Details

Autor(en) / Beteiligte

• Tran, Scott B.
• Maxwell, Brad D.
• Burrell, Richard
• Bonacorsi Jr, Samuel J.

Titel

The syntheses of isotopically labelled CB-1 antagonists for the treatment of obesity

Ist Teil von

• Journal of labelled compounds & radiopharmaceuticals, 2016-12, Vol.59 (14), p.665-672

Ort / Verlag

England: Blackwell Publishing Ltd

Erscheinungsjahr

2016

Quelle

Wiley-Blackwell Journals

Beschreibungen/Notizen

• BMS‐725519, BMS‐811064, and BMS‐812204 are potent and selective central cannabinoid receptor antagonists that have been investigated for the treatment of human obesity. To further understand their biotransformation profiles, radiolabelled and stable‐labelled products were required. This paper describes the utility of [14C]1,1‐carbonyldiimidazole as a radiolabelling reagent for the syntheses of carbonyl‐labelled [14C]BMS‐725519, [14C]BMS‐811064, and [14C]BMS‐812204. The syntheses of stable‐labelled [13C6]BMS‐725519 and [13CD313CD2]BMS‐812204 synthesized from of [13C6]4‐chloroacetophenone and [13CD313CD2]iodoethane, respectively, are also described. BMS‐725519, BMS‐811064 and BMS‐812204 are potent and selective central cannabinoid receptor antagonists that have been investigated for the treatment of human obesity. To further understand their biotransformation profiles, radiolabelled and stable‐labelled products were required. This paper describes the utility of [14C]1,1‐carbonyldiimidazole as a radiolabelling reagent for the syntheses of carbonyl‐labelled [14C]BMS‐725519, [14C]BMS‐811064 and [14C]BMS‐812204. The syntheses of stable‐labelled [13C6]BMS‐725519 and [13CD313CD2]BMS‐812204 synthesized from of [13C6]4‐chloroacetophenone and [13CD313CD2]iodoethane, respectively, are also described.