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1. 发明专利

JPS58203974A Optically active imidazolylpropanediol derivative and its preparation 失效
标题翻译：光学有效的咪唑并吡喃衍生物及其制备
公开(公告)号：JPS58203974A
公开(公告)日：1983-11-28
申请号：JP5332783
申请日：1983-03-28
申请人： Sumitomo Chem Co Ltd
发明人： SAJI KITAROU , SATOU RENZOU , AONO SHIYUNJI , ICHINOSE KATSUAKI , OKUDA TAKAO , ATAMI TOSHIO
IPC分类号： C07D233/60 , A61K31/415 , A61P31/04 , A61P31/10
摘要： NEW MATERIAL:(R)-2-(2,4-Dichlorophenyl)-1-(imidazol-1-yl)-2,3-propanediol of formula I .
USE: A synthetic intermediate of optically active imidazolylalkylthiopropanol derivative having strong mycostatic activity.
PROCESS: The optically active diol derivative of formula I can be prepared e.g. by (1) reacting the racemic imidazolyldiol derivative of formula II with an optically active carboxylic acid or its reactive derivative, preferably the optically active carboxylic acid of formula III to obtain the 1:1 mixture of two kinds of diastereomer esters, (2) separating the objective ester from the diastereomer mixture by chromatography, fractional recrystallization, etc., and (3) hydrolyzing the resultant ester.
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式I的（R）-2-（2,4-二氯苯基）-1-（咪唑-1-基）-2,3-丙二醇。用途：具有很强的静电活性的光学活性咪唑基烷基硫代丙醇衍生物的合成中间体。方法：式I的光学活性二醇衍生物可以例如制备。通过（1）使式II的外消旋咪唑烷二醇衍生物与光学活性羧酸或其反应性衍生物，优选式III的光学活性羧酸反应，得到两种非对映体酯的1:1混合物，（2）分离通过色谱法，分级重结晶等来自非对映异构体混合物的目标酯，和（3）水解所得酯。

2. 发明专利

JPS58203988A Optically active imidazolylmethyloxirane derivative and its preparation 失效
标题翻译：光学活性的咪唑啉衍生物衍生物及其制备
公开(公告)号：JPS58203988A
公开(公告)日：1983-11-28
申请号：JP5332683
申请日：1983-03-28
申请人： Sumitomo Chem Co Ltd
发明人： SAJI KITAROU , SATOU RENZOU , AONO SHIYUNJI , ICHINOSE KATSUAKI , OKUDA TAKAO , ATAMI TOSHIO
IPC分类号： C07C57/58 , C07B31/00 , C07B57/00 , C07C51/00 , C07C67/00 , C07D405/06
摘要： NEW MATERIAL:(R)-2-(2,4-Dichlorophenyl)-2-(imidazol-1-yl)methyloxirane of formula I .
USE: A synthetic intermediate of optically active imidazolylalkylthiopropanol derivative having strong antifungal activity.
PROCESS: The racemic isomer of the imidazolyldiol derivative of formula II is made to react with an optically active carboxylic acid (or its reactive derivative) (preferably the compound of formula III) to obtain two kinds of diastereomer esters, from which the objective ester is separated. The separated ester is hydrolyzed under alkaline condition, and the resultant optically active imidazolyldiol derivative of formula IV is methylated with methanesulfonyl chloride, and without isolating from the reaction system, treated with an alkali to obtain the objective compound of formula I .
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式I的（R）-2-（2,4-二氯苯基）-2-（咪唑-1-基）甲基环氧乙烷。用途：具有强抗真菌活性的光学活性咪唑基烷基硫代丙醇衍生物的合成中间体。方法：使式II的咪唑烷二醇衍生物的外消旋异构体与光学活性羧酸（或其反应性衍生物）（优选式III化合物）反应，得到两种非对映异构体酯，其中目标酯为分开将分离的酯在碱性条件下水解，将得到的式Ⅳ的旋光性咪唑烷二醇衍生物用甲磺酰氯甲基化，不用从反应体系中分离，用碱处理，得到目的化合物Ⅰ。

3. 发明专利

JPS58203973A Optically active imidazolyl alcohol derivative and its preparation 失效
标题翻译：光学活性咪唑啉醇衍生物及其制备
公开(公告)号：JPS58203973A
公开(公告)日：1983-11-28
申请号：JP8853082
申请日：1982-05-24
申请人： Sumitomo Chem Co Ltd
发明人： SAJI KITAROU , SATOU RENZOU , AONO SHIYUNJI , ICHINOSE KATSUAKI , OKUDA TAKAO , ATAMI TOSHIO
IPC分类号： A61K31/415 , A61P31/04 , A61P31/10 , C07C55/07 , C07D233/60 , C07D521/00
CPC分类号： C07D231/12 , C07C55/07 , C07D233/56 , C07D249/08
摘要： NEW MATERIAL:The optically active imidazolyl alcohol derivative of formula I (n is 3 or 4; *C is asymmetric carbon atom) having (-) optical rotation in methanol solution, and its salt.
EXAMPLE: (-)-3-( n-Butylthio )-2-( 2,4-dichlorophenyl )-1-(imidazol-1-yl)-2-propanol hydrochloride.
USE: An antifungal agent. It has especially strong antifungal activity, and exhibits remarkable life-elongating effect in the life-elongation test using mouse.
PROCESS: The compound of formula I can be prepared by reacting the optically active epoxide derivative of formula II having (-)-optical rotation in methanol solution with an alkali metal salt of the thiol derivative of formula III (M is alkali metal) in a proper solvent at 0W30°C.
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：在甲醇溶液中具有（ - ）旋光性的式I的光学活性咪唑基醇衍生物（n为3或4; * C为不对称碳原子）及其盐。实施例：（ - ） - 3-（正丁硫基）-2-（2,4-二氯苯基）-1-（咪唑-1-基）-2-丙醇盐酸盐。用途：抗真菌剂。它具有特别强的抗真菌活性，并且在使用小鼠的寿命延长试验中显示出显着的寿命延长效果。方法：式I化合物可以通过在甲醇溶液中具有（ - ） - 旋光性的式II的光学活性环氧化物衍生物与式III的硫醇衍生物的碱金属盐（M是碱金属）反应来制备适当的溶剂在0-30℃。

4. 发明专利

JPS5758680A 1,2,4-triazines 失效
标题翻译： 1,2,4-TRIAZINES
公开(公告)号：JPS5758680A
公开(公告)日：1982-04-08
申请号：JP13334880
申请日：1980-09-24
申请人： Sumitomo Chem Co Ltd
发明人： TAMOTO KATSUMI , AONO SHIYUNJI , OKUDA TAKAO , YASUKUI HIDEO
IPC分类号： C07D401/04 , A61K31/53 , A61P31/04 , A61P31/10
摘要： NEW MATERIAL:A 1,2,4-triazine derivative shown by the formulaI[Ar is phenyl containing a substituent group (phenyl or phenoxy), naphtyl, or thienyl capable of containing halogen substituted group].
EXAMPLE: 3-Pyridyl-6-(4-phenoxyphenyl)-1,2,4-triazine-5-one.
USE: An antifungal agent.
PROCESS: a ketocarbonic acid derivative shown by the formula II (R is H or lower alkyl) is condensed with a 2-pyridylhydrazine to give a Schiff base shown by the formula IV, which is subjected to ring closure to give a compound shown by the formulaI.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：由式I [Ar表示的1,2,4-三嗪衍生物是含有取代基（苯基或苯氧基）的苯基，萘基或可含有卤素取代基的噻吩基]。实施例：3-吡啶基-6-（4-苯氧基苯基）-1,2,4-三嗪-5-酮。用途：抗真菌剂。方法：将式II表示的酮碳酸衍生物（R为H或低级烷基）与2-吡啶基肼缩合，得到式IV所示的席夫碱，其通过闭环以得到由公式I

5. 发明专利

JPS5748912A Antiulcer agent 失效
标题翻译：抗体药剂
公开(公告)号：JPS5748912A
公开(公告)日：1982-03-20
申请号：JP12497580
申请日：1980-09-08
申请人： Sumitomo Chem Co Ltd
发明人： SUGIE AKIHIKO , KAWAKAMI HAJIME , FUKUDA TOKUO , ONO KEIICHI , AONO SHIYUNJI , KATSUBE SUMIMOTO
IPC分类号： A61K31/19 , A61K31/215 , A61P1/04
摘要： NEW MATERIAL:A compound of formula I (R
1 is H or 1W4C lower alkyl) and a salt thereof.
EXAMPLE: The compound of formula II.
USE: A chemically stable antiulcer agent, having excellent selectivity, with little side effects, and useful for diseases, e.g. duodenal ulcer, and administrable orally and parenterally.
PROCESS: As shown in the reaction formulas, a cyclohexene derivative of formula III is subjected to the oxidative ring cleavage to give a dialdehyde derivative of formula IV, which is then subjected to the intramolecular aldol reaction to afford a compound of formula V. The resultant compound of formula V is then reacted with a wittig reagent to give a compound of formula VI, which is subsequently reduced to afford a compound of formula VII. The protecting group of the ketal ketonic group expressed by W is then removed from the resultant compound of formula VII to give a compound of formula VIII, which is then reacted with a Wittig reagent to afford the compound of formula I.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式Ⅰ化合物（R1为H或1-4C低级烷基）及其盐。实施例：式II化合物。用途：化学稳定的抗溃疡剂，具有优异的选择性，副作用小，可用于疾病，例如十二指肠溃疡，口服和肠胃外给药。方法：如反应式所示，将式III的环己烯衍生物进行氧化环切割，得到式IV的二醛衍生物，然后将其进行分子内醛醇缩合反应，得到式V化合物。所得物然后将式V化合物与无机试剂反应，得到式Ⅵ化合物，随后将其还原，得到式Ⅶ化合物。然后将由W表示的缩酮酮基团的保护基从所得到的式VII化合物中除去，得到式VIII化合物，然后与Wittig试剂反应，得到式I化合物。

6. 发明专利

JPS5767579A 1-substituted imidazole 失效
标题翻译： 1-取代的咪唑
公开(公告)号：JPS5767579A
公开(公告)日：1982-04-24
申请号：JP14339080
申请日：1980-10-13
申请人： Sumitomo Chem Co Ltd
发明人： SAJI KITAROU , AONO SHIYUNJI , OKUDA TAKAO , YASUKUI HIDEO
IPC分类号： C07D405/04 , A61K31/415 , A61P31/04 , A61P31/10
摘要： NEW MATERIAL:A compound of formulaI(Ph is phenyl, which may be substituted with halogen; Alk is alkyl, aralkyl, which may be substituted with halogen) and its acid adduct.
EXAMPLE: L-[1,2-Epoxy-2-(2,4-dichlorophenyl)propyl]imidazole nitrate.
USE: Antimycotic: a part of these compounds shows effects against fungi causing plant diseases as well.
PREPARATION: The reaction of a haloaldehyde derivative of formula II (Z is halogen) with a imidazole formula III or its reactive derivative in an appropriate solvent gives the compound of formulaI.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式I化合物（Ph为苯基，可被卤素取代; Alk为可被卤素取代的烷基，芳烷基）及其酸加成物。实施例：L- [1,2-环氧-2-（2,4-二氯苯基）丙基]咪唑硝酸盐。用途：抗真菌：这些化合物的一部分也显示对引起植物病害的真菌的作用。制备：式II的卤代醛衍生物（Z是卤素）与咪唑式III或其反应性衍生物在合适的溶剂中的反应得到式I化合物。

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