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The Sonogashira coupling reaction of polymer‐supported propargylamine (=prop‐2‐yn‐1‐amine) with aryl iodides in the presence of the [Pd(PPh3)2]Cl2/CuI catalyst system produces 3‐arylprop‐1‐yn‐1‐amines smoothly at room temperature (Scheme). When propargylamine is attached on Wang resin through a carbamate linker, the common problems with amino functionality in palladium‐catalyzed couplings are overcome...
Three angiotensin II receptor antagonists—losartan, candesartan, and zolarsartan—were investigated. All the compounds, which are structural analogues, are metabolized via conjugation to glucuronic acid. Interestingly, both O- and N-glucuronidation take place, so that regioisomers are formed. One ether O-glucuronide, two acyl O-glucuronides, and five tetrazole-N-glucuronides were biosynthesized, in...
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