One-Pot Synthesis of Novel 3,5-Disubstituted-1,2,4-oxadiazoles from Indazole Carboxylic Acid Esters and Amidoximes

Abstract

Oxadiazoles are important class of heterocycles due to their biological importance and are stable to physiological environment. 1,2,4-Oxadiazoles have often been used as bioisosteres of esters and amides 1 and are found in several drugs and drug leads 2 which includes potent sphingosine-1phosphate-1 (S1P1) agonist (I) 3 , the metabotropic glutamate subtype 5 (mGlu5) receptor (II) 4 and muscarinic receptor (III) 5 for the treatment of Alzheimer's diseases. They can also be found in a number of biologically important molecules, such as serotoninergic (5-HT 3) antagonists (IV) 6 , benzodiazepine receptor agonists (V) 7 and dopamine ligands (VI) 8. Several papers reported the use of 1,2,4-oxadiazole in a number of

Ferrocene modified analogues of imatinib and nilotinib as potent anti-cancer agents

“…38 We were able to overcome these problems by using Fe dust and aqueous NH 4 Cl in boiling ethanol media. 39 This cheap, environmentally friendly and easy to perform reaction afforded N-(3-amino-4methylphenyl)benzamide 7 quantitatively without purification. The latter was transformed into its guanidinium salt 8 in 96% yield following the already described procedure.…”