烃甲硅烷基，或与羟基的氧原子一起形成缩醛键的基团; R6表示氢原子，C1-C4烷基或乙烯基; R7表示可含有氧原子的直链或支链C 3 -C 8烷基，链烯基或炔基; 可被取代的苯基，苯氧基或C3-C10环烷基; 或被可被取代的C1-C6烷氧基，苯基苯氧基或C3-C10环烷基取代的直链或支链C1-C5烷基; Y表示CH2X或XCH2，其中X表示亚乙基，顺式或反式亚乙烯基或亚乙炔基。

9. 发明授权

US4421914A 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.

10. 发明授权

US4139717A 1,3-Dicarbonyl compounds 失效
标题翻译： 1,3-二羰基化合物
公开(公告)号：US4139717A
公开(公告)日：1979-02-13
申请号：US756739
申请日：1977-01-04
申请人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto
发明人： Seizi Kurozumi , Takeshi Toru , Toshio Tanaka , Shuzi Miura , Makiko Kobayashi , Sachio Ishimoto
IPC分类号： C07C45/45 , C07C49/12 , C07C49/76 , C07C405/00 , C07F1/00 , C07F7/18 , C07C65/20 , C07C69/95
CPC分类号： C07F7/1804 , C07C405/00 , C07F1/00
摘要： 1,3-Dicarbonyl compounds useful as medicines, agricultural chemicals, perfumes, and their intermediates are prepared by reacting a specific .alpha.,.beta.-unsaturated carbonyl compound with a specific organic copper lithium compound in the presence of an aprotic inert organic solvent, and then reacting the reaction product with an organic carboxylic acid halide or anhydride. In particular, novel 2-acyl-3-substituted cyclopentan-1-ones and 2-acyl-3-substituted cyclohexan-1-ones having important physiological activities are provided.
摘要翻译：用作药物，农药，香料及其中间体的1,3-二羰基化合物通过在非质子惰性有机溶剂存在下使特定的α，β-不饱和羰基化合物与特定的有机铜锂化合物反应制备，然后使反应产物与有机羧酸卤化物或酸酐反应。特别地，提供了具有重要生理活性的新的2-酰基-3-取代的环戊烷-1-酮和2-酰基-3-取代的环己烷-1-酮。

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