Patent classifications
C07C231/12
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##
Synthesis intermediates for obtaining derivatives of sphingosines, ceramides and sphingomyelins with good yields
The subject matter of the present invention is the novel molecules of formulae E, E′ and F. These molecules prove to be synthesis intermediates that are very advantageous for the manufacture of derivatives of sphingosine or of ceramides functionalized in position 1, with good yields, in which R.sub.1 and R.sub.2 are fatty chains, R.sub.3 is an alkyl group and R.sub.4 is a protective group for alcohol functions. Another subject of the invention is the use of the intermediates of type F for converting same into intermediates of type G, by means of reduction in the presence of lithium borohydride. The G molecules are precursors that are known to make it possible to obtain sphingolipids or sphingomyelin.
Synthesis intermediates for obtaining derivatives of sphingosines, ceramides and sphingomyelins with good yields
The subject matter of the present invention is the novel molecules of formulae E, E′ and F. These molecules prove to be synthesis intermediates that are very advantageous for the manufacture of derivatives of sphingosine or of ceramides functionalized in position 1, with good yields, in which R.sub.1 and R.sub.2 are fatty chains, R.sub.3 is an alkyl group and R.sub.4 is a protective group for alcohol functions. Another subject of the invention is the use of the intermediates of type F for converting same into intermediates of type G, by means of reduction in the presence of lithium borohydride. The G molecules are precursors that are known to make it possible to obtain sphingolipids or sphingomyelin.
Method for preparing lacosamide
The present invention provides a novel method for preparing lacosamide with high chiral purity from D-serine. The method of the present invention can obtain lacosamide with high chiral purity in a high yield through a simple and environmentally-friendly process and thus can be easily applied to mass production.
Method for preparing lacosamide
The present invention provides a novel method for preparing lacosamide with high chiral purity from D-serine. The method of the present invention can obtain lacosamide with high chiral purity in a high yield through a simple and environmentally-friendly process and thus can be easily applied to mass production.
Method for preparing lacosamide
The present invention provides a novel method for preparing lacosamide with high chiral purity from D-serine. The method of the present invention can obtain lacosamide with high chiral purity in a high yield through a simple and environmentally-friendly process and thus can be easily applied to mass production.
Reagents and methods for esterification
Methods and reagents for esterification of biological molecules including proteins, polypeptides and peptides. Diazo compounds of formula I: ##STR00001##
where R is hydrogen, an alkyl, an alkenyl or an alkynyl, R.sub.A represents 1-5 substituents on the indicated phenyl ring and R.sub.M is an organic group, which includes a label, a cell penetrating group, a cell targeting group, or a reactive group or latent reactive group for reaction to bond to a label, a cell penetrating group, or a cell targeting group, among other organic groups are useful for esterification of biological molecules. Also provided are diazo compounds which are bifunctional and trifunctional coupling reagents as well as reagents for the synthesis of compounds of formula I.
Reagents and methods for esterification
Methods and reagents for esterification of biological molecules including proteins, polypeptides and peptides. Diazo compounds of formula I: ##STR00001##
where R is hydrogen, an alkyl, an alkenyl or an alkynyl, R.sub.A represents 1-5 substituents on the indicated phenyl ring and R.sub.M is an organic group, which includes a label, a cell penetrating group, a cell targeting group, or a reactive group or latent reactive group for reaction to bond to a label, a cell penetrating group, or a cell targeting group, among other organic groups are useful for esterification of biological molecules. Also provided are diazo compounds which are bifunctional and trifunctional coupling reagents as well as reagents for the synthesis of compounds of formula I.
Reagents and methods for esterification
Methods and reagents for esterification of biological molecules including proteins, polypeptides and peptides. Diazo compounds of formula I: ##STR00001##
where R is hydrogen, an alkyl, an alkenyl or an alkynyl, R.sub.A represents 1-5 substituents on the indicated phenyl ring and R.sub.M is an organic group, which includes a label, a cell penetrating group, a cell targeting group, or a reactive group or latent reactive group for reaction to bond to a label, a cell penetrating group, or a cell targeting group, among other organic groups are useful for esterification of biological molecules. Also provided are diazo compounds which are bifunctional and trifunctional coupling reagents as well as reagents for the synthesis of compounds of formula I.
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.