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公开(公告)号：US4665227A
公开(公告)日：1987-05-12
申请号：US867348
申请日：1986-05-23
IPC分类号： A61K31/18 , C07C311/15 , C07C143/78
CPC分类号： A61K31/18 , C07C311/15
摘要： Compounds presenting the following structural formula: ##STR1## in which the nitro substituent is in 3 or 4 position of the phenyl ring; R.sup.1 is hydrogen or alkyl;R.sup.2 is alkyl;R.sup.3 is hydrogen or alkyl;and n is one of the integers 0, 1 or 2;or a pharmaceutically acceptable salt thereof, are Class III anti-arrhythmic agents.
摘要翻译： 具有以下结构式的化合物：其中硝基取代基位于苯环的3或4位的
R1是氢或烷基; R2是烷基; R3是氢或烷基; 并且n是整数0,1或2之一; 或其药学上可接受的盐是III类抗心律失常药。 -
2.发明授权Resolution of 3-benzoylthio-2-methyl-propanoic acid with (+)-dehydroabietylamine 失效用（+） - 脱氢枞胺拆分3-苯甲酰硫基-2-甲基 - 丙酸
公开(公告)号：US4559178A
公开(公告)日：1985-12-17
申请号：US367126
申请日：1982-04-09
IPC分类号： A47K13/16 , C07C153/07
CPC分类号： C07C327/32
摘要： Disclosed herein is a process for the preparation of optically active compounds of the formula: ##STR1## in which R is a lower alkyl, lower alkoxy, benzyloxy, phenyl, o-nitrophenyl, p-nitrophenyl, or p-tolyl group, or salts or esters thereof, which process comprises the following steps:(a) starting with a racemic mixture of the compound of Formula I in which R is phenyl, namely, (+)-3-benzoylthio-2-methylpropanoic acid;(b) adding thereto 0.40-0.60 moles of (+)-dehydroabietylamine per mole of (+)-3-benzoylthio-2-methyl-propanoic acid as the resolving agent, in the presence of an aliphatic carboxylic acid lower alkyl ester as the resolution solvent;(c) crystallizing out and isolating the (-)-3-benzoylthio-2-methylpropanoic acid, (+)-dehydroabietylamine salt, which is dextrorotary;(d) if necessary, recrystallizing said dextrorotary salt to further purify it;(e) hydrolyzing the resulting dextrorotary salt with a base to separate the (+)-dehydroabietylamine resolving agent from the (-)-3-benzoylthio-2-methyl propanoate;(f) hydrolyzing the (-)-3-benzoylthio-2-methyl-propanoate with an acid to form the acid thereof;(g) optionally, converting the phenyl group of the resulting (-)-3-benzoylthio-2-methyl-propanoic acid to one of the other R groups of Formula I.
摘要翻译： 本文公开了一种制备下式的光学活性化合物的方法：其中R是低级烷基，低级烷氧基，苄氧基，苯基，邻硝基苯基，对硝基苯基或对甲苯基，或 其盐或酯，该方法包括以下步骤：（a）由R为苯基的式I化合物即（+） - 3-苯甲酰硫基-2-甲基丙酸的外消旋混合物开始; （b）在脂肪族羧酸低级烷基酯的存在下，向每摩尔作为拆分剂的（+） - 3-苯甲酰硫基-2-甲基 - 丙酸加入0.40-0.60摩尔（+） - 脱氢枞胺 分辨率溶剂; （c）结晶并分离（ - ） - 3-苯甲酰硫基-2-甲基丙酸，（+） - 脱氢枞胺盐，其为右旋的; （d）如果需要，将所述右旋盐重结晶以进一步净化; （e）用碱水解所得右旋盐，以从（ - ） - 3-苯甲酰硫基-2-甲基丙酸酯分离（+） - 脱氢枞胺分解剂; （f）用酸水解（ - ） - 3-苯甲酰硫基-2-甲基 - 丙酸酯以形成其酸; （g）任选地将所得（ - ） - 3-苯甲酰硫基-2-甲基 - 丙酸的苯基转化为式I的其它R基团之一。
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公开(公告)号：US5144072A
公开(公告)日：1992-09-01
申请号：US260855
申请日：1988-10-21
IPC分类号： C07C311/41
CPC分类号： C07C311/41
摘要： This invention provides Class III anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido, R.sup.2 is ethyl, R.sup.3 is hydrogen, R.sup.4 is ethyl, and n is 2 to 4, or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明提供下式的III类抗心律不齐剂：其中R1是烷基磺酰氨基，R2是乙基，R3是氢，R4是乙基，n是2至4，或其药学上可接受的盐。
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公开(公告)号：US4720580A
公开(公告)日：1988-01-19
申请号：US850805
申请日：1986-04-11
申请人： George C. Buzby, Jr.
发明人： George C. Buzby, Jr.
IPC分类号： C07C311/15 , C07C143/78
CPC分类号： C07C311/15
摘要： This invention provides a group of anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy or halo;R.sup.2 is hydrogen, alkoxy, halo or trifluoromethyl, with the proviso that R.sup.2 is not hydrogen when R.sup.1 is hydrogen;R.sup.3 is alkyl or, when R.sup.2 is trifluoromethyl and R.sup.1 is hydrogen, R.sup.3 may be hydrogen;R.sup.4 is alkyl, cycloalkyl or cycloalkylmethyl;R.sup.5 is hydrogen or alkyl;n is 2-4;or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明提供一组下式的抗心律不齐剂：其中R1是氢，羟基，烷氧基或卤素; R2是氢，烷氧基，卤素或三氟甲基，条件是当R1是氢时，R2不是氢; R 3是烷基，或者当R 2是三氟甲基且R 1是氢时，R 3可以是氢; R4是烷基，环烷基或环烷基甲基; R5是氢或烷基; n为2-4; 或其药学上可接受的盐。
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5.发明授权Process for the asymmetric synthesis of chiral .alpha.-hydroxy-2-nitrobenzenepropanoic acid 失效手性α-羟基-2-硝基苯丙酸的不对称合成方法
公开(公告)号：US4727183A
公开(公告)日：1988-02-23
申请号：US925430
申请日：1986-10-31
IPC分类号： C07D209/42 , C07C99/00
CPC分类号： C07D209/42
摘要： Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, which comprises:(a) assymetrically reducing an o-nitrophenylpyruvic acid III by contacting the acid III with a reducing complex formed from (R)-proline or (S)-proline, respectively, and sodium borohydride in an inert solvent to form, respectively, an (S) or (R)-.alpha.-hydroxy-2-nitrobenzenepropanoic acid IV;(b) reacting, respectively, said (S) or (R)-.alpha.-hydroxy-2-nitrobenzenepropanoic acid III with a Vilsmeier chlorinating reagent in which the chlorinating agent thereof is selected from a group consisting of thionyl chloride, oxalyl chloride, phosphorus oxychloride, phosphorus pentachloride and sulfuryl chloride and the amide thereof is selected from a group consisting of dimethylformamide, diethylformamide, dimethylacetamide and diethylacetamide, said reaction being run at temperatures of at least 20.degree. C., in order to obtain, respectively, and (R) or (S)-.alpha.-chloro-2-nitrobenzenepropanoic acid IV;(c) reducing the nitro group of said (R) or (S)-.alpha.-chloro-2-nitrobenzenepropanoic acid (V) to an amino group; and(d) cyclizing the resulting (R) or (S)-.alpha.-chloro-2-aminobenzenepropanoic acid in aqueous base.
摘要翻译： 本文公开了一种制备结构式：其中X是氢，溴，氯，C 1-4烷基或C 1-4烷氧基的结构式的不对称二氢吲哚-2-羧酸的方法，其包括： （a）通过使酸III与由（R） - 脯氨酸或（S） - 脯氨酸分别形成的还原络合物和硼氢化钠在惰性溶剂中分别形成的（III）化合物分别对（ - S）或（R）-α-羟基-2-硝基苯丙酸IV; （b）分别使所述（S）或（R）-α-羟基-2-硝基苯丙酸III与Vilsmeier氯化试剂反应，其中氯化剂选自亚硫酰氯，草酰氯，磷 三氯氧化物，五氯化磷和磺酰氯，其酰胺选自二甲基甲酰胺，二乙基甲酰胺，二甲基乙酰胺和二乙基乙酰胺，所述反应在至少20℃的温度下进行，以分别得到（R ）或（S）-α-氯-2-硝基苯丙酸IV; （c）将所述（R）或（S）-α-氯-2-硝基苯丙酸（V）的硝基还原成氨基; 和（d）使得到的（R）或（S）-α-氯-2-氨基苯丙酸在碱性水溶液中环化。
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6.发明授权
公开(公告)号：US4614806A
公开(公告)日：1986-09-30
申请号：US700379
申请日：1985-02-11
IPC分类号： C07D209/42
CPC分类号： C07D209/42
摘要： Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, which comprises:(a) assymetrically reducing an o-nitrophenylpyruvic acid III by contacting the acid III with a reducing complex formed from (R)-proline or (S)-proline, respectively, and sodium borohydride in an inert solvent to form, respectively, an (S) or (R)-.alpha.-hydroxy-2-nitrobenzenepropanoic acid IV;(b) reacting, respectively, said (S) or (R)-.alpha.-hydroxy-2-nitrobenzenepropanoic acid III with a Vilsmeier chlorinating reagent in which the chlorinating agent thereof is selected from a group consisting of thionyl chloride, oxalyl chloride, phosphorus oxychloride, phosphorus pentachloride and sulfuryl chloride and the amide thereof is selected from a group consisting of dimethylformamide, diethylformamide, dimethylacetamide and diethylacetamide, said reaction being run at temperatures of at least 20.degree. C., in order to obtain, respectively, and (R) or (S)-.alpha.-chloro-2-nitrobenzenepropanoic acid IV;(c) reducing the nitro group of said (R) or (S)-.alpha.-chloro-2-nitrobenzenepropanoic acid (V) to an amino group; and(d) cyclizing the resulting (R) or (S)-.alpha.-chloro-2-aminobenzenepropanoic acid in aqueous base.
摘要翻译： 本文公开了一种制备结构式：其中X是氢，溴，氯，C 1-4烷基或C 1-4烷氧基的结构式的不对称二氢吲哚-2-羧酸的方法，其包括： （a）通过使酸III与由（R） - 脯氨酸或（S） - 脯氨酸分别形成的还原络合物和硼氢化钠在惰性溶剂中分别形成的（III）化合物分别对（ - S）或（R）-α-羟基-2-硝基苯丙酸IV; （b）分别使所述（S）或（R）-α-羟基-2-硝基苯丙酸III与Vilsmeier氯化试剂反应，其中氯化剂选自亚硫酰氯，草酰氯，磷 三氯氧化物，五氯化磷和磺酰氯，其酰胺选自二甲基甲酰胺，二乙基甲酰胺，二甲基乙酰胺和二乙基乙酰胺，所述反应在至少20℃的温度下进行，以分别得到（R ）或（S）-α-氯-2-硝基苯丙酸IV; （c）将所述（R）或（S）-α-氯-2-硝基苯丙酸（V）的硝基还原成氨基; 和（d）使得到的（R）或（S）-α-氯-2-氨基苯丙酸在碱性水溶液中环化。
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7.发明授权N-aminoalkylperfluoroalkanoylaminobenzene-sulfonamide anti-arrhythmic agents 失效N-氨基烷基全氟烷酰氨基苯磺酰胺抗心律失常药
公开(公告)号：US4794196A
公开(公告)日：1988-12-27
申请号：US12969
申请日：1987-02-10
IPC分类号： C07C311/15 , C07C311/37 , C07C143/80
CPC分类号： C07C311/15 , C07C311/37
摘要： N-Aminoalkyl(perfluoroalkanoylaminophenyl)sulfonic acid amides of the formula: ##STR1## in which R.sup.1 is perfluoroalkanoylamino of 2 to 4 carbon atoms, in 3- or 4- position of the benzene ring;R.sup.2 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sup.3 is hydrogen or straight or branched chain alkyl of 1 to 4 carbon atoms;R.sup.4 is straight or branched chain alkyl of 1 to 4 carbon atoms; andn is one of the integers 2, 3 or 4;or a pharmaceutically acceptable salt thereof, are Class I anti-arrhythmic agents useful in the treatment of cardiac arrhythmias and conditions characterized by coronary arteries vasospasm and myocardial ischemia.
摘要翻译： 式中：R 1是2至4个碳原子的全氟烷酰基氨基，在苯环的3-或4-位的N-氨基烷基（全氟烷酰氨基苯基）磺酰胺，其结构如下： R2是氢或1-4个碳原子的烷基; R3是氢或1至4个碳原子的直链或支链烷基; R4是1-4个碳原子的直链或支链烷基; n是整数2,3或4之一; 或其药学上可接受的盐是可用于治疗心律失常和以冠状动脉血管痉挛和心肌缺血为特征的病症的I类抗心律失常药。
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公开(公告)号：US4721809A
公开(公告)日：1988-01-26
申请号：US909133
申请日：1986-09-18
IPC分类号： C07C311/18 , A61K31/18 , A61P9/06 , C07C311/15 , C07C311/37 , C07C143/72
CPC分类号： A61K31/18 , C07C311/15 , C07C311/37
摘要： This invention provides Class III anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido, arylsulfonamido, perfluoroalkylsulfonamido, R.sup.2 and R.sup.3 are hydrogen or alkyl, R.sup.4 is alkyl, and n is 2 to 4, or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明提供下式的III类抗心律不齐剂：其中R1是烷基磺酰氨基，芳基磺酰氨基，全氟烷基磺酰氨基，R2和R3是氢或烷基，R4是烷基，n是2-4，或其药学上可接受的盐 其中。
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9.发明授权
公开(公告)号：US4644081A
公开(公告)日：1987-02-17
申请号：US829662
申请日：1986-02-14
IPC分类号： C07D209/42 , C07C101/447
CPC分类号： C07D209/42
摘要： Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C.sub.1-4 alkyl or C.sub.1-4 alkoxy, which comprises:(a) assymetrically reducing an o-nitrophenylpyruvic acid III by contacting the acid III with a reducing complex formed from (R)-proline or (S)-proline, respectively, and sodium borohydride in an inert solvent to form, respectively, an (S) or (R)-.alpha.-hydroxy-2-nitrobenzenepropanoic acid IV;(b) reacting, respectively, said (S) or (R)-.alpha.-hydroxy-2-nitrobenzenepropanoic acid III with a Vilsmeier chlorinating reagent in which the chlorinating agent thereof is selected from a group consisting of thionyl chloride, oxalyl chloride, phosphorus oxychloride, phosphorus pentachloride and sulfuryl chloride and the amide thereof is selected from a group consisting of dimethylformamide, diethylformamide, dimethylacetamide and diethylacetamide, said reaction being run at temperatures of at least 20.degree. C., in order to obtain, respectively, and (R) or (S)-.alpha.-chloro-2-nitrobenzenepropanoic acid IV;(c) reducing the nitro group of said (R) or (S)-.alpha.-chloro-2-nitrobenzenepropanoic acid (V) to an amino group; and(d) cyclizing the resulting (R) or (S)-.alpha.-chloro-2-aminobenzenepropanoic acid in aqueous base.
摘要翻译： 本文公开了一种制备结构式：其中X是氢，溴，氯，C 1-4烷基或C 1-4烷氧基的不对称二氢吲哚-2-羧酸的方法，其包括：（a）按比例减少 通过使酸III与由（R） - 脯氨酸或（S） - 脯氨酸分别形成的还原络合物和硼氢化钠在惰性溶剂中分别与（S）或（R（R））形成的邻硝基苯基丙酮酸III反应， ）-α-羟基-2-硝基苯丙酸IV; （b）分别使所述（S）或（R）-α-羟基-2-硝基苯丙酸III与Vilsmeier氯化试剂反应，其中氯化剂选自亚硫酰氯，草酰氯，磷 三氯氧化物，五氯化磷和磺酰氯，其酰胺选自二甲基甲酰胺，二乙基甲酰胺，二甲基乙酰胺和二乙基乙酰胺，所述反应在至少20℃的温度下进行，以分别得到（R ）或（S）-α-氯-2-硝基苯丙酸IV; （c）将所述（R）或（S）-α-氯-2-硝基苯丙酸（V）的硝基还原成氨基; 和（d）使得到的（R）或（S）-α-氯-2-氨基苯丙酸在碱性水溶液中环化。
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公开(公告)号：US4698445A
公开(公告)日：1987-10-06
申请号：US875816
申请日：1986-06-18
IPC分类号： C07C311/37 , C07C143/80
CPC分类号： C07C311/37
摘要： N-Aminoalkyl(aminophenyl)sulfonic acid amides of the formula: ##STR1## in which R.sup.1 is --NH.sub.2, alkylamino of 1 to 3 carbon atoms or alkanoylamino of 2 to 4 carbon atoms, in 3- or 4-position of the benzene ring;R.sup.2 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sup.3 is hydrogen or straight or branched chain alkyl of 1 to 4 carbon atoms;R.sup.4 is straight or branched chain alkyl of 1 to 4 carbon atoms; with the proviso that R.sup.3 and R.sup.4 are branched chain alkyl when R.sup.2 is hydrogen;and n is one of the integers 2, 3 or 4;or a pharmaceutically acceptable salt thereof, an anti-arrhythmic agents useful in the treatment of cardiac arrhythmias and conditions characterized by coronary arteries vasospasm.
摘要翻译： 式中：R 1是-NH 2，1至3个碳原子的烷基氨基或2至4个碳原子的烷酰基氨基，在苯环的3-或4-位的下式的N-氨基烷基（氨基苯基）磺酸酰胺 ; R2是氢或1-4个碳原子的烷基; R3是氢或1至4个碳原子的直链或支链烷基; R4是1-4个碳原子的直链或支链烷基; 条件是当R 2为氢时，R 3和R 4为支链烷基; n是整数2,3或4之一; 或其药学上可接受的盐，可用于治疗心律失常的抗心律失常药物和以冠状动脉血管痉挛为特征的病症。
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