Patent classifications
C07C273/1854
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##
BENZAMIDE DERIVATIVE
The present invention relates to a benzamide derivative of general formula I, a drug composition containing same and a use thereof as a drug, wherein the definitions of R.sub.1, Z and Q are as described in the description.
##STR00001##
Gemini surfactant and their use
Disclosed herein are gemini surfactants, and methods for making and using these gemini surfactants. These gemini surfactants may be incorporated in paints and coatings to provide hydrophilic and/or self-cleaning properties.
Gemini surfactant and their use
Disclosed herein are gemini surfactants, and methods for making and using these gemini surfactants. These gemini surfactants may be incorporated in paints and coatings to provide hydrophilic and/or self-cleaning properties.
Enantiomerically pure binaphthol derivatives and method for preparing the same
The present invention relates to compounds 1, 1a (S-enantiomer) and 1b (R-enantiomer) of the following formula 1, and a method for preparing the same. [formula 1] The novel compound of the formula 1 is used as an important intermediate for preparing compounds 6, 6a (S-enantiomer) and 6b (R-enantiomer) of the following formula 6, which are 2,2-binaphthol-3-aldehyde derivatives. Also, the present invention provides a method for preparing the compound of formula 1 with a very safe method at low cost. [formula 6]
6-amino-5,6,7,8-tetrahydronaphthalen-2-yl or 3-aminochroman-7-yl derivatives
The present invention relates to compounds TAAR receptor antagonists of formula I wherein X, R, L, Ar and R.sup.1 are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric disorders with compounds of formula I. ##STR00001##
COMPOUNDS USEFUL IN PREVENTION AND/OR TREATMENT OF SENESCENT CELL-RELATED PATHOLOGIES AND DISEASES
A compound of formula (I) or pharmaceutically acceptable salts or hydrates thereof:
##STR00001## wherein R is chosen from phenyl, a 6-membered heteroaryl group, cyclohexyl, a 5-membered heteroaryl group; a bicyclo [3.1.0] hexanyl group; a C.sub.2-C.sub.5 alkynyl group; and a cubanyl group; wherein R1 and R2, independently, are chosen from H; C.sub.1-C.sub.6 alkyl (optionally substituted with one or more halogens); C.sub.1-C.sub.6 alkyl-S(O).sub.n; CO.sub.2H (or C.sub.1-C.sub.6 alkyl esters thereof or C.sub.1-C.sub.6 alkyl amides thereof); halogen; C.sub.1-C.sub.6 alkoxy; CN; NO.sub.2; and NR.sub.7R.sub.8; wherein R.sub.7 and R.sub.8, independently, each represent H, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 alkylcarbonyl, C.sub.1-C.sub.6 alkoxycarbonyl, arylsulphonyl, heteroarylsulphonyl, heterocyclosulphonyl, arylcarbonyl, heteroarylcarbonyl, heterocyclocarbonyl, or C.sub.1-C.sub.6 alkylsulphonyl, or R.sub.7, R.sub.8 and the nitrogen to which they are attached form a 5 or 6 membered heterocyclic ring (such as morpholine or piperidine); and wherein n represents 0-2.
Crosslinking component for binder resins
This invention relates to a crosslinking component for binder resins which is especially suitable to be used together with epoxy-group containing binders and/or (poly)isocyanates such as blocked (poly)isocyanates and which comprises at least two blocked isocyanate groups per molecule of the crosslinking component whereby at least one of the at least two blocked isocyanate groups is a group according to structural unit (I), wherein the ratio of structural units of formula (II), if present, to structural units of formula (I) is 0.40 or below. The cross-linking component may also be self-cross-linkable. The present invention further relates to a coating composition, e.g. a one-component coating composition comprising the crosslinking component and a method of its manufacture.
COMPOUNDS AND METHOD OF USE THEREOF FOR TREATING BACTERIAL DISEASES
The present disclosure provides compounds that can inhibit the type III secretion system (TTSS) to decrease the pathogenesis of gram-negative bacteria. These compounds may have wide applications for treating bacteria diseases caused by gram-negative bacteria in a host species, including but not limited to, plants and animals. The present invention further relates to compositions that inhibit pathogenesis of gram-negative bacteria without killing the bacteria. Methods relating to preventing and/or treating infection of a host species by bacterial pathogens are also provided herein.