Identification of a novel and orally available benzimidazole derivative as an NPY Y5 receptor antagonist with in vivo efficacy

Synthetic Methods for Compounds Having CF3–S Units on Carbon by Trifluoromethylation, Trifluoromethylthiolation, Triflylation, and Related Reactions

“…Triflyl substituted anilines are useful building blocks for the synthesis of various heteroaryl triflones (Scheme ). Triflyl substituted benzimidazole derivatives were readily prepared from 4-triflylbenzene-1,2-diamine (eq a and b, Scheme ). − The cyclocondensation reaction of 4-triflylaniline and malonate gave 4-hydroxy-3-phenyl-6-triflylquinolin-2­(1 H )-one in 71% yield (eq c, Scheme ). , …”

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

“…Compound 486 appeared to be the most promising agent ( Tamura et al, 2012a ). In another study by the same research group ( Tamura et al, 2012b ), compound 487 was reported to show high NPY Y5 receptor binding affinity along with good absorption, distribution, metabolism and elimination (ADME) profile resulting in notable in vivo efficacy as NPY Y5 receptor antagonist.…”

Synthesis of morpholino nucleosides starting from enantiopure glycidol

“…Beyond the interest in the oligonucleotide field, 2,6-substituted morpholines are widely embedded in compounds with a range of biological activities. 10 For example, this class of heterocycles has found wide application in peptide synthesis, 11 and has been used as HIV protease inhibitors, 12 antimicrobial agents, 13 or therapeutics in obesity and diabetes, 14 tumors, 15 sexual dysfunction, 16 and pain experience. 17 Therefore, various synthetic strategies have been reported in the literature to access the 2,6-substituted morpholine skeleton.…”