1443623-92-4Relevant articles and documents
Efficient preparation of (R)-2-(2,5-difluorophenyl)pyrrolidine via a recycle process of resolution
Lv, Xunlei,Chen, Liang,Pan, Jing,Meng, Xue,Bi, Siju,Liu, Weiyuan,Zhou, Ting,Lin, Kuaile,Ye, Deyong,Zhou, Weicheng
, p. 931 - 937 (2021/10/19)
An efficient preparation of (R)-2-(2,5-difluorophenyl)pyrrolidine ((R)-1) from the racemate based on a recycle process of resolution/racemization was described. In the process, the desired (R)-1 was obtained by resolution with D-malic acid in 95% EtOH. Me
Preparation method for intermediate of Larotrectinib
-
Paragraph 0025; 0028; 0029, (2020/07/15)
The invention discloses a preparation method for an intermediate of Larotrectinib, belonging to the field of drug synthesis. The preparation method comprises the following steps: with 4-chloro-1-(2,5-difluorophenyl)butane-1-one (I) as a raw material, carrying out a delbin reaction on the 4-chloro-1-(2,5-difluorophenyl)butane-1-one (I) so as to obtain 4-amino-1-(2,5-difluorophenyl)butane-1-one hydrochloride (II), and carrying out intramolecular cyclization under an alkaline condition so as to obtain 5-(2,5-difluorophenyl)-3,4-dihydro-2H-pyrrole (III). The preparation method provided by the invention is mild in reaction conditions, simple to operate and applicable to industrial production.
Synthesis method of larotrectinib intermediate
-
Paragraph 0018; 0025-0028; 0031-0032, (2020/07/21)
The invention discloses a synthesis method of a larotrectinib intermediate, and belongs to the field of drug synthesis. The method uses 4-chloro-1-(2, 5-difluorophenyl)butane-1-one (I) as the raw material to synthesize 5-(2, 5-difluorophenyl)-3, 4-dihydro-2H-pyrrole (III) through ammonolysis and ring closing one-pot method. The invention provides the synthesis method of the larotrectinib intermediate. The method is controllable in reaction process, easy to operate and high in yield.