C07C219/20

MILD AND EFFICIENT PREPARATION METHOD FOR A-ACYLOXYENAMIDE COMPOUNDS AND USE THEREOF IN SYNTHESIS OF AMIDE AND POLYPEPTIDE
20200299226 · 2020-09-24 ·

Disclosed are a mild and efficient preparation method for an -acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The -acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0 C. to 50 C.; the produced -acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

MILD AND EFFICIENT PREPARATION METHOD FOR A-ACYLOXYENAMIDE COMPOUNDS AND USE THEREOF IN SYNTHESIS OF AMIDE AND POLYPEPTIDE
20200299226 · 2020-09-24 ·

Disclosed are a mild and efficient preparation method for an -acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The -acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0 C. to 50 C.; the produced -acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

MILD AND EFFICIENT PREPARATION METHOD FOR A-ACYLOXYENAMIDE COMPOUNDS AND USE THEREOF IN SYNTHESIS OF AMIDE AND POLYPEPTIDE
20200299226 · 2020-09-24 ·

Disclosed are a mild and efficient preparation method for an -acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The -acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0 C. to 50 C.; the produced -acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

MILD AND EFFICIENT PREPARATION METHOD FOR A-ACYLOXYENAMIDE COMPOUNDS AND USE THEREOF IN SYNTHESIS OF AMIDE AND POLYPEPTIDE
20190210957 · 2019-07-11 ·

Disclosed are a mild and efficient preparation method for an -acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The -acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0 C. to 50 C.; the produced -acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

MILD AND EFFICIENT PREPARATION METHOD FOR A-ACYLOXYENAMIDE COMPOUNDS AND USE THEREOF IN SYNTHESIS OF AMIDE AND POLYPEPTIDE
20190210957 · 2019-07-11 ·

Disclosed are a mild and efficient preparation method for an -acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The -acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0 C. to 50 C.; the produced -acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

MILD AND EFFICIENT PREPARATION METHOD FOR A-ACYLOXYENAMIDE COMPOUNDS AND USE THEREOF IN SYNTHESIS OF AMIDE AND POLYPEPTIDE
20190210957 · 2019-07-11 ·

Disclosed are a mild and efficient preparation method for an -acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The -acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0 C. to 50 C.; the produced -acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.

SOLID FORMS OF (R)-OXYBUTYNIN D-MALATE
20240217918 · 2024-07-04 ·

(R)-Oxybutynin D-malate salts, including crystalline and amorphous forms, are prepared and characterized. Uses of (R)-oxybutynin D-malate for obstructive sleep apnea (OSA) treatment are also disclosed. Solid forms of (R)-oxybutynin L-tartrate are also disclosed.

SOLID FORMS OF (R)-OXYBUTYNIN D-MALATE
20240217918 · 2024-07-04 ·

(R)-Oxybutynin D-malate salts, including crystalline and amorphous forms, are prepared and characterized. Uses of (R)-oxybutynin D-malate for obstructive sleep apnea (OSA) treatment are also disclosed. Solid forms of (R)-oxybutynin L-tartrate are also disclosed.

Compound and Method for Identifying Impurities Included Therein

The present invention relates to a compound including a quaternary ammonium structure having an acrylate group or a methacrylate group and a method for confirming the presence (or lack thereof) or target impurities. The method for confirming impurities can be applied to quality management such as quality control (QC) and is capable of efficiently being carried out in a short time period.

Compound and Method for Identifying Impurities Included Therein

The present invention relates to a compound including a quaternary ammonium structure having an acrylate group or a methacrylate group and a method for confirming the presence (or lack thereof) or target impurities. The method for confirming impurities can be applied to quality management such as quality control (QC) and is capable of efficiently being carried out in a short time period.