1217630-38-0Relevant 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
METHODS FOR PREPARING TYROSINE RECEPTOR KINASE INHIBITORS
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Paragraph 00460; 00463, (2021/10/22)
The present disclosure relates to pyrazolo[1,5-α]pyrimidine compounds useful as TRK inhibitors and compounds useful in preparing pyrazolo[1,5-α]pyrimidine compounds, and methods of making and using same. This abstract is intended as a scanning tool for pu
Synthesis method of (R)-2-(2, 5-difluorophenyl) pyrrolidine
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Paragraph 0089-0091, (2021/04/10)
The invention belongs to the technical field of chemical pharmacy, and relates to a synthetic method of (R)-2-(2, 5-difluorophenyl)pyrrolidine. The synthesis method comprises the following steps: (1) carrying out dehydration condensation reaction on a compound as shown in a formula 1 and a chiral induction reagent (R) tert-butylsulfinamide to obtain a compound as shown in a formula 2; (2) carrying out addition reaction on the compound in the formula 2 and a Grignard reagent to obtain a compound in a formula 3; (3) carrying out a reduction/cyclization reaction on the compound shown in the formula 3, trifluoroacetic acid and triethylsilane to obtain a compound shown in a formula 4; (4) splitting the compound shown in the formula 4 by (D)-malic acid to obtain the (R)-2-(2, 5-difluorophenyl) pyrrolidine*D malate compound with EE being greater than 98% shown in the formula 5; and (5) dissociating the compound in the formula 5 with a sodium hydroxide solution to obtain (R)-2-(2, 5-difluorophenyl) pyrrolidine. By utilizing the synthetic method of (R)-2-(2,5-difluorophenyl)pyrrolidine, the cost is low, the optical purity is high, the subsequent separation process is simplified, the raw materials are easy to obtain, the process conditions are mild, and the synthetic method is suitable for synthesizing (R)-2-(2, 5-difluorophenyl) pyrrolidine in large-scale production.