Process Development and Scale Up of a Selective JAK3 Covalent Inhibitor PF-06651600

Author:

Tao YongORCID,McWilliams J. ChristopherORCID,Wiglesworth Kristin E.,Girard Kevin P.,Makowski Teresa M.,Sach Neal W.1,Mustakis Jason G.,Mehta Ruchi,Trujillo John I.,Chen Xiaofeng2,Li Tangqing2,Shi Feng2,Xie Chengfu2,Zhang Qing2

Affiliation:

1. La Jolla Laboratories, Pfizer Worldwide Research and Development, 10770 Science Center Drive, San Diego, California 92121, United States

2. STA Pharmaceutical Co. Ltd., 90 Delin Road, Waigaoqiao, China (Shanghai) Free Trade Zone, Shanghai 200131, China

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Reference13 articles.

1. Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans

2. bBrown, M. F.; Casimiro-Garcia, A.; Che, Y.; Coe, J. W.; Flanagan, M. E.; Gilbert, A. M.; Hayward, M. M.; Langille, J. D.; Montgomery, J. I.; Telliez, J.B.; Thorarensen, A.; Unwalla, R. J. Pyrrolo[2,3-d]pyrimidinyl- pyrrolo[2,3-b]pyrazinyl- and pyrrolo[2,3-d]pyridinylacrylamides as JAK inhibitor and their preparation WO 2015083028.

3. Pfizer Receives Breakthrough Therapy Designation from FDA for PF-06651600, an oral JAK3 Inhibitor, for the Treatment of Patients with Alopecia Areata. https://www.businesswire.com/news/home/20180905005542/en/Pfizer-Receives-Breakthrough-Therapy-Designation-FDA-PF-06651600. Accessed on April 28, 2019.

4. Asymmetric Hydrogenation of Six-Membered Monocyclic N-Heteroaromatic Compounds

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