Patent classifications
C07D319/12
Process for preparing glycolide
According to the present invention a process is provided for producing glycolide which comprises contacting glycolaldehyde dimer with an oxidizing agent to produce a glycolide product. Preferably, the process is carried out in an aprotic environment, such as in a reaction mixture comprising the glycolaldehyde dimer, the oxidizing agent, the glycolide product and an aprotic solvent.
Process for preparing glycolide
According to the present invention a process is provided for producing glycolide which comprises contacting glycolaldehyde dimer with an oxidizing agent to produce a glycolide product. Preferably, the process is carried out in an aprotic environment, such as in a reaction mixture comprising the glycolaldehyde dimer, the oxidizing agent, the glycolide product and an aprotic solvent.
SSAO inhibitors and use thereof
The application relates to a compound of Formula (I′) or (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.
SSAO inhibitors and use thereof
The application relates to a compound of Formula (I′) or (I): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of Formula (I′) or (I), and a method of treating or preventing a disease in which SSAO plays a role.
METHODS FOR SYNTHESIZING N-(PHENYLSULFONYL)BENZAMIDE COMPOUNDS AND INTERMEDIATES THEREOF
Disclosed is a method for synthesizing N-(phenylsulfonyl)benzamide compound and intermediate thereof. The method comprises a method for synthesizing a compound 1, comprising conducting a Buchwald-Hartwig coupling reaction as shown below with compound A and compound B in a solvent and in the presence of a base and a palladium catalyst to obtain the compound 1; wherein R is C.sub.1-C.sub.8 alkyl. The present disclosure synthesizes three intermediate compounds required by the target compound and their preparation methods for the first time. Using the method disclosed in the present disclosure to synthesize the target compound 3 has the advantages of high yield, good purity, easy-to-obtain reaction raw materials, suitable for industrial production.
##STR00001##
METHODS FOR SYNTHESIZING N-(PHENYLSULFONYL)BENZAMIDE COMPOUNDS AND INTERMEDIATES THEREOF
Disclosed is a method for synthesizing N-(phenylsulfonyl)benzamide compound and intermediate thereof. The method comprises a method for synthesizing a compound 1, comprising conducting a Buchwald-Hartwig coupling reaction as shown below with compound A and compound B in a solvent and in the presence of a base and a palladium catalyst to obtain the compound 1; wherein R is C.sub.1-C.sub.8 alkyl. The present disclosure synthesizes three intermediate compounds required by the target compound and their preparation methods for the first time. Using the method disclosed in the present disclosure to synthesize the target compound 3 has the advantages of high yield, good purity, easy-to-obtain reaction raw materials, suitable for industrial production.
##STR00001##
Production of meso-lactide, D-lactide, and L-lactide by back biting of polylactide
Process for increasingly producing D-Lactide and meso lactide by depolymerizing by back biting polylactide (PLA) said process which comprises: (i) Depolymerizing polylactide into its corresponding dimeric cyclic esters by heating the polylactide in the presence of a catalyst system comprising a catalyst and a co-catalyst in a reaction zone at temperature and pressure at which the polylactide is molten; (ii) Forming a vapor product stream from the reaction zone; (iii) Removing the vapor product stream and optionally condense it; (iv) Recovering, either together or separately meso-lactide, D-lactide and L-lactide.
Production of meso-lactide, D-lactide, and L-lactide by back biting of polylactide
Process for increasingly producing D-Lactide and meso lactide by depolymerizing by back biting polylactide (PLA) said process which comprises: (i) Depolymerizing polylactide into its corresponding dimeric cyclic esters by heating the polylactide in the presence of a catalyst system comprising a catalyst and a co-catalyst in a reaction zone at temperature and pressure at which the polylactide is molten; (ii) Forming a vapor product stream from the reaction zone; (iii) Removing the vapor product stream and optionally condense it; (iv) Recovering, either together or separately meso-lactide, D-lactide and L-lactide.
LIPIDS FOR DELIVERY OF NUCLEIC ACID SEGMENTS
Disclosed herein are compounds of Formula (I), Formula (III) or Formula (IIIa), or pharmaceutically acceptable salts thereof, wherein A, L, X.sup.1, X.sup.2, a, b, R.sup.1 and R.sup.2 are as defined herein. Also disclosed are lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a plurality of lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof and a nucleic acid segment; as well as methods for delivering a nucleic acid segment comprising administering a plurality of lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof, and a nucleic acid segment.
LIPIDS FOR DELIVERY OF NUCLEIC ACID SEGMENTS
Disclosed herein are compounds of Formula (I), Formula (III) or Formula (IIIa), or pharmaceutically acceptable salts thereof, wherein A, L, X.sup.1, X.sup.2, a, b, R.sup.1 and R.sup.2 are as defined herein. Also disclosed are lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a plurality of lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof and a nucleic acid segment; as well as methods for delivering a nucleic acid segment comprising administering a plurality of lipid nanoparticles comprising a compound of Formula (I), Formula (III) or Formula (IIIa), or a pharmaceutically acceptable salt thereof, and a nucleic acid segment.