1204176-45-3

Upstream product

• 3430-27-1 3-amino-4-methylpyridine 
• 694495-63-1 O-methyl-N-(4-methylpyridin-3-yl)carbamate 

Downstream Products

• 1616833-40-9 1-triryI-N,4-dimethylpiperidin-3-amine 
• 1616761-04-6 (3S,4S)-1-trityl-N,4-dimethylpiperidin-3-amine di-p-toluyl-L-tartaric acid salt 
• 1616760-93-0 (3R,4R)-1-trityl-N,4-dimethylpiperidin-3-amine 
• 1616760-94-1 C₃₉H₃₈ClN₅O₂S 
• 1616760-95-2 C₂₀H₂₄ClN₅O₂S 
• 1616760-96-3 C₃₂H₃₂ClN₅ 
• 1616760-97-4 N-((3R,4R)-4-methyl-piperidin-3-yl)-N-methyl-2-chloro-7H-pyrrolo[2,3-D]pyrimidine-4-amine 
• 477600-74-1 tert-butyl (3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidine-1-carboxylate 
• 1259404-17-5 tasocitinib 
• 540737-29-9 Tofacitinib citrate 
• 540737-29-9 tofacitinib hemi-citrate 
• 1354621-59-2 cis-N-benzyl-3-methoxycarbonylamino-4-methylpiperidine 
• 1228879-37-5 cis-N-benzyl-3-methoxycarbonylamino-4-methylpiperidine bis(hydrochloride) 
• 1616760-91-8 methyl-(1-trityl-4-methylpiperidin-3-yl)carbamate 

Relevant academic research and scientific papers

Synthesis method of tofacitinib intermediate

The invention provides a synthesis method of a tofacitinib intermediate. According to synthesis of cis-(4-methylpiperidine-3-yl) methyl carbamate, (4-methylpiperidine-3-yl) methyl carbamate is taken as an initial raw material, samarium iodide is taken as a hydrogenation agent, and water is taken as a hydrogen source to generate the cis-(4-methylpiperidine-3-yl) methyl carbamate. The method provided by the invention has the advantages of few byproducts, simple operation, high product yield and purity, and small amount of three wastes, and has excellent economic and environmental benefits.

Synthesis method for tofacitinib

The invention relates to a synthesis method for tofacitinib serving as a JAK inhibitor. According to the method, the tofacitinib is prepared by taking (4-picoline-3-yl)methyl carbamate as a raw material, and performing catalytic hydrogenation, benzyl protection, reduction, salification, separation, deprotection and amidation salification. The method specifically comprises the following steps: (1) performing catalytic hydrogenation and reduction on (4-picoline-3-yl)methyl carbamate in sulfuric acid and Pd/C; (2) reacting cis-(4-picoline-3-yl)methyl carbamate and benzyl chloride to obtain cis-(1-benzyl-4-methylpiperidine-3-yl)methyl carbamate; (3) performing HOBT catalytic condensation on N-[(3R,4R)-4-methylpiperidine-3-yl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidine-4-amine and cyanoacetic acid to obtain tofacitinib free alkali. The preparation method provided by the invention has easily obtained raw materials, mild reaction conditions, easiness and convenience in operation and high yield, and is suitable for industrial production.

THE PRESENT INVENTION RELATES TO PROCESS FOR THE PREPARATION OF TOFACITINIB AND INTERMEDIATES THEREOF.

The present invention relates to process for the preparation of tofacitinib and intermediates thereof.

Investigation of practical routes for the kilogram-scale production of cis-3-methylamino-4-methylpiperidines

Two routes for the synthesis of cis-N-protected-3-methylamino-4- methylpiperidine (3) were examined: a route hinging on the electrochemical oxidation of carbamate 1 to install a ketone at the 3 position of the piperidine followed by reductive animation (disconnection A), and a route involving the hydrogenation of an appropriately functionalized pyridine (disconnection B). While both routes to the desired compound were ultimately successful, the pyridine hydrogenation approach proved to be more amenable to kilogram-scale preparations due to the crystallinity and purity of intermediates in that route.

3-Amino-piperadine derivatives and methods of manufacture

This invention relates to 3-amino piperadine derivatives, their intermediates and methods of manufacture. As such, the present invention includes methods of making a compound of the formulas (Ia) and (Ib) wherein R1, R2, R3/sub