2. Academic Validation
  3. Synthesis of S-2-((S)-3-(4-chlorophenyl)-N'-((4-chlorophenyl)sulfonyl)-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboximidamido)-3-(methyl-d3 )butanamide-d5 , octadeuterated JD5037

Synthesis of S-2-((S)-3-(4-chlorophenyl)-N'-((4-chlorophenyl)sulfonyl)-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboximidamido)-3-(methyl-d3 )butanamide-d5 , octadeuterated JD5037

  • J Labelled Comp Radiopharm. 2017 Aug;60(10):460-465. doi: 10.1002/jlcr.3521.
Malliga R Iyer 1,  Resat Cinar 1,  Nathan J Coffey 1,  Robert J Chorvat 2,  George Kunos 1
Affiliations

Affiliations

  • 1 Laboratory of Physiologic Studies, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Rockville, MD, USA.
  • 2 Jenrin Discovery LLC, Chadds Ford, PA, USA.
PMID: 28545167 DOI: 10.1002/jlcr.3521
Abstract

JD5037 (1) is a potent and selective, peripherally acting inverse agonist of the cannabinoid (CB1 R) receptor. Peripheral CB1 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 [2 H8 ]-JD5037 (S, S) (8) along with its (S, R) diastereomer (13) from commercially available L-valine-d8 starting material. The [2 H8 ]-JD5037 compound will be used to quantitate unlabeled JD5037 during clinical ADME studies and will be used as an LC-MS/MS bioanalytical standard.

Keywords

ADME; CB1R; EC; PSA.

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