910789-32-1

Upstream product

• 479633-63-1 4-chloro-7-[(4-methylphenyl)sulfonyl]-7H-pyrrolo[2,3-d]pyrimidine 
• 74-89-5 methylamine 
• 98-59-9 p-toluenesulfonyl chloride 
• 78727-16-9 4-(methylamino)-7H-pyrrolo<2,3-d>pyrimidine 
• 3680-69-1 4-chloro-1H-pyrrolo[2,3-d]pyrimidine 

Downstream Products

• 1325182-06-6 N-methyl-7-[(4-methylphenyl)sulfonyl]-N-[(3R,4R)-4-methylpiperidin-3-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine 
• 1259404-17-5 tasocitinib 
• 78727-16-9 4-(methylamino)-7H-pyrrolo<2,3-d>pyrimidine 

Relevant academic research and scientific papers

Preparation method of tofacitinib

The invention discloses a preparation method of tofacitinib. The preparation method comprises the following steps: carrying out asymmetric hydrogenation on 3-chloro-4-methylpyridine to prepare a compound III; carrying out a reaction on the compound III and a compound IV to prepare a compound V; and finally, carrying out acylation and de-protection to obtain a final product tofacitinib (I). The preparation method is simple in process route, high in total yield and purity, few in side products and suitable for industrial production.

Preparation method of tofacitinib citrate compound

The invention discloses a preparation method of a tofacitinib citrate compound. According to the preparation method, 3-bromo-4-piperidone (II) and methyl magnesium bromide are subjected to Grignard reaction and dehydration reaction to obtain a compound III; the compound III is subjected to asymmetric hydrogenation to obtain a compound IV; the compound IV is subjected to substitution and acylationreaction to obtain a compound VI; the compound VI is subjected to deprotection and salt formation to prepare tofacitinib citrate (I). The preparation method has the advantages of simple technologicalroute, easiness for operation and high total yield and purity and is suitable for industrial production.

COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Abl, Bcr-Abl, Bmx, BTK, b-RAF, c RAF, CSK, cSRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK1α1, JNK2α2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFRα, PKA, PKCα, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB kinases.