Synthetic approaches to site selective deuterium incorporation in a novel CRTh2 receptor antagonist clinical candidate.
Selection of acidic or basic reaction conditions, combined with appropriate temperatures, allowed for site selective direct incorporation of deuterium at multiple positions in the 7-azaindole-3-acetic acid CRTh2 receptor antagonist clinical candidate NVP-QAV680.
Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, RH12 5AB, UK.
David A
DA
Sandham
Christopher J
CJ
Page
D060326:Chemistry Techniques, Synthetic; D003903:Deuterium / Q000737:chemistry*; D006801:Humans; D006868:Hydrolysis; D007212:Indolizines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*
D007212:Indolizines; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C588117:NVP-QAV680; D003903:Deuterium; C036293:prostaglandin D2 receptor
CRTh2 antagonist; D2O; clinical candidate; selective deuteration