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公开(公告)号：US11724979B2
公开(公告)日：2023-08-15
申请号：US17377125
申请日：2021-07-15
发明人： Imre Juhász , Irén Hortobágyi , Tamás Altsach , István Lászlófi , Ágnes Nagyné Borkó , Imre Rozsumberszki , Gábor Havasi , Zsuzsanna Kardos , Péter Buzder-Lantos
IPC分类号： C07C51/347 , C07C41/26 , C07C45/30 , C07C45/65 , C07C51/09 , C07C51/41 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C41/30 , C07C41/48 , C07C43/315 , C07C13/547 , C07C35/37 , C07C59/72
CPC分类号： C07C51/347 , C07C13/547 , C07C35/37 , C07C41/26 , C07C41/30 , C07C41/48 , C07C43/315 , C07C45/30 , C07C45/305 , C07C45/65 , C07C51/09 , C07C51/412 , C07C59/72 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C2603/14 , C07C45/305 , C07C49/84 , C07C45/30 , C07C49/84 , C07C45/65 , C07C49/755 , C07C51/09 , C07C59/70 , C07C41/48 , C07C43/315 , C07C67/14 , C07C69/76 , C07C67/29 , C07C69/76 , C07C67/293 , C07C69/76 , C07C51/412 , C07C59/70
摘要： Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.
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公开(公告)号：US10322990B2
公开(公告)日：2019-06-18
申请号：US15518096
申请日：2015-09-28
发明人： Imre Juhász , Irén Hortobágyi , Tamás Altsach , István Lászlófi , Ágnes Nagyné Borkó , Imre Rozsumberszki , Gábor Havasi , Zsuzsanna Kardos , Péter Buzder-Lantos
IPC分类号： C07C51/347 , C07C41/26 , C07C45/30 , C07C45/65 , C07C51/09 , C07C51/41 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C41/30 , C07C41/48 , C07C43/315 , C07C13/547 , C07C35/37 , C07C59/72
摘要： Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.
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公开(公告)号：US11098001B2
公开(公告)日：2021-08-24
申请号：US16397139
申请日：2019-04-29
发明人： Imre Juhász , Irén Hortobágyi , Tamás Altsach , István Lászlófi , Ágnes Nagyné Borkó , Imre Rozsumberszki , Gábor Havasi , Zsuzsanna Kardos , Péter Buzder-Lantos
IPC分类号： C07C51/347 , C07C41/26 , C07C45/30 , C07C45/65 , C07C51/09 , C07C51/41 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C41/30 , C07C41/48 , C07C43/315 , C07C13/547 , C07C35/37 , C07C59/72
摘要： Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. Also disclosed are treprostinil intermediates and the preparation of the intermediates.
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公开(公告)号：US09290432B2
公开(公告)日：2016-03-22
申请号：US14648504
申请日：2013-11-26
发明人： Zoltán Bischof , Ádám Bódis , Mária Kömüves-Mars , Gábor Havasi
IPC分类号： C07C67/42 , C07C405/00
CPC分类号： C07C67/42 , C07C405/00 , C07C2601/08
摘要： The subject of the invention is process the preparation of travoprost of formula (I) characterized by that the free acid of formula (II) is a.) activated with 2-chloro-1,3-dimethyl-imidazolinium chloride (DMC) and the resulting activated carboxylic acid intermediate is reacted with isopropyl alcohol, or b.) reacted with alkyl haloformate and the resulting mixed anhydride is reacted with isopropyl alcohol, or c.) activated with a straight or branched C1-8 dialkyl dicarbonate and reacted with isopropanol in the presence of water-free magnesium salt.
摘要翻译： 本发明的主题是制备式（I）的曲伏前列素，其特征在于式（II）的游离酸是由2-氯-1,3-二甲基 - 咪唑啉鎓氯化物（DMC）活化的， 使活化的羧酸中间体与异丙醇反应，或b）与卤代甲酸烷基酯反应，并将得到的混合酸酐与异丙醇反应，或c。用直链或支链C 1-8二烷基二碳酸酯活化并与异丙醇反应 存在无水镁盐。
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公开(公告)号：US09212125B2
公开(公告)日：2015-12-15
申请号：US14367317
申请日：2012-12-10
发明人： Zsuzsanna Kardos , Tibor Kiss , István Lászlofi , Irén Hortobágyi , Zoltán Bischof , Ádám Bódis , Gábor Havasi
IPC分类号： C07D407/00 , C07C67/333 , C07D307/935 , C07C405/00 , C07D307/937
CPC分类号： C07D307/935 , C07C67/333 , C07C405/00 , C07C2601/08 , C07D307/937 , Y02P20/55
摘要： The invention relates to a process for the preparation of travoprost of formula (I), comprising that, the compound of formula (II), is stereoselectively reduced, the resulting compound of formula (III), is if desired crystallized, the lactone group of the compound of formula (III) is reduced, the p-phenyl-benzoyl protecting group of the thus obtained compound of formula (IV), is removed, the resulting triol of formula (V), is, if desired after crystallization, transformed by Wittig reaction into the acid of formula (VI), which is then esterified.
摘要翻译： 本发明涉及一种制备式（I）的曲伏前列素的方法，其包括立体选择性地还原式（II）化合物，如果需要结晶，所得到的式（III）化合物，所述内酯基团 将式（Ⅳ）化合物还原，由此得到的式（Ⅳ）化合物的对 - 苯基 - 苯甲酰基保护基被除去，如果结晶后所需的式（Ⅴ）三元醇是 维t希反应成式（Ⅵ）的酸，然后酯化。
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公开(公告)号：US20140343299A1
公开(公告)日：2014-11-20
申请号：US14367317
申请日：2012-12-10
发明人： Zsuzsanna Kardos , Tibor Kiss , István Lászlofi , Irén Hortobágyi , Zoltán Bischof , Ádám Bódis , Gábor Havasi
IPC分类号： C07C67/333 , C07D307/937
CPC分类号： C07D307/935 , C07C67/333 , C07C405/00 , C07C2601/08 , C07D307/937 , Y02P20/55
摘要： The invention relates to a process for the preparation of travoprost of formula (I), comprising that, the compound of formula (II), is stereo selectively reduced, the resulting compound of formula (III), is if desired crystallized, the lactone group of the compound of formula (III) is reduced, the p-phenyl-benzoyl protecting group of the thus obtained compound of formula (IV), is removed, the resulting triol of formula (V), is, if desired after crystallization, transformed by Wittig reaction into the acid of formula (VI), which is then esterified.
摘要翻译： 本发明涉及一种制备式（I）的曲伏前列素的方法，其包括式（II）化合物立体选择性还原，所得式（III）化合物如果需要结晶，则内酯基 的式（Ⅳ）化合物被还原，得到如此得到的式（Ⅳ）化合物的对 - 苯基 - 苯甲酰基保护基，如果需要，结晶后所得到的式（Ⅴ）三醇被转化 通过Wittig反应进入式（VI）的酸，然后将其酯化。
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