We report herein the asymmetric coupling of flow-generated unstabilized diazo compounds and propargylated amine derivatives, using a new pyridinebis(imidazoline) ligand, a copper catalyst and base. The reaction proceeds rapidly, generating chiral allenes in 10-20 minutes with high enantioselectivity (89-98 % de/ee), moderate yields and a wide functional group tolerance.

Clonidine, like many other imidazoline drugs, is usually thought of as a selective α2-adrenergic agonist and is approved for use as a centrally acting antihypertensive agent. In addition, clonidine is prescribed off-label to treat some cases of Tourette’s syndrome, and it may also have a role in the treatment of other psychiatric conditions, including obsessive–compulsive disorders, panic state...

Two decades of investigations have failed to unequivocally clarify the functions and the molecular nature of imidazoline-2 receptors (I2R). However, there is robust pharmacological evidence for the functional modulation of monoamino oxidase (MAO) and other important enzyme activities by I2 site ligands. Some compounds of this class proved to be active experimental tools in preventing both exper...

Canavanine is a guanidinium derivative that has the basic structure of a ligand for the imidazoline receptor (I-R). Furthermore, canavanine is found in an herb that has been shown to improve diabetic disorders. Thus, the present study was designed to investigate the anti-hyperglycemic action of canavanine in rats with streptozotocin (STZ)-induced type 1-like diabetes. Canavanine decreased hyper...

Dowex-50W-hyodrgen ion exchange resin was used as a reusable catalyst for the synthesis of oxazoline, imidazoline and thiazoline derivatives through condensation reaction between arylnitriles and 2-aminoalcohol, ethylenediamine or 2-aminoethanthiol. This process provides several advantages such as excellent yields of the products, simple operation, convenient separation and inexpensive and recy...