公开(公告)号：US11028057B2

公开(公告)日：2021-06-08

申请号：US16975800

申请日：2019-02-13

Applicant: Procos S.P.A.

Inventor： Fabio Morana ,  Stefano Gobbato ,  Jacopo Roletto ,  Paolo Paissoni

IPC: C07D239/54

Abstract: The invention relates to a process for the synthesis of 6-chloromethyluracil (6-(chloromethyl)pyrimidin-2,4(1H,3H)-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(1H)-one, and its subsequent treatment with aqueous sulfuric acid. Formula (I).

公开(公告)号：US11344550B2

公开(公告)日：2022-05-31

申请号：US16760685

申请日：2018-10-23

Applicant: Procos S.P.A.

Inventor： Fabio Morana ,  Stefano Gobbato ,  Lucia Cozzi ,  Jacopo Roletto ,  Paolo Paissoni

IPC: C07D403/06 ,  A61K31/513

Abstract: 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.

公开(公告)号：US20200330465A1

公开(公告)日：2020-10-22

申请号：US16760685

申请日：2018-10-23

Applicant: Procos S.P.A.

Inventor： Fabio Morana ,  Stefano Gobbato ,  Lucia Cozzi ,  Jacopo Roletto ,  Paolo Paissoni

IPC: A61K31/513

Abstract: 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.