C07C259/10

TRIFLUOROMETHOXYLATION OF ARENES VIA INTRAMOLECULAR TRIFLUOROMETHOXY GROUP MIGRATION

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 subsutitution; 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##

TRIFLUOROMETHOXYLATION OF ARENES VIA INTRAMOLECULAR TRIFLUOROMETHOXY GROUP MIGRATION

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 subsutitution; 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##

18-20 MEMBER BI-POLYCYCLIC COMPOUNDS

The invention relates to 18-20 member bi-polycyclic compounds, methods of making these compounds, and methods of using them in treating hyperproliferative disorders (e.g., cancer) and non-malignant tumors; promoting muscle formation; inhibiting muscle degeneration or the loss of muscle mass or muscle function; and myofibers ex vivo.

18-20 MEMBER BI-POLYCYCLIC COMPOUNDS

The invention relates to 18-20 member bi-polycyclic compounds, methods of making these compounds, and methods of using them in treating hyperproliferative disorders (e.g., cancer) and non-malignant tumors; promoting muscle formation; inhibiting muscle degeneration or the loss of muscle mass or muscle function; and myofibers ex vivo.

Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration

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 subsutitution; 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##

Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration

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 subsutitution; 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##

N-hydroxybenzamides as HDAC inhibitors for the treatment of parasitic diseases

Compounds of formula ##STR00001##
wherein n is 0, 1 or 2; X is ##STR00002##
and Ar is a benzyl substituted at the meta position by a C.sub.1 to C.sub.8 alkoxy group, or a pharmaceutically acceptable salt thereof, for treating, preventing or inhibiting a parasitic disease, such as toxoplasmosis, in a subject are provided. Methods for preparing the compounds are also presented.

N-hydroxybenzamides as HDAC inhibitors for the treatment of parasitic diseases

Compounds of formula ##STR00001##
wherein n is 0, 1 or 2; X is ##STR00002##
and Ar is a benzyl substituted at the meta position by a C.sub.1 to C.sub.8 alkoxy group, or a pharmaceutically acceptable salt thereof, for treating, preventing or inhibiting a parasitic disease, such as toxoplasmosis, in a subject are provided. Methods for preparing the compounds are also presented.

AMINOXY ACID-BASED ANTIBACTERIAL COMPOUNDS AND METHODS THEREOF
20240315992 · 2024-09-26 ·

The subject invention pertains to novel compounds, compositions containing the novel compounds, and methods for targeting gram-positive bacteria with the compounds or compositions of the subject invention. The subject invention further pertains to novel compounds, novel compositions, and methods for targeting gram-positive bacteria persister cells and gram-positive bacterial biofilms. The subject compounds and compositions can target gram-positive bacteria by modulating the proton motive force, calcium influx, autolysis, or any combination thereof. The novel compounds are synthetic, small molecules that can induce the death of gram-positive bacteria.

AMINOXY ACID-BASED ANTIBACTERIAL COMPOUNDS AND METHODS THEREOF
20240315992 · 2024-09-26 ·

The subject invention pertains to novel compounds, compositions containing the novel compounds, and methods for targeting gram-positive bacteria with the compounds or compositions of the subject invention. The subject invention further pertains to novel compounds, novel compositions, and methods for targeting gram-positive bacteria persister cells and gram-positive bacterial biofilms. The subject compounds and compositions can target gram-positive bacteria by modulating the proton motive force, calcium influx, autolysis, or any combination thereof. The novel compounds are synthetic, small molecules that can induce the death of gram-positive bacteria.