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公开(公告)号：WO2019086292A1
公开(公告)日：2019-05-09
申请号：PCT/EP2018/078964
申请日：2018-10-23
Applicant: PROCOS S.P.A.
Inventor： MORANA, Fabio , GOBBATO, Stefano , COZZI, Lucia , ROLETTO, Jacopo , PAISSONI, Paolo
IPC: C07D403/06 , A61K31/506 , A61P35/00
Abstract: PROCESS FOR THE PREPARATION OF THE CRYSTALLINE FORM III OF TIPIRACIL HYDROCHLORIDE The present invention concerns a process for the preparation of the crystalline form III of Tipiracil hydrochloride having a content of residual solvents lower than the ICH limits. Said process is advantageous with respect to the known processes because it allows the production of the form III of Tipiracil hydrochloride suitable for use in the preparation of pharmaceutical finished products.
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公开(公告)号：WO2020075082A1
公开(公告)日：2020-04-16
申请号：PCT/IB2019/058593
申请日：2019-10-09
Applicant: PROCOS S.P.A.
Inventor： MORANA, Fabio , GRANDE, Vincenzo , GOBBATO, Stefano , ROLETTO, Jacopo , PAISSONI, Paolo
IPC: C07C273/18 , C07C275/16
Abstract: The invention relates to a process for the synthesis of carglumic acid from L-glutamic acid and sodium cyanate by treatment with a lithium compound in an aqueous medium. The process according to the invention is easily industrially scalable, and is faster and cheaper than the known procedures. Formula (I)
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Patent Agency Ranking
公开(公告)号：WO2019166901A1
公开(公告)日：2019-09-06
申请号：PCT/IB2019/051155
申请日：2019-02-13
Applicant: PROCOS S.P.A.
Inventor： MORANA, Fabio , GOBBATO, Stefano , ROLETTO, Jacopo , PAISSONI, Paolo
IPC: C07D239/46 , C07D239/22
Abstract: The invention relates to a process for the synthesis of 6-chloromethyluracil (6-(chloromethyl)pyrimidin-2,4(1 H ,3 H )-dione) from ethyl 4-chloroacetoacetate and S- methylisothiourea hemisulfate via isolation of the novel intermediate 6- (chloromethyl)-6-hydroxy-2-(methylthio)-5,6-dihydropyrimidin-4(1 H )-one, and its subsequent treatment with aqueous sulfuric acid. Formula (I).
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公开(公告)号：WO2017021378A1
公开(公告)日：2017-02-09
申请号：PCT/EP2016/068347
申请日：2016-08-01
Applicant: PROCOS S.P.A.
Inventor： BETTONI, Piergiorgio , GOBBATO, Stefano , VERONESE, Martino , ROLETTO, Jacopo , PAISSONI, Paolo
IPC: C07D207/24 , C07D207/16
CPC classification number: C07D207/24 , C07D207/16
Abstract: Disclosed is a process for the synthesis of N-protected 4-keto-prolines (1), starting with the corresponding protected 4-hydroxyproline, in the presence of the oxidising system P 2 O 5 /dimethylsulphoxide (DMSO). Said process can also be applied in the presence of a chiral centre in the position bearing carboxylic acid (the 3 position) without significant epimerisation of said centre. Said process is particularly advantageous from the environmental standpoint and in terms of yields, productivity and the purity of the product obtained, since it does not use chromium-based oxidants, metals such as ruthenium, or oxidising systems which are precursors of genotoxic impurities.
Abstract translation: 公开了在氧化体系P2O5 /二甲基亚砜（DMSO）存在下合成N-保护的4-酮基 - 脯氨酸（1）的方法，起始于相应的保护的4-羟基脯氨酸。 所述方法也可以在携带羧酸（3位）的位置存在手性中心的情况下使用，而不会使所述中心显着差向异构化。 所述方法从环境观点和所得产物的产率，生产率和纯度方面都是特别有利的，因为它不使用铬基氧化剂，诸如钌的金属或作为遗传毒性杂质的前体的氧化体系。
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公开(公告)号：EP3759082A1
公开(公告)日：2021-01-06
申请号：EP19709566.4
申请日：2019-02-13
Applicant: Procos S.p.A.
Inventor： MORANA, Fabio , GOBBATO, Stefano , ROLETTO, Jacopo , PAISSONI, Paolo
IPC: C07D239/46 , C07D239/22
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公开(公告)号：EP3864004A1
公开(公告)日：2021-08-18
申请号：EP19795055.3
申请日：2019-10-09
Applicant: Procos S.p.A.
Inventor： MORANA, Fabio , GRANDE, Vincenzo , GOBBATO, Stefano , ROLETTO, Jacopo , PAISSONI, Paolo
IPC: C07C273/18 , C07C275/16
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公开(公告)号：EP3704109A1
公开(公告)日：2020-09-09
申请号：EP18795409.4
申请日：2018-10-23
Applicant: Procos S.p.A.
Inventor： MORANA, Fabio , GOBBATO, Stefano , COZZI, Lucia , ROLETTO, Jacopo , PAISSONI, Paolo
IPC: C07D403/06 , A61K31/506 , A61P35/00
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