Welcome to Hodoodo Chemicals

Ruxolitinib

CAT#: H201512

CAS#: 941678-49-5

Description: Ruxolitinib, also known as INC424 and INCB18424 or INCB018424, is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.

Synthetic Routes

Ruxolitinib - Synthetic Route 1

Synthetic reference

Lin, Qiyan; Meloni, David; Pan, Yongchun; Xia, Michael; Rodgers, James; Shepard, Stacey; Li, Mei; Galya, Laurine; Metcalf, Brian; Yue, Tai-Yuen; Liu, Pingli; Zhou, Jiacheng. Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction. Jiacheng. Organic Letters. Volume 11. Issue 9. Pages 1999-2002. Journal. (2009).

Ruxolitinib - Synthetic Route 2

Synthetic reference

Anon. Processes for preparing (S-(3R)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile. IP.com Journal. Volume 13. Issue 1B. Pages 10. Journal; Patent. (2013).

Ruxolitinib - Synthetic Route 3

Synthetic reference

Haydl, Alexander M.; Xu, Kun; Breit, Bernhard. Regio- and Enantioselective Synthesis of N-Substituted Pyrazoles by Rhodium-Catalyzed Asymmetric Addition to Allenes. Angewandte Chemie, International Edition. Volume 54. Issue 24. Pages 7149-7153. Journal; Online Computer File. (2015).

Ruxolitinib - Synthetic Route 4

Synthetic reference

: Cao, Biao; Zhu, Hanghang; Wu, Jianzhong; Tian, Guanghui. Intermediate of JAK inhibitor and preparation method thereof. Assignee Suzhou Vigonvita Life Sciences Co., Ltd., Peop. Rep. China. CN 107759623. (2018).

Ruxolitinib - Synthetic Route 5

Synthetic reference

: Zhang, Xiquan; Zhang, Aiming; Zhou, Zhou; Yang, Leilei; Yao, Huadong; Zhu, Xueyan; Wang, Hubo. Process for synthesis of ruxolitinib. Assignee Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Peop. Rep. China. WO 2017114461. (2017).

Ruxolitinib - Synthetic Route 6

Synthetic reference

Hamdy, Ahmed; Rothbaum, Wayne; Izumi, Raquel; Lannutti, Brian; Covey, Todd; Ulrich, Roger; Johnson, Dave; Barf, Tjeerd; Kaptein, Allard. Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor, a JAK-2 inhibitor, a PD-1 inhibitor and/or a PD-L1 inhibitor. Assignee Acerta Pharma B.V., Neth. WO 2016024228. (2016).

Ruxolitinib - Synthetic Route 7

Synthetic reference

Albrecht, Wolfgang; Selig, Roland. Process of preparing oxalate salt of ruxolitinib. Assignee Ratiopharm GmbH, Germany. WO 2016026974. (2016).

Ruxolitinib - Synthetic Route 8

Synthetic reference

: Zhou, Jiacheng; Liu, Pingli; Lin, Qiyan; Metcalf, Brian W.; Meloni, David; Pan, Yongchun; Xia, Michael; Li, Mei; Yue, Tai-Yuen; Rodgers, James D.; Wang, Haisheng. Processes for preparing JAKs inhibitors and related intermediate compounds. Assignee Incyte Corporation, USA. WO 2010083283. (2010).