77862-24-9Relevant articles and documents
Preparation method of tofacitinib intermediate cis-1-benzyl-N, 4-dimethylpiperidine-3-amine dihydrochloride
-
Paragraph 0046; 0060-0062, (2021/01/29)
The invention discloses a preparation method of a tofacitinib intermediate cis-1benzyl-N, 4-dimethyl piperidine-3-amine dihydrochloride. The synthetic method comprises the following steps: taking 3-bromo-4-methylpyridine as an initial raw material, performing substitution reaction with amine to obtain a compound III, and performing acetyl or tert-butyloxycarbonyl protection and catalytic hydrogenation on the compound III to obtain a piperidine compound V. The compound V and benzaldehyde are subjected to reductive amination or react with benzyl halide to obtain a compound VI. A protecting groupis removed from the compound VI, and a hydrochloride compound I. 2HCl is formed at the same time. The synthesis method is simple to operate, high in total yield, high in product purity, stable in quality and suitable for industrial production.
Synthesis method for preparing intermediates of tofacitinib
-
Paragraph 0038-0040; 0049-0050; 0058; 0059; 0063; 0064, (2018/11/04)
The invention provides a novel method for synthesizing primary ring cis-4-methyl-3-methylamino-1-benzylpiperidine bis-hydrochloride of tofacitinib. The primary ring cis-4-methyl-3-methylamino-1-benzylpiperidine bis-hydrochloride is made from 3-halogenation-picoline. The novel method includes steps of catalytic Ullman coupling, 3-halogenation-picoline and benzyl halide salifying, hydroboration reagent reduction, salifying and the like to obtain target compounds. The method has the advantages of simple conditions, easily available reagents and operational safety.
A synthetic cis - 1 - benzyl - 3 - methylamino - 4 - methyl - piperidine
-
Paragraph 0031; 0033, (2017/08/25)
The invention relates to a method for synthesizing cis-1-benzyl-3-methylamino-4-methyl-piperidine, in particular to a method for synthesizing cis-1-benzyl-3-methylamino-4-methyl-piperidine by taking 1-benzyl-3-methylamino-4-methyl-piperidine bromide as an