Solid-phase synthesis of naltrindole derivatives using Fischer indole synthesis based on one-pot release and cyclization methodology.
[reaction: see text] We describe a new approach for the solid-phase synthesis of indoles 1 that involves a one-pot release and cyclization reaction of a solid-supported hydrazone through a Wang-type linker. Using this solid-phase methodology, we accomplished the synthesis of 40 naltrindole derivatives.
Tanaka
Hiroshi
H
Department of Applied Chemistry, Tokyo Institute of Technology, Meguro, Tokyo 152-8552, Japan.
Ohno
Hiroshi
H
Kawamura
Kuniaki
K
Ohtake
Atsushi
A
Nagase
Hiroshi
H
Takahashi
Takashi
T
D020650:Combinatorial Chemistry Techniques; D003500:Cyclization; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry
D009271:Naltrexone; C055382:naltrindole