Efficient stereoselective syntheses of 5- and 6-[2,3]-dihydrobenzofuran bet
a-amino acids are described. These 3-aryl beta-amino acids are aspartic aci
d mimetics that are structurally related to known benzodioxole systems. In
many cases, the benzodioxole can inhibit and induce cytochrome P-450; neith
er of these dihydrobenzofuran beta-amino esters is a potent inhibitor of se
veral human P-450 enzymes. (C) 2000 Elsevier Science Ltd. All rights reserv
ed.