Abstract

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

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