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公开(公告)号：US06903220B2
公开(公告)日：2005-06-07
申请号：US10439313
申请日：2003-05-15
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24 , C07C321/00
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
摘要翻译： 非天然氨基酸例如2-烷基化氨基酸允许合成更多种类的肽和非肽类药物活性剂。 制备2-烷基氨基酸的方法包括使半胱氨酸（或其盐或其酯）和芳基羧酸反应形成噻唑啉环，立体特异性烷基化噻唑啉环，并水解噻唑啉环以获得2-烷基半胱氨酸 （或相关化合物）。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。 在该方法中，芳基腈或亚氨酸酯与半胱氨酸，2-烷基半胱氨酸或半胱氨酸酯缩合。
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公开(公告)号：US07285676B2
公开(公告)日：2007-10-23
申请号：US11085824
申请日：2005-03-21
IPC分类号： C07C323/52
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
摘要翻译： 非天然氨基酸例如2-烷基化氨基酸允许合成更多种类的肽和非肽类药物活性剂。 制备2-烷基氨基酸的方法包括使半胱氨酸（或其盐或其酯）和芳基羧酸反应形成噻唑啉环，立体特异性烷基化噻唑啉环，并水解噻唑啉环以获得2-烷基半胱氨酸 （或相关化合物）。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。 在该方法中，芳基腈或亚氨酸酯与半胱氨酸，2-烷基半胱氨酸或半胱氨酸酯缩合。
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公开(公告)号：US07038073B2
公开(公告)日：2006-05-02
申请号：US10439265
申请日：2003-05-15
IPC分类号： C07C321/00
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： A method of preparing a 2-alkyl amino acid involves the aziridination of an alkylacrylate and the opening of the aziridine ring by addition of a side chain. This method can result in the preparation of enantiomeric excess of a 2-alkyl amino acid. The invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
摘要翻译： 制备2-烷基氨基酸的方法包括丙烯酸烷基酯的氮丙啶化和通过加入侧链打开氮丙啶环。 该方法可以导致制备2-烷基氨基酸的对映体过量。 本发明还公开了一种制备与脱铁硫蛋白有关的一类铁螯合剂的方法，所有这些都含有噻唑啉环。 在该方法中，芳基腈或亚氨酸酯与半胱氨酸，2-烷基半胱氨酸或半胱氨酸酯缩合。
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公开(公告)号：US06861532B2
公开(公告)日：2005-03-01
申请号：US10438745
申请日：2003-05-15
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkylcysteine involves condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, followed by alkylating the 2-arylthiazoline-4-carboxylic acid at the 4-position. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine.
摘要翻译： 非天然氨基酸例如2-烷基化氨基酸允许合成更多种类的肽和非肽类药物活性剂。 制备2-烷基半胱氨酸的方法包括将半胱氨酸与芳基腈缩合以形成2-芳基噻唑啉-4-羧酸，随后在4-位烷基化2-芳基噻唑啉-4-羧酸。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。 在该方法中，芳基腈或亚氨酸酯与半胱氨酸或2-烷基半胱氨酸缩合。
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公开(公告)号：US07002036B2
公开(公告)日：2006-02-21
申请号：US10438770
申请日：2003-05-15
IPC分类号： C07C34/00
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
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公开(公告)号：US07576234B2
公开(公告)日：2009-08-18
申请号：US11305305
申请日：2005-12-16
IPC分类号： C07C321/00
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
摘要翻译： 非天然氨基酸例如2-烷基化氨基酸允许合成更多种类的肽和非肽类药物活性剂。 制备2-烷基氨基酸的方法包括向2-甲基亚烷基丙-1,3-二酸二烷基酯的双键加成亲核试剂，并将酯部分转化成氨基部分。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。 在该方法中，芳基腈或亚氨酸酯与半胱氨酸，2-烷基半胱氨酸或半胱氨酸酯缩合。
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公开(公告)号：US07294718B2
公开(公告)日：2007-11-13
申请号：US11008084
申请日：2004-12-09
IPC分类号： C07D277/02
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Benzimidates can be reacted with a large number of nucleophiles, leading to a wide variety of products. The present invention discloses a facile synthesis for ethyl 2,4-dihydroxybenzimidate, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid or 2,4-dibenzyloxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.
摘要翻译： 苯甲酰胺可与大量的亲核试剂反应，导致产品种类繁多。 本发明公开了2,4-二羟基苯甲酸或2,4-二苄氧基苯甲酸的2,4-二羟基苯甲亚胺乙酯及其醚和二醚的简便合成。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。 在该方法中，2,4-二羟基苄腈与（S）-2-甲基半胱氨酸缩合。
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公开(公告)号：US06875883B2
公开(公告)日：2005-04-05
申请号：US10439286
申请日：2003-05-15
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24 , C07C253/12
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： There is a significant demand for organic nitriles, based on their versatility in reactions. Compounds prepared from nitriles have properties including superoxide inhibition, ferrielectric liquid crystal dopant, antipicornaviral agents, anti-inflammatory agents, anti-asthma agents, and fibringoen antagonists. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzaldehyde or 2,4-dimethoxybenzaldehyde. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.
摘要翻译： 根据反应的多样性，对有机腈有很大的需求。 由腈制备的化合物具有包括超氧化物抑制，电介质液晶掺杂剂，止痒病毒药，抗炎剂，抗哮喘药和纤维蛋白拮抗剂的性质。 本发明公开了从2,4-二羟基苯甲醛或2,4-二甲氧基苯甲醛中轻松合成2,4-二羟基苄腈及其醚和二醚。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。 在该方法中，2,4-二羟基苄腈与（S）-2-甲基半胱氨酸缩合。
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公开(公告)号：US06875882B2
公开(公告)日：2005-04-05
申请号：US10439341
申请日：2003-05-15
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24 , C07C255/50
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： There is a significant demand for organic nitriles, based on their versatility in reactions. Compounds prepared from nitriles have properties including superoxide inhibition, ferrielectric liquid crystal dopant, antipicornaviral agents, anti-inflammatory agents, anti-asthma agents, and fibringoen antagonists. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.
摘要翻译： 根据反应的多样性，对有机腈有很大的需求。 由腈制备的化合物具有包括超氧化物抑制，电介质液晶掺杂剂，止痒病毒药，抗炎剂，抗哮喘药和纤维蛋白拮抗剂的性质。 本发明公开了2,4-二羟基苯甲酸的2,4-二羟基苯甲腈及其醚和二醚的容易合成。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。 在该方法中，2,4-二羟基苄腈与（S）-2-甲基半胱氨酸缩合。
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公开(公告)号：US06846958B2
公开(公告)日：2005-01-25
申请号：US10439342
申请日：2003-05-15
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Benzimidates can be reacted with a large number of nucleophiles, leading to a wide variety of products. The present invention discloses a facile synthesis for ethyl 2,4-dihydroxybenzimidate, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid or 2,4-dibenzyloxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.
摘要翻译： 苯甲酰胺可与大量的亲核试剂反应，导致产品种类繁多。 本发明公开了2,4-二羟基苯甲酸或2,4-二苄氧基苯甲酸的2,4-二羟基苯甲亚胺乙酯及其醚和二醚的简便合成。 本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。 在该方法中，2,4-二羟基苄腈与（S）-2-甲基半胱氨酸缩合。
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