SYNTHESIS OF ETOPOSIDE LACTAM VIA A MITSUNOBU REACTION SEQUENCE
A novel chemical sequence for the conversion of a lactone antitumor agent 1 (etoposide) to the corresponding lactam 2 is described.The key steps involve a Mitsunobu cyclization (Ph3P, DEAD) of the γ-hydroxymethyl acyl benzaldehyde hydrazone 6 to a lactam derivative 7 followed by reductive cleavage (Ra-Ni) to lactam 2.
Kadow, J. F.,Vyas, D. M.,Doyle, T. W.
p. 3299 - 3302
(2007/10/02)
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