Efficient method for the preparation of tofacitinib citrate

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United States of America Patent

PATENT NO 9828380
APP PUB NO 20160297825A1
SERIAL NO

15092651

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Abstract

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Disclosed is a novel process for the synthesis of tofacitinib citrate on an industrial scale with high yields and purity starting with cis-(1-benzyl-4-methyl-piperidin-3-yl)methylamine bis-hydrochloride racemate (intermediate VIII), which comprises:

    1. Condensation between intermediates VII and VIII to give intermediate VI2. Hydrogenation of intermediate VI to give intermediate V3. Resolution of intermediate V to give intermediate IV with enantiomeric purity >99%4. Release of intermediate IV in a basic medium to give intermediate III5. N-acylation reaction of intermediate III to give II (tofacitinib)6. Salification of intermediate II to give tofacitinib monocitrate (I)

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Patent Owner(s)

Patent OwnerAddress
OLON S P A20090 RODANO (MI)

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Bonanomi, Jacopo Rodano, IT 9 5
Defiore, Stella Rodano, IT 2 5
Novo, Barbara Rodano, IT 12 5

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