Patent classifications
C07C233/25
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.7, —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.7, —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.7, —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##
2,2' -DIAMINOBIARYLS HAVING ONE PRIMARY AND ONE SECONDARY AMINE
Novel 2,2′-diaminobiaryls having one primary and one secondary amine and an electrochemical process for preparation thereof.
2,2' -DIAMINOBIARYLS HAVING ONE PRIMARY AND ONE SECONDARY AMINE
Novel 2,2′-diaminobiaryls having one primary and one secondary amine and an electrochemical process for preparation thereof.
COMPOSITIONS AND METHODS FOR TREATMENT OF PROSTATE CARCINOMA
Disclosed herein are 1,4-naphthoquinone analogs, pharmaceutical compositions that include one or more of such 1,4-naphthoquinone analogs, and methods of treating and/or ameliorating diseases and/or conditions associated with a cancer, such as prostate cancer with such 1,4-naphthoquinone analogs. Also included are combination therapies wherein a 1,4-naphthoquinone analog disclosed herein, and a hormone therapy agent are provided to a subject suffering from a condition such as cancer.
COMPOSITIONS AND METHODS FOR TREATMENT OF PROSTATE CARCINOMA
Disclosed herein are 1,4-naphthoquinone analogs, pharmaceutical compositions that include one or more of such 1,4-naphthoquinone analogs, and methods of treating and/or ameliorating diseases and/or conditions associated with a cancer, such as prostate cancer with such 1,4-naphthoquinone analogs. Also included are combination therapies wherein a 1,4-naphthoquinone analog disclosed herein, and a hormone therapy agent are provided to a subject suffering from a condition such as cancer.
System for crystalizing chemical compounds and methodologies for utilizing the same
A system including a fluid receiver defined by a crystallization chamber, three or more fluid input conduits, wherein each fluid input conduit is configured to direct a fluid into the crystallization chamber such that the fluids from the fluid input conduits converge on a single spatial coordinate (X—Y—Z) within the crystallization chamber, and a fluid outlet body portion. A process for crystallization of the chemical compound is also disclosed. Polymorphs of paracetamol, carbamazapine, ketoprofen, atorvastatin, and itraconazole also are disclosed.
System for crystalizing chemical compounds and methodologies for utilizing the same
A system including a fluid receiver defined by a crystallization chamber, three or more fluid input conduits, wherein each fluid input conduit is configured to direct a fluid into the crystallization chamber such that the fluids from the fluid input conduits converge on a single spatial coordinate (X—Y—Z) within the crystallization chamber, and a fluid outlet body portion. A process for crystallization of the chemical compound is also disclosed. Polymorphs of paracetamol, carbamazapine, ketoprofen, atorvastatin, and itraconazole also are disclosed.
System for crystalizing chemical compounds and methodologies for utilizing the same
A system including a fluid receiver defined by a crystallization chamber, three or more fluid input conduits, wherein each fluid input conduit is configured to direct a fluid into the crystallization chamber such that the fluids from the fluid input conduits converge on a single spatial coordinate (X—Y—Z) within the crystallization chamber, and a fluid outlet body portion. A process for crystallization of the chemical compound is also disclosed. Polymorphs of paracetamol, carbamazapine, ketoprofen, atorvastatin, and itraconazole also are disclosed.