Patent classifications
C07C217/40
Preparation method for tedizolid, tedizolid intermediate, and preparation method therefor
The present invention relates to a preparation method for a tedizolid compound in Formula I. In Formula I, R is selected from hydrogen, formula A, formula B, benzyl or benzyl substituted by a substituent, the substituent is selected from a group consisting of halogen, nitryl, C.sub.1-C.sub.6 alkyl, and C.sub.1-C.sub.6 alkoxy, and R.sub.1 is C.sub.1-C.sub.6 alkyl or C.sub.1-C.sub.6 alkyl substituted by halogen. The method comprises: generating a compound having a structure as shown in Formula C and a compound having a structure as shown in Formula D by a coupled reaction under the catalysis of a metal catalyst, a substituent of R being defined as above, where X is a leaving group, the leaving group comprising chlorine, bromine, iodine, and sulfonyl oxy such as trifluoromethane sulfonic oxy, methylsulfonyl oxy and benzenesulfonyl oxy, or benzenesulfonyl oxy substituted by one or more substituents, the substituent being selected from a group consisting of halogen, C.sub.1-C.sub.6 alkyl, and C.sub.1-C.sub.6 alkoxy. ##STR00001##
Cationic polyglyceryl compositions and compounds
Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DP.sub.OH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.
Cationic polyglyceryl compositions and compounds
Provided are polyglyceryl compositions comprising one or more polyglyceryl compounds having: (a) a node structure comprising at least three contiguous glyceryl remnant units; (b) one or more cationic groups each linked to the node structure by an independently selected linking group; and (c) one or more hydrophobic moieties each independently (i) linked to the node structure by a linking group, or (ii) constituting a portion of one of the one or more cationic groups, wherein the composition has an average degree of polymerization determined by hydroxyl value testing (DP.sub.OH) of from about 3 to about 20. Also provided are polyglyceryl compounds which may compose such compositions, and uses of the polyglyceryl compositions and compounds.
LIPID COMPOUNDS AND LIPID NANOPARTICLE COMPOSITIONS
Provided herein are lipid compounds that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination. Also provided herein are lipid nanoparticle compositions comprising said lipid compounds.
LIPID COMPOUNDS AND LIPID NANOPARTICLE COMPOSITIONS
Provided herein are lipid compounds that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination. Also provided herein are lipid nanoparticle compositions comprising said lipid compounds.
DENDRIMER AND FORMULATIONS THEREOF
The present invention relates to a novel dendrimer. The present invention also relates to formulations comprising the dendrimer with improved characteristics. For instance, the present invention relates to formulations comprising pesticides such as 2-(2,4-dichlorophenoxy)acetic acid with improved characteristics such as reduced crystallisation, compatibility with hard water and an extended shelf life at low temperatures.
DENDRIMER AND FORMULATIONS THEREOF
The present invention relates to a novel dendrimer. The present invention also relates to formulations comprising the dendrimer with improved characteristics. For instance, the present invention relates to formulations comprising pesticides such as 2-(2,4-dichlorophenoxy)acetic acid with improved characteristics such as reduced crystallisation, compatibility with hard water and an extended shelf life at low temperatures.
AMINE-FUNCTIONAL MONOMERS AND METHODS OF MAKING SAME
Disclosed herein are addition-polymerizable monomer composition including an amine-derivatized alpha-methyl styrene (ADAMS) monomer according to structure (I) and/or an aminated conjugated aliphatic methylated polyene (ACAMP) monomer according to structure (II):
##STR00001##
with k, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 defined herein. Difunctional monomers of these types with two polymerizable loci and/or two amine loci are also disclosed herein. Further disclosed herein are methods for making such compositions.
AMINE-FUNCTIONAL MONOMERS AND METHODS OF MAKING SAME
Disclosed herein are addition-polymerizable monomer composition including an amine-derivatized alpha-methyl styrene (ADAMS) monomer according to structure (I) and/or an aminated conjugated aliphatic methylated polyene (ACAMP) monomer according to structure (II):
##STR00001##
with k, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 defined herein. Difunctional monomers of these types with two polymerizable loci and/or two amine loci are also disclosed herein. Further disclosed herein are methods for making such compositions.
PREPARATION METHOD FOR TEDIZOLID, TEDIZOLID INTERMEDICATE, AND PREPARATION METHOD THEREFOR
The present invention relates to a preparation method for a tedizolid compound in Formula I. In Formula I, R is selected from hydrogen, formula A, formula B, benzyl or benzyl substituted by a substituent, the substituent is selected from a group consisting of halogen, nitryl, C.sub.1-C.sub.6 alkyl, and C.sub.1-C.sub.6 alkoxy, and R.sub.1 is C.sub.1-C.sub.6 alkyl or C.sub.1-C.sub.6 alkyl substituted by halogen. The method comprises: generating a compound having a structure as shown in Formula C and a compound having a structure as shown in Formula D by a coupled reaction under the catalysis of a metal catalyst, a substituent of R being defined as above, where X is a leaving group, the leaving group comprising chlorine, bromine, iodine, and sulfonyl oxy such as trifluoromethane sulfonic oxy, methylsulfonyl oxy and benzenesulfonyl oxy, or benzenesulfonyl oxy substituted by one or more substituents, the substituent being selected from a group consisting of halogen, C.sub.1-C.sub.6 alkyl, and C.sub.1-C.sub.6 alkoxy.
##STR00001##