An asymmetric synthesis of 7-deoxypancratistatin 1 has been accomplish
ed starting from diol 2 via two pathways in overall yields of 2.6 and
3.0%, respectively. The key step involved the regioselective ring open
ing of tosylaziridine 3 or the new carbomethoxyaziridine 15 with a hig
her-order cuprate and the cyclization of urethane 11.