| 12423172 |
Andrus MB, Mettath SN, Song C: A modified synthesis of iodoazidoaryl prazosin. . J Org Chem. 2002 Nov 15;67(23):8284-6.
The antihypertension agent iodoazidoaryl prazosin (IAAP) has been made using a convergent route involving addition of an acylated piperazine 7 to 2-chloroquinazoline 5. IAAP has been shown to function as a multidrug resistance (MDR) reversal agent and bind to P-glycoprotein, a transmembrane transport protein. A study is also reported involving palladium-catalyzed substitution with amine heterocycles. With N,N-bis (2,6-diisopropyl) dihydroimidazolium chloride (10) as the ligand (2 mol %) for palladium (II) acetate (2 mol %) in THF at room temperature, morpholine added to 5 in 81% yield. |
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