Preclinical development of a treatment for systemic lupus erythematosus

  • Erin Murray

Student thesis: Master's Thesis


Janus Kinase 1 (JAK1) inhibitor 1 is being developed between GlaxoSmithKline (GSK) and Galapagos for the treatment of systemic lupus erythematosus (SLE). The medicinal chemistry route to 1 has been scaled up to provide kilogram quantities of 1 for clinical trials. A new sustainable route to 1 is required to fund larger clinical studies and enable commercial manufacture. A new route was identified to prepare 1 using a Suzuki-Miyaura coupling in the final synthetic step. For the new route to be carried out in the pilot plant, it was necessary to develop the final synthetic step to control palladium and impurity levels in order for 1 to be prepared in acceptable quality for clinical use. The new Suzuki-Miyaura coupling has been scaled up using an 45 Kg input of 149 preparing a total of 165 Kg 1 containing
Date of Award15 Nov 2014
Original languageEnglish
Awarding Institution
  • University Of Strathclyde
SponsorsUniversity of Strathclyde

Cite this