JD5037 (1) is a potent and selective, peripherally acting inverse agonist of the cannabinoid (CB R) receptor. Peripheral CB receptor antagonists/inverse agonists have great potential in the treatment of metabolic disorders like type 2 diabetes, obesity, and nonalcoholic steatohepatitis. We report the synthesis of octadeuterated [ H ]-JD5037 (S, S) (8) along with its (S, R) diastereomer (13) from commercially available L-valine-d starting material. The [ H ]-JD5037 compound will be used to quantitate unlabeled JD5037 during clinical ADME studies and will be used as an LC-MS/MS bioanalytical standard.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5568925PMC
http://dx.doi.org/10.1002/jlcr.3521DOI Listing

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