886503-15-7Relevant articles and documents
Racemization method of larotinib intermediate
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Paragraph 0050; 0068-0069; 0071-0072; 0074-0075; 0077-0078, (2021/03/11)
The invention discloses a racemization method of a larotinib intermediate, which comprises the following steps: in a solvent, heating (2S)-2-(2, 5-difluorophenyl)pyrrolidine(compound I, S-type I) or aracemic mixture mainly comprising S-type I, and convert
Method for preparing larotrectinib intermediate through one-pot method
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, (2020/07/15)
The invention discloses a method for preparing a larotrectinib intermediate through a one-pot method. The preparation method is characterized by comprising the following steps: 1) dissolving a compound VI serving as a raw material in a solvent, adding isopropyl magnesium chloride to generate a Grignard reagent, and reacting with N-Boc-pyrrolidone to obtain a compound I; 2) adding an acid into thereaction solution, and carrying out a Boc removal reaction on the compound I to obtain a compound II; 3) adding an alkali into the reaction solution, and carrying out a ring closing reaction on the compound II to obtain a compound III; 4) carrying out reduction on the compound III in the reaction solution to obtain a compound IV; and 5) carrying out salification on the compound IV and D-malic acid, and re-crystallizing to obtain a compound V.
Stereocomplementary Synthesis of Pharmaceutically Relevant Chiral 2-Aryl-Substituted Pyrrolidines Using Imine Reductases
Chen, Fei-Fei,Chen, Qi,Li, Bo-Bo,Xu, Jian-He,Zhang, Yu-Hui,Zheng, Gao-Wei,Zhou, Xin-Yi
, p. 3367 - 3372 (2020/04/21)
Exploring a collection of naturally occurring imine reductases (IREDs) identified two stereocomplementary IREDs with reducing activity toward sterically hindered 2-aryl-substituted pyrrolines. Using (R)-selective ScIR and (S)-selective SvIR, various chiral 2-aryl-substituted pyrrolidines with excellent enantioselectivity (>99% ee) were stereocomplementarily synthesized in good yield (60-80%), demonstrating the feasibility of IREDs for generating pharmaceutically relevant chiral 2-aryl-substituted pyrrolidine intermediates.