An Improved and Efficient Process for the Preparation of Tofacitinib Citrate
Yogesh S. Patil, Nilesh L. Bonde, Ankush S. Kekan, D. G. Sathe, Arijit Das · Organic Process Research & Development · 2014
The present invention is related to a simple and efficient process for the preparation of tofacitinib citrate 1, a Pfizer molecule approved for the treatment of rheumatoid arthritis. The process relies upon an improved process for the preparation of a key intermediate (3 R,4 R )-(1-benzyl-4-methylpiperidin-3-yl)methylamine as tartarate salt 3 and its simple and impurity-free conversion to tofacitinib citrate 1 . The current invention is aimed at addressing process development issues related to quality and yields. The disclosed process is capable of delivering much higher yield compared to the prior state-of-the-art process and is able to yield very highly pure compound.