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公开(公告)号：US20230115500A1
公开(公告)日：2023-04-13
申请号：US17973129
申请日：2022-10-25
发明人： Imre ROZSUMBERSZKI , Zsuzsanna KARDOS , Irén HORTOBÁGYI , Tibor SZABÓ , Csaba VÁRADI , Tamás BÁN
摘要： The present invention relates to a process for the preparation of iloprost of formula I through new intermediates, isolation of iloprost of formula I in solid form, as well as preparation of the 16(S)-iloprost and 16(R)-iloprost isomers of formulae (S)-I and (R)-I and isolation of iloprost of formula I and 16(S)-iloprost of formula (S)-I in solid, crystalline form.
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公开(公告)号：US20190248725A1
公开(公告)日：2019-08-15
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 , C07C59/72 , C07C67/14 , C07C13/547 , C07C35/37 , C07C51/41 , C07C51/09 , C07C45/65 , C07C45/30 , C07C41/26 , C07C43/315 , C07C41/48 , C07C41/30 , C07C69/76 , C07C67/293 , C07C67/29
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 , C07C49/84 , C07C49/755 , 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：US20170313643A1
公开(公告)日：2017-11-02
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 , C07C35/37 , C07C13/547 , C07C59/72 , C07C51/41 , C07C2603/14
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 , C07C49/84 , C07C49/755 , C07C59/70
摘要： The invention provides a new process for the preparation of treprostinil of formula (I) and its salts using several new intermediates during the building of the ring system.
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公开(公告)号：US20210340093A1
公开(公告)日：2021-11-04
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
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：US20210147329A1
公开(公告)日：2021-05-20
申请号：US17048053
申请日：2019-04-16
发明人： Imre ROZSUMBERSZKI , Zsuzsanna KARDOS , Irén HORTOBÁGYI , Tibor SZABÓ , Csaba VÁRADI , Tamás BÁN
摘要： The present invention relates to a process for the preparation of iloprost of formula I through new intermediates, isolation of iloprost of formula I in solid form, as well as preparation of the 16(S)-iloprost and 16(R)-iloprost isomers of formulae (S)-I and (R)-I and isolation of iloprost of formula I and 16(S)-iloprost of formula (S)-I in solid, crystalline form.
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