Ko143 is a tetracyclic, synthetic analog of the fungal metabolite fumitremorgin C. potent and specific inhibitor membrane-bound efflux transporter ABCG2, it reverses ABCG2-mediated drug resistance in cancer cells. Here, we describe an improved synthesis that relies on highly selective, substrate-controlled reduction imine formed Bischler–Napieralski reaction with amide derived from 6-methoxy-l-...

The first syntheses of 4-methyl-2-t-butyland 2-methyl-4.6-di-t-butyl-indole are described. Rates of diazocoupling at the 3-position of both these compounds together with those for 2-methyland 2-t-butyl-indole are reported for various para-substituted arenediazonium ions in mixed aqueous and some aprotic solvents a t 25". The kinetic behaviour of 2-methylindole is examined in detail and it is sh...

The substituted indole nucleus [indole is the acronym from indigo (the natural dye) and oleum (used for the isolation)] is a structural component of a vast number of biologically active natural and unnatural compounds. The synthesis and functionalization of indoles has been the object of research for over 100 years, and a variety of well-established classical methods are now available, to name ...

The heterocyclic analogs of o-quinodimethane (OQDM, o-xylylene) are of considerable interest both from a theoretical point of view and for their potential in organic synthesis 1 as useful dienes. This has been elegantly demonstrated in the indole series 2 for the synthesis of several naturally occurring and biologically important indole 3 and carbazole 4 alkaloids. However, with the exception o...