Disclosed herein are novel iodonium analogs having anticancer and anti-inflammatory activity.

Disclosed herein are novel iodonium analogs having anticancer and anti-inflammatory activity.

The present disclosure relates to compounds that bind to flavin-containing enzymes and inhibit mitochondrial function, referred to herein as mitoflavoscins. Methods of screening compounds for mitochondrial inhibition and anti-cancer properties are disclosed. Also described are methods of using mitoflavoscins to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitoflavoscins to provide anti-aging benefits. Specific mitoflavoscin compounds are also disclosed.

The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: ##STR00001##
wherein
A is an aryl or heteroaryl, each with or without substitution; and
R.sub.1 is H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), NH-(alkyl), N(alkyl).sub.2, NH-(alkenyl), NH-(alkynyl) NH-(aryl), NH-(heteroaryl), O-(alkyl), O-(alkenyl), O-(alkynyl), O-(aryl), O-(heteroaryl); S-(alkyl), S-(alkenyl), S-(alkynyl), S-(aryl), or S-(heteroaryl), comprising:
(a) reacting a compound having the structure: ##STR00002##
with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: ##STR00003##
and
(b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure: ##STR00004##

The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: ##STR00001##
wherein
A is an aryl or heteroaryl, each with or without substitution; and
R.sub.1 is H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), NH-(alkyl), N(alkyl).sub.2, NH-(alkenyl), NH-(alkynyl) NH-(aryl), NH-(heteroaryl), O-(alkyl), O-(alkenyl), O-(alkynyl), O-(aryl), O-(heteroaryl); S-(alkyl), S-(alkenyl), S-(alkynyl), S-(aryl), or S-(heteroaryl), comprising:
(a) reacting a compound having the structure: ##STR00002##
with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: ##STR00003##
and
(b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure: ##STR00004##

The present invention relates compounds useful as reagents for the diazomethylation reaction, their preparation and the use thereof as reagents in a method for the diazomethylation reaction of aromatic substrates. It relates in particular to a compound of formula (I) wherein E is an electron withdrawing group. ##STR00001##

The present invention relates compounds useful as reagents for the diazomethylation reaction, their preparation and the use thereof as reagents in a method for the diazomethylation reaction of aromatic substrates. It relates in particular to a compound of formula (I) wherein E is an electron withdrawing group. ##STR00001##

Described herein are hypervalent iodine reagents.

Described herein are hypervalent iodine reagents.

The present invention relates compounds useful as reagents for the diazomethylation reaction, their preparation and the use thereof as reagents in a method for the diazomethylation reaction of aromatic substrates. It relates in particular to a compound of formula (I) wherein E is an electron withdrawing group.

##STR00001##