1334412-55-3Relevant articles and documents
A 1 - R1 - 3, 3 - difluoro (or 3 - fluoro) - 4 - R2 - 4 - aminomethyl piperidine and its derivatives
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Paragraph 0101; 0102; 0103; 0104; 0105; 0106; 0107, (2017/02/17)
The invention relates to a preparation method for 1-R1-3,3-difluoro(or3-fluoro)-4-R2-4-aminomethylpiperidine shown as a formula (1-A) and a formula (1-B) and derivatives thereof. In the formulas, R1 is hydrogen, C1-C9 alkyl, aryl, benzyl, CF3CO, R5CO or R6OCO; R5 is C1-C9 alkyl, aryl or benzyl; R6 is C1-C9 alkyl, aryl or benzyl; R2 is C1-C9 alkyl, aryl or benzyl; R3 is hydrogen, C1-C9 alkyl, aryl, benzyl, CF3CO, R5CO or R6OCO; R4 is hydrogen, C1-C9 alkyl, aryl, benzyl, CF3CO, R5CO or R6OCO; and the above optional groups are not substituted or substituted by a group consisting of one or more selected from alkyl, haloalkyl, hydroxyalkyl, halogen, alkyloxy or hydroxyl. The preparation method is novel, raw materials and reagents are cheap, the reaction conditions are mild, the operation is easy and simple, and generated 1-R1-3,3-difluoro(or3-fluoro)-4-R2-4-aminomethylpiperidine and the derivatives thereof can be used as important intermediates of new drug research and development.