C07H5/02

PROCESS FOR PRODUCING FLUORINATED COMPOUNDS USING ALCOHOL SOLVENT HAVING CARBONYL GROUP
20190202820 · 2019-07-04 ·

The present invention relates to a process for producing an organic fluoro compound containing [.sup.18F]fluorine. The method of the present invention for producing the organic fluoro compound is not only advantageous for producing the organic fluoro compound with high yield by using the solvent represented by formula 1 for nucleophilic fluorination reaction but also suitable for automatic synthesis of .sup.18F-labeled radiopharmaceuticals due to the excellent solubility of the precursor compound in the solvent.

Sugar Derivatives and Uses Thereof to Prepare Novel Senolytic Agents
20240182506 · 2024-06-06 ·

Provided herein are novel sugar derivatives which are intermediates for preparing senolytic agents that selectively kill senescent cells associated with numerous pathologies and discases. including age-related pathologies and discases.

Sucrose ester based cationic gene vector and preparation method thereof

The invention provides a class of sucrose ester based cationic lipids and preparation method thereof. The vector prepared using the cationic lipid can be used to deliver nucleic acid. The sucrose ester based cationic lipid is prepared by using a chemical synthesis method in the invention, wherein the synthesis method is simple, and has a relatively high product yield. A composition, including suspension, emulsion, micelle and liposome and the like, can be prepared by mixing the sucrose ester based cationic lipid compound of the invention with a co-lipid. Sucrose ester based cationic lipid complex can be prepared by using the said composition and nucleic acid, which has advantages such as simple preparation, low toxicity and high transfection efficiency, and is a novel and highly efficient gene vector.

Sucrose ester based cationic gene vector and preparation method thereof

The invention provides a class of sucrose ester based cationic lipids and preparation method thereof. The vector prepared using the cationic lipid can be used to deliver nucleic acid. The sucrose ester based cationic lipid is prepared by using a chemical synthesis method in the invention, wherein the synthesis method is simple, and has a relatively high product yield. A composition, including suspension, emulsion, micelle and liposome and the like, can be prepared by mixing the sucrose ester based cationic lipid compound of the invention with a co-lipid. Sucrose ester based cationic lipid complex can be prepared by using the said composition and nucleic acid, which has advantages such as simple preparation, low toxicity and high transfection efficiency, and is a novel and highly efficient gene vector.

Chlorination of sucrose-6-esters

There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1 and 6 positions thereof; (v) quenching said mixture to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises perfluorooctane.

Chlorination of sucrose-6-esters

There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1 and 6 positions thereof; (v) quenching said mixture to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises perfluorooctane.

METHOD FOR PRODUCING ALPHA-HALO-TETRAACYL-GLUCOSE

There is provided an efficient and excellent preparation method of an -halo-tetraacyl-glucose which is suitable for industrial preparation, which comprises reacting D-glucose or lower alkyl D-glucoside with a reactive derivative of a carboxylic acid and a metal halide to prepare the -halo-tetraacyl-glucose represented by the formula (III):

##STR00001## wherein R represents an optionally substituted lower alkyl group or an optionally substituted aryl group, and X represents a halogen atom,
in one step, and the resulting -halo-tetraacyl-glucose (III) can be converted into a compound of the formula (I) or a salt thereof by subjecting to a conventional method.

METHOD FOR PRODUCING ALPHA-HALO-TETRAACYL-GLUCOSE

There is provided an efficient and excellent preparation method of an -halo-tetraacyl-glucose which is suitable for industrial preparation, which comprises reacting D-glucose or lower alkyl D-glucoside with a reactive derivative of a carboxylic acid and a metal halide to prepare the -halo-tetraacyl-glucose represented by the formula (III):

##STR00001## wherein R represents an optionally substituted lower alkyl group or an optionally substituted aryl group, and X represents a halogen atom,
in one step, and the resulting -halo-tetraacyl-glucose (III) can be converted into a compound of the formula (I) or a salt thereof by subjecting to a conventional method.

DMF distillation

A method of obtaining purified DMF from a mixture comprising DMF and hydrogen chloride (HCl) involving distillation is provided.

Chlorination of sucrose-6-esters

There is provided a method for the chlorination of a sucrose-6-acylate to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate, wherein said method comprises the following steps (i) to (v): (i) providing a first component comprising sucrose-6-acylate; (ii) providing a second component comprising a chlorinating agent; (iii) combining said first component and said second component to afford a mixture; (iv) heating said mixture for a heating period in order to provide chlorination of sucrose-6-acylate at the 4, 1 and 6 positions thereof; (v) quenching said mixture to produce a 4,1,6-trichloro-4,1,6-trideoxy-galactosucrose-6-acylate; wherein at least one of said first component and said second component comprises a reaction vehicle, and said reaction vehicle comprises a tertiary amide; and wherein said mixture comprises a cosolvent during a least a portion of the heating period of step (iv), wherein said cosolvent comprises dimethylacetamide (DMAc).