O. Stanciuc et At. Balaban, REACTION OF PYRYLIUM-SALTS WITH NUCLEOPHILES .23. TRIARYLETHENE DERIVATIVES CONTAINING AN OXYALKYLENEAMINO OR OXYALKYLENE-N-PYRIDINIUM SIDE-CHAIN, Journal of pharmaceutical sciences, 82(9), 1993, pp. 927-933
A synthetic design was devised for preparing primary amines related to
anticancer drugs clomiphene and tamoxifen on the basis of key interme
diates with a phenolic group, to which a side chain (omega-aminoethoxy
or omega-aminopropoxy) was attached. These compounds were then reacte
d with 2,4,6-trimethyl- or 2,4,6-triphenylpyrylium salts.1 This afford
ed pyridinium analogues of clomiphene and tamoxifen as potential thera
peutic agents for treatment against hormone-dependent tumors.