摘要:
A process comprising (i) providing a mixture comprising a compound of formula (I) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof; (ii)subjecting the mixture provided in (i) to fluorinating conditions in the presence of a fluorination agent selected from the group consisting of diethylamino (difluoro) sulfonium tetrafluoroborate and difluoro(morpholino) sulfonium tetrafluoroborate obtaining a mixture comprising a compound of formula (II) or isomers, stereoisomers diastereomers, enantiomers or salts thereof; (iii) optionally subjecting the mixture obtained in (ii) to deprotection conditions, obtaining a mixture comprising the compound of formula (III) or isomers, stereoisomers, diastereomers, enantiomers or salts thereof.
摘要:
The present invention relates to a solid composition comprising amorphous sofosbuvir and amorphous daclatasvir and to a process for the preparation of the solid composition. The pre- sent invention further relates to a pharmaceutically acceptable composition comprising the solid composition. Yet further, the present invention relates the use of the solid composition and the pharmaceutically acceptable composition comprising the solid composition for use in the treatment of hepatitis C.
摘要:
The present invention relates to a process for producing a sterile solution containing a cellulose ether derivative, comprising the steps of i) providing a non-sterile solution containing a cellulose ether derivative, ii) sterile filtrating the solution of step i), and iii) removing the solvent under reduced pressure.
摘要:
A process for preparing a compound of formula (I) or a salt thereof, the process comprising providing a compound of formula (III) wherein PG is an inert electron withdrawing hydroxyl protecting group, reacting the compound of formula (III) with a fluorinating agent, obtaining a compound of formula (II) and deprotecting the compound of formula (II).
摘要:
An improved process for preparing Carfilzomib of Formula 13 is provided, as well as novel compounds that can be used as intermediates in the process for preparing Carfilzomib.
摘要:
The invention relates to synthetic routes for preparing telaprevir and boceprevir, and its intermediates as well as peptides other than telaprevir. The synthetic routes are based on a Mukaiyama aldol addition reaction of a silyl enol ether or an enolate with an imine. The invention also refers to novel intermediates for preparing telaprevir/boceprevir or other peptides.
摘要:
The invention relates to a process for the preparation of telaprevir, or a pharmaceutically acceptable salt or solvate thereof, wherein the process requires a smaller number of process steps and/or does not require the use of toxic and instable compounds compared to the known processes. Another embodiment refers to telaprevir, or a pharmaceutically acceptable salt or solvate thereof as well as to intermediate products for preparation of the same, wherein the afore-mentioned products are obtained by the process described herein.
摘要:
The present invention is directed to a compound of formula (III), its preparation and to its use for the preparation of a compound of formula (IV). The present invention hence is directed to a process for the preparation of compound of formula (III) and for the preparation of a compound of formula (IV) from a compound of formula (III) via reduction of the compound of formula (III). The present invention is further directed to intermediate compounds for preparing the compound of formula (III) and hence compound of formula (IV).