TY - JOUR
T1 - Tofacitinib synthesis – An asymmetric challenge
AU - Carvalho, Luísa C. R.
AU - Lourenço, Ana
AU - Ferreira, Luísa Maria
AU - Branco, Paula Sério
N1 - info:eu-repo/grantAgreement/FCT/5876/147218/PT#
co-financed by the ERDF under the PT2020 Partnership Agreement (POCI-01-0145-FEDER-007265).
The authors would like to thank Hovione FarmaCiencia SA for financial support.
PY - 2019
Y1 - 2019
N2 - Tofacitinib is a Janus activated kinase (JAK) inhibitor approved for the treatment of rheumatoid arthritis and active psoriatic arthritis. Its synthesis normally involves long synthetic sequences due to the chirality associated to the piperidine ring. This review is a comprehensive analysis of the different synthetic methods used to prepare this active pharmaceutical ingredient (API), covering the related journal and patent literature.
AB - Tofacitinib is a Janus activated kinase (JAK) inhibitor approved for the treatment of rheumatoid arthritis and active psoriatic arthritis. Its synthesis normally involves long synthetic sequences due to the chirality associated to the piperidine ring. This review is a comprehensive analysis of the different synthetic methods used to prepare this active pharmaceutical ingredient (API), covering the related journal and patent literature.
KW - Asymmetric synthesis
KW - Chiral resolution
KW - Nitrogen heterocycles
KW - Piperidine rings
KW - Tofacitinib
UR - http://www.scopus.com/inward/record.url?scp=85057631075&partnerID=8YFLogxK
U2 - 10.1002/ejoc.201801180
DO - 10.1002/ejoc.201801180
M3 - Review article
AN - SCOPUS:85057631075
VL - 2019
SP - 615
EP - 624
JO - European Journal of Organic Chemistry
JF - European Journal of Organic Chemistry
SN - 1434-193X
IS - 4
ER -