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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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