1039738-27-6Relevant articles and documents
Synthesis method of tofacitinib citrate diastereomer impurities
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Paragraph 0032; 0035-0036; 0049; 0052-0053, (2021/10/27)
The invention discloses a synthesis method of tofacitinib citrate diastereomer impurities, relates to the technical field of drug organic synthesis, and relates to 3 - amino -4 - methylpyridine as a starting material and a quaternary ammonium salt. Raw materials of the whole synthetic route are easily available, the reaction conditions are mild, the post-treatment separation and purification operation is simple and feasible, and the preparation method is good in repeatability.
Preparation method of tofacitinib intermediate
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, (2017/10/13)
The invention discloses a preparation method of a tofacitinib intermediate compound-1-benzyl-3-methyl amino-4-methyl piperidine dihydrochloride. The method comprises the following steps: (1) carrying out selective deprotection on a compound as shown in a structural formula (V) to synthesize a compound-1-benzyl-3-amino-4-methyl piperidine as shown in a structural formula (VI); (2) enabling the compound as shown in the structural formula (VI) to have a primary amine monomethylation reaction to generate the target compound-1-benzyl-3-methyl amino-4-methyl piperidine dihydrochloride as shown in a structural formula (I). The method has the characteristics of being easy in obtaining of raw materials, novel in route, less in by-products, simple and convenient to operate, high in yield, and the like.