Efficient preparation of (R)‐2‐(2,5‐difluorophenyl)pyrrolidine via a recycle process of resolution

Efficient preparation of (R)‐2‐(2,5‐difluorophenyl)pyrrolidine via a recycle process of resolution

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. Meanwhile, the undesired (S)‐1 could be racemiz...

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Veröffentlicht in:Chirality (New York, N.Y.) N.Y.), 2021-12, Vol.33 (12), p.931-937
Hauptverfasser: Lv, Xunlei, Chen, Liang, Pan, Jing, Meng, Xue, Bi, Siju, Liu, Weiyuan, Zhou, Ting, Lin, Kuaile, Ye, Deyong, Zhou, Weicheng
Format: Artikel
Sprache:eng
Schlagworte:
(R)‐2‐(2,5‐difluorophenyl)pyrrolidine
Larotrectinib
Malic acid
Potassium
Potassium hydroxide
Potassium hydroxides
Pyrrolidine
Racemization
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Zusammenfassung: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. Meanwhile, the undesired (S)‐1 could be racemized in the presence of potassium hydroxide in DMSO. After three times of recycle process, the desired freebase (R)‐1 was obtained in a yield of 61.7% with excellent ee (98.4%).
ISSN:0899-0042
1520-636X
DOI:10.1002/chir.23366