| 摘要 |
<p>21AbstractMETHOD FOR PREPARING COMBRETASTATINThe invention relates to a method for preparing a combretastatin (A) in the form of a base or of an addition salt with an acid, which comprises coupling, in the presence of a base and of T3P, the salt of the (Z)-amino compound of formula (I) with a doubly protected L-serine derivative of formula (II) in which PG denotes a group protecting the amine function, so as to obtain the compound of formula (Z)-(Ib): then deprotecting and opening the ring of (Z)-(lb) in the presence of an acid, so as to obtain the combretastatin (A) in the form of a salt; and, optionally, adding a base, so as to obtain the combretastatin (A) in the form of a base, the salt of the (Z)-amino compound having been obtained by enrichment of the salt of the amino compound of formula (II) in (Z) isomer.</p> |
