C07B57/00

Processes for the preparation of sofosbuvir and intermediates thereof

The present disclosure provides procedures and intermediates for the preparation of Sofosbuvir, comprising the step of reacting a compound of formula 2: wherein R.sub.1 and R.sub.2 can independently be hydrogen or halogen, provided that at least one of R.sub.1 and R.sub.2 is a halogen. ##STR00001##

PROCESSES FOR THE RESOLUTION OF BENZODIAZEPIN-2-ONE AND BENZOAZEPIN-2-ONE DERIVATIVES
20200157057 · 2020-05-21 ·

The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to processes and intermediates for the preparation of compounds of Formula (I-0) and Formula (I):

##STR00001##

PROCESSES FOR THE RESOLUTION OF BENZODIAZEPIN-2-ONE AND BENZOAZEPIN-2-ONE DERIVATIVES
20200157057 · 2020-05-21 ·

The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to processes and intermediates for the preparation of compounds of Formula (I-0) and Formula (I):

##STR00001##

Method for Separating Optically Active Hydroxy Cineole Derivatives

The present invention relates to a method for separating an optically active hydroxy cineole derivatives by lixiviation and crystallization and enantiomerically pure optically active hydroxy cineole derivatives of purity greater than 99.5% that have been prepared by this process. The present invention further relates to use of the desired enantiomer having enantiomeric excess of at least 99.5% ee as prepared according to the present invention, for the synthesis of enantiomerically pure 7-oxabicyclo[2.2.1]heptane derivatives.

Method for Separating Optically Active Hydroxy Cineole Derivatives

The present invention relates to a method for separating an optically active hydroxy cineole derivatives by lixiviation and crystallization and enantiomerically pure optically active hydroxy cineole derivatives of purity greater than 99.5% that have been prepared by this process. The present invention further relates to use of the desired enantiomer having enantiomeric excess of at least 99.5% ee as prepared according to the present invention, for the synthesis of enantiomerically pure 7-oxabicyclo[2.2.1]heptane derivatives.

Cinchonium betaine catalysts and methods of using same
20200147593 · 2020-05-14 ·

Provided herein are cinchonium betaine catalysts and methods of promoting asymmetric imine isomerization reactions using the same.

Cinchonium betaine catalysts and methods of using same
20200147593 · 2020-05-14 ·

Provided herein are cinchonium betaine catalysts and methods of promoting asymmetric imine isomerization reactions using the same.

Process for the Separation of Optical Isomers of Racemic 3-Alkylpiperidine-Carboxylic Acid Ethyl Esters
20200131126 · 2020-04-30 ·

The subject-matter of the invention is process for the separation of optical isomers of racemic 3-alk-3-carboxylic acid ethyl esters of formula rac-I with the resolving agent (II) ()-2,3:4,5-di-O-izopropylidene-2-keto-L-gulonic acid (hereinafter: diacetone-L-ketogulonic acid).

Process for the Separation of Optical Isomers of Racemic 3-Alkylpiperidine-Carboxylic Acid Ethyl Esters
20200131126 · 2020-04-30 ·

The subject-matter of the invention is process for the separation of optical isomers of racemic 3-alk-3-carboxylic acid ethyl esters of formula rac-I with the resolving agent (II) ()-2,3:4,5-di-O-izopropylidene-2-keto-L-gulonic acid (hereinafter: diacetone-L-ketogulonic acid).

SYNTHETIC ROUTE TO 2'-DEOXY-2',2'-DIFLUOROTETRAHYDROURIDINES

The present invention relates to methods and intermediates for synthesizing 2-deoxy-2,2-difluorotetrahydrouridine compounds.