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1. 发明授权

US06521764B1 Process for the preparation of fumagillin 失效
标题翻译：烟曲霉素的制备方法
公开(公告)号：US06521764B1
公开(公告)日：2003-02-18
申请号：US10009116
申请日：2002-03-05
申请人： Gyula Farkas , Andrea Györbiró , István Hermecz , Kálmán Simon , Anna Szabó , Árpádné Vasvári
发明人： Gyula Farkas , Andrea Györbiró , István Hermecz , Kálmán Simon , Anna Szabó , Árpádné Vasvári
IPC分类号： C07D30514
CPC分类号： C07D303/22
摘要： The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium. According to the process Fumagillin can be produced in high yield and pure condition and with higher stability than products obtained by other preparation methods
摘要翻译：本发明涉及一种通过从其盐中释放制备烟曲霉素的方法，其特征在于将富马青霉素二环己胺盐与醇介质中的有机酸反应。根据该方法，富马林可以以高产率和纯度的条件生产，并且具有比通过其它制备方法获得的产品更高的稳定性

2. 发明授权

US06884895B2 Process for the preparation of spiro[(4-cyclohexanone)-[3]indol]-2′[1′H]-one derivatives 失效
标题翻译：制备螺[（4-环己酮） - [3]吲哚] -2'[1'H] - 酮衍生物的方法
公开(公告)号：US06884895B2
公开(公告)日：2005-04-26
申请号：US10409488
申请日：2003-04-08
申请人： Csaba Gönczi , Éva Csikós , István Hermecz , Gergely Héja , Árpád Illár , Lajos Nagy , Andrea Sántáné Csutor , Attila Simon , Kálmán Simon , Ágota Smelkóné Esek , Tiborné Szomor , Györgyné Szvoboda
发明人： Csaba Gönczi , Éva Csikós , István Hermecz , Gergely Héja , Árpád Illár , Lajos Nagy , Andrea Sántáné Csutor , Attila Simon , Kálmán Simon , Ágota Smelkóné Esek , Tiborné Szomor , Györgyné Szvoboda
IPC分类号： C07B61/00 , C07D209/34 , C07D209/96 , C07D405/04 , C07D209/54
CPC分类号： C07D405/04 , C07D209/34 , C07D209/96 , Y02P20/55
摘要： The invention relates to a process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of the general formula I wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of the general formula II wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group, selected from 2-tetrahydropyranyl, 1-diethoxy-methylene or C1-4alkoxycarbonylethyl group—with an acrylic acid C1-4ester, cyclizing the resulting compound of the general formula IV wherein R1, R2 and A are as defined above, R3 stands for C1-4 alkyl group—, eliminating the —COOR3 group and the A protective group of the keto-ester of general formula V wherein R1, R2, R3 and A are as defined above, optionally without isolation of the compounds of the general formulae IV
摘要翻译：本发明涉及制备通式I的螺[（4-环己酮） - [3 H]吲哚] -2'[1'H] - 酮衍生物的方法，其中R 1和 R 2独立地代表氢，C 1-4烷基，C 1-4 - 烷氧基，C 1-4 - 烷基 >烷硫基，C 1-4 - 多氟烷基，C 1-4 - 多氟烷氧基，C 3-7环烷氧基，C 3-7 - 其中R 1和R 2各自独立地表示：其中R 1，R 2和R 2各自为与可以引入选自2-四氢吡喃基，1-二乙氧基 - 亚甲基或C 1-4烷氧基羰基乙基的保护基的化合物，将由此得到的通式III的化合物 - 其中R 1和R 2如上定义，A代表保护基团，其选自2-四氢吡喃基，1-二乙氧基 - 亚甲基或C 1〜 4烷氧基羰基与丙烯酸C 1-4 - 酯反应，将得到的通式Ⅳ化合物环化，其中R 1，R 2和R 2， A如上所定义，R 3代表C 1-4烷基，除去-COOR 3 O 3基团和A保护基团的通式V的酮酯，其中R 1，R 2，R 3和A如上所定义，任选地不分离通式IV的化合物

3. 发明授权

US06548702B1 Method for the preparation of 2-methoxy-4-(N-t-butylamino-carbonyl)-benzenesulfonyl chloride 失效
标题翻译： 2-甲氧基-4-（N-叔丁基氨基 - 羰基） - 苯磺酰氯的制备方法
公开(公告)号：US06548702B1
公开(公告)日：2003-04-15
申请号：US10030655
申请日：2002-04-26
申请人： Csaba Gönczi , Éva Csikós , Félix Hajdú , István Hermecz , Gergely Héja , Gergelyné Héja , Lajos Nagy , Andrea Sántáné Csutor , Kálmán Simon , Ágota Smelkóné Esek , Tiborné Szomor , Györgyné Szvoboda
发明人： Csaba Gönczi , Éva Csikós , Félix Hajdú , István Hermecz , Gergely Héja , Gergelyné Héja , Lajos Nagy , Andrea Sántáné Csutor , Kálmán Simon , Ágota Smelkóné Esek , Tiborné Szomor , Györgyné Szvoboda
IPC分类号： C07C30306
CPC分类号： C07C303/32 , C07C303/06 , C07C303/22 , C07C309/60 , C07C309/89
摘要： The invention relates to a process for the preparation of 2-methoxy-4-(N-t-butylaminocarbonyl)benzenesulfonyl chloride by sulfonating m-hydroxybenzoic acid, methylating the hydroxy group of the resulting sulfonic acid or its salt, transforming the carboxylic acid group and the sulfonic acid group to acid chloride groups and reacting the 4-chlorosulfonyl-3-methoxy-benzoyl chloride with t-butylamine, which comprises carrying out the sulfonation of the 3-methoxy-benzoic acid of general formula (II) with 96% sulfuric acid, separating the resulting 3-hydroxy-4-sulfobenzoic acid of general formula (III) in the form of its salt of general formula (IV), wherein Z stands for alkali metal or ammonium group, methylating the compound of general formula (IV) in the presence of a phase transfer catalyst at a pH value of about 11.5, transforming the 3-methoxy-4-sulfobenzoic acid mono salt of general formula (V), wherein the meaning of Z is as defined above, to the acid chloride of general formula (VI), and reacting the compound of general formula (VI) with t-butylamine used in equimolar amount or in a small excess, in the presence of an acid binding agent, in aprotic solvent, at low temperature.
摘要翻译：本发明涉及通过磺化间羟基苯甲酸制备2-甲氧基-4-（N叔丁基氨基羰基）苯磺酰氯的方法，甲基化所得磺酸或其盐的羟基，转化羧酸基团和磺酸基团与酰氯基团反应，并使4-氯磺酰基-3-甲氧基苯甲酰氯与叔丁胺反应，其中包括用96％硫酸进行磺化通式（II）的3-甲氧基 - 苯甲酸将通式（III）的3-羟基-4-磺基苯甲酸以通式（Ⅳ）的盐形式分离，其中Z代表碱金属或铵基，甲基化通式（Ⅳ）的化合物，在pH值为约11.5的相转移催化剂的存在下，将Z的含义如上定义的通式（Ⅴ）的3-甲氧基-4-磺基苯甲酸单盐转化为通式（六），并且在非质子传递溶剂中在低温下使通式（VI）的化合物与等摩尔量或少量过量的叔丁胺在酸结合剂的存在下反应。

4. 发明授权

US06541643B1 Process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3h]indol]-2′[1′H]one derivatives 失效
标题翻译：螺[顺-4-（β-羟乙氧基）环己烷 - [3h]吲哚] -2'[1'H]一种衍生物的制备方法
公开(公告)号：US06541643B1
公开(公告)日：2003-04-01
申请号：US10030649
申请日：2002-04-17
申请人： Gergely Héja , Éva Csikós , Csaba Gönczi , Judit Halász , Félix Hajdú , István Hermecz , László Kis , Lajos Nagy , Andrea Sántáné Csutor , Kálmán Simon , Tiborné Szomor , Györgyné Szvoboda
发明人： Gergely Héja , Éva Csikós , Csaba Gönczi , Judit Halász , Félix Hajdú , István Hermecz , László Kis , Lajos Nagy , Andrea Sántáné Csutor , Kálmán Simon , Tiborné Szomor , Györgyné Szvoboda
IPC分类号： C07D20996
CPC分类号： C07D209/96
摘要： The invention relates to a process for the preparation of spiro[cis-4-(&bgr;-hydroxyethyloxy)cyclohexane-[3H]indol]-2′[1′H]-one derivatives of the formula (I) wherein R1 and R2 are as defined herein, by reduction of a dispiro[(1,3-dioxolane)-2,4′-cyclohexane-1′3′-[3H]indol]-2″[1″H]-one derivative of general formula (II), wherein R1 and R2 are as defined herein, which comprises carrying out the reduction (a) with sodium cyanoborohydride in the presence of a Lewis acid, or (b) with sodium borohydride in the presence of a strong acid.
摘要翻译：本发明涉及制备式（I）的螺[顺-4-（β-羟乙氧基）环己烷 - [3 H]吲哚] -2'[1'H] - 酮衍生物的方法，其中R 1和R 2是通过还原一般的[（1,3-二氧戊环）-2,4'-环己烷-1,3' - [3 H]吲哚] -2“[1'H] - 酮衍生物式（II）其中R1和R2如本文所定义，其包括在路易斯酸存在下用氰基硼氢化钠进行还原（a），或（b）在强酸存在下用硼氢化钠进行还原（a）。

5. 发明授权

US06600039B1 PROCESS FOR THE PREPARATION OF N-(1,1-DIMETHYLETHYL)-4-[[5′-ETHOXY-4-CIS[2-(4-MORPHOLINO)ETHOXY]-2′-OXOSPIRO[CYCLOHEXAN-1,3′[H]INDOL]1′(2′-H)-YL]-SULFONYL]-3-METHOXYBENZAMIDE AND ITS SALTS 失效
标题翻译：制备N-（1,1-二甲基乙基）-4 - [[5'-乙氧基-4- CIS [2-（4-吗啉基）乙氧基] -2'-氧代吡咯并[环己基] -1,3- H]吲哚] 1'（2'-H）-YL] - 磺基] -3-甲氧基苯甲酸及其盐
公开(公告)号：US06600039B1
公开(公告)日：2003-07-29
申请号：US10030647
申请日：2002-04-17
申请人： Gergely Héja , Éva Csikós , Tünde Erösné Takácsy , Csaba Gönczi , Judit Halász , István Hermecz , Csilla Majláth , Lajos Nagy , Andrea Sántáné Csutor , Péter Sárosi , Kálmán Simon , Tiborné Szomor , Györgyné Szvoboda
发明人： Gergely Héja , Éva Csikós , Tünde Erösné Takácsy , Csaba Gönczi , Judit Halász , István Hermecz , Csilla Majláth , Lajos Nagy , Andrea Sántáné Csutor , Péter Sárosi , Kálmán Simon , Tiborné Szomor , Györgyné Szvoboda
IPC分类号： C07D27300
CPC分类号： C07D209/96
摘要： The invention relates to a process for the preparation of a compound of formula (I) and the salts thereof by reacting the compound of formula (II) with the compound of formula (III), which comprises carrying out the reaction in dimethyl sulfoxide, at a temperature between 10° C. and 40° C., preferably at room temperature and transforming the resulting base of formula (I), if desired, into its salt by a method known per se.
摘要翻译：本发明涉及制备式（I）化合物及其盐的方法，其通过使式（II）化合物与式（III）化合物反应，其包括在二甲基亚砜中进行反应，温度在10℃至40℃之间，优选在室温下，如果需要，通过本身已知的方法将得到的式（I）碱转化成其盐。

6. 发明授权

US06573386B1 Process for the preparation of spiro[(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives 失效
标题翻译：制备螺[（4-环己酮） - [3H]吲哚] -2'[1'H] - 酮衍生物的方法
公开(公告)号：US06573386B1
公开(公告)日：2003-06-03
申请号：US10030648
申请日：2002-04-17
申请人： Csaba Gönczi , Éva Csikós , István Hermecz , Gergely Héja , Árpád Illár , Lajos Nagy , Andrea Sántáné Csutor , Attila Simon , Kálmán Simon , Ágota Smelkóné Esek , Tiborné Szomor , Györgyné Szvoboda
发明人： Csaba Gönczi , Éva Csikós , István Hermecz , Gergely Héja , Árpád Illár , Lajos Nagy , Andrea Sántáné Csutor , Attila Simon , Kálmán Simon , Ágota Smelkóné Esek , Tiborné Szomor , Györgyné Szvoboda
IPC分类号： C07D20954
CPC分类号： C07D405/04 , C07D209/34 , C07D209/96 , Y02P20/55
摘要： The invention relates to a process for the preparation of spiro [(4-cyclohexanone)-[3H]indol]-2′[1′H]-one derivatives of general formula I—wherein R1 and R2 independently stand for hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4polyfluoroalkyl, C1-4polyfluoroalkoxy, C3-7cycloalkyloxy, C3-7cycloalkylthio, phenoxy, benzyloxy or nitro group—, characterized by reacting an indolin-2-one derivative of general formula II—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of general formula III, thus obtained—wherein R1 and R2 are as defined above and A stands for a protective group—with acrylic acid C1-4ester; cyclizing the resulting compound of general formula IV—wherein R1 and R2 are as defined above—with a compound capable for introducing a protective group, coupling the compound of formula III thus obtained,—wherein R1 and R2 are as defined above and A stands for a protective group—with an acrylic acid C1-4ester, cyclizing the resulting compound of formula IV—wherein R1 and R2 are as defined above R3 stands for C1-4alkyl and A stands for a protective group—, eliminating the—COOR3 group and the A protective group of the keto-ester of general formula V—wherein R1 and R2 are as defined above, R3 stands for C1-4alkyl and A stands for a protective group—, optionally without isolation of the compounds of general formulae IV and/or V and/or VI.
摘要翻译：本发明涉及制备通式I的螺[（4-环己酮） - [3 H]吲哚] -2'[1'H] - 酮衍生物的方法，其中R 1和R 2独立代表氢，C1- 4-烷基，C 1-4烷氧基，C 1-4烷硫基，C 1-4多氟烷基，C 1-4多氟烷氧基，C 3-7环烷氧基，C 3-7环烷硫基，苯氧基，苄氧基或硝基，其特征在于使通式II的二氢吲哚-2-酮衍生物 - R1和R2如上定义 - 与能够引入保护基团的化合物偶合，由此得到的通式III化合物 - 其中R 1和R 2如上所定义，A代表保护基 - 与丙烯酸C1- 4ester; 使所得到的通式IV化合物（其中R 1和R 2如上定义）与可引入保护基的化合物环化，将所得式III化合物偶联，其中R 1和R 2如上所定义，A代表保护基 - 与丙烯酸C1-4酯，使所得到的式IV化合物环化，其中R 1和R 2如上所定义。R3代表C 1-4烷基，A代表保护基，除去-COOR 3基团和通式V的酮酯的保护基 - 其中R 1和R 2如上所定义，R 3表示C 1-4烷基，A代表保护基 - 任选地不分离通式IV和/或 V和/或VI。

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