Ranbaxy Laboratories, Inc.

Sun Pharmaceutical Industries Limited

Kaptan Singh

Mohan Prasad

Yatendra Kumar

Gyanendra Pandey

Rakesh Kumar Arora

Santosh Richhariya

Satish Manohar Bhoge

Prakash Kshirsagar

Md Abul Kalam Azad

Shravan Kumar Singh

Shyam Sunder Verma

Pankaj Sharma

Javeena

Prakash Bhimaji Kshirsagar

The present invention provides processes for the preparation of baricitinib of Formula I and an intermediate of Formula V. The present invention also provides the use of the intermediate of Formula V for the preparation of baricitinib. 

Process for the preparation of baricitinib and an intermediate thereof

The present invention provides a crystalline Form I of afatinib dimaleate, its process for preparation and pharmaceutical composition thereof, and its use in the treatment of metastatic non-small cell lung cancer.

Crystalline form of afatinib dimaleate

The present invention provides a crystalline form of baricitinib characterized by an XRPD pattern substantially as depicted in FIG., a process for its preparation, a pharmaceutical composition comprising it, and its use for the treatment of JAK-associated diseases.

Crystalline form of baricitinib

The present invention provides a process for the preparation of baricitinib and an intermediate thereof. The present invention provides a convenient, economical, and industrially advantageous two-step process for the preparation of [4-(IH-pyrazol-4-yl)-7Hpyrrolo[2,3-d] pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention involves the use of an alkali or alkaline earth metal hydroxide, carbonate, or bicarbonate as a base for reacting 4-chloro-7H-pyrrolo[2,3-d]pyrimidine of Formula (III) with chloromethyl pivalate of Formula (IV), and the use of an unprotected pyrazole borolane of Formula (VIII) for the conversion of (4-chloro-7H-pyrrolo[2,3-d] pyrimidin-7-yl)methyl 2,2-dimethylpropanoate of Formula V into [4-(1H-pyrazol-4-yl)-7Hpyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention provides [4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (I) in high yield.

The present invention provides a process for the preparation of 4-dimethylaminocrotonic acid of Formula (II) or its salts, which is used as an intermediate for the preparation of afatinib or its salts. 

Process for the preparation of 4-dimethylaminocrotonic acid

The present invention relates to process for the preparation of fosamprenavir calcium.

Process for the preparation of fosamprenavir calcium

The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and pharmaceutically acceptable salts thereof.

Process for stereoselective synthesis of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine

The present invention relates to a cost effective and industrially useful process for the preparation of substantially pure acitretin. More specifically, the present invention relates to the preparation of acitretin of high purity and yield.

Process for the preparation of acitretin

The present invention relates to an improved and cost effective process for the industrial manufacture of cefpodoxime proxetil. More specifically, the present invention relates to the preparation of cefpodoxime proxetil of high purity and yield. The process comprises a) dissolving impure cefpodoxime proxetil or adding a solution containing cefpodoxime proxetil into a polar organic solvent or mixture(s) thereof, optionally reducing the solvent by concentration, and adding into a non-polar organic solvent or mixture(s) thereof to precipitate the solid; and b) dissolving the solid obtained from the above step into water-miscible polar organic solvent, optionally reducing the solvent by concentration, adding it into water to obtain the pure cefpodoxime proxetil.

Cefpodixime proxetil

A novel process for the production of an improved amorphous form of cefpodoxime proxetil &lsqb;(6R-&lsqb;6&agr;,7&bgr;(Z))&rsqb;-7-&lcub;E(2-Amino-4-thiazolyl)(methoxyimino)acetyl&rsqb;amino&rsqb;-3-(methoxymethyl)-8-oxo-5-thia-1-azabicyclo&lsqb;4.2.0&rsqb;oct-2-ene-2-carboxylic acid-1-&lsqb;&lsqb;(1-methylethoxy)carboxylic acid-1-&lsqb;&lsqb;(1-methylethoxy)carbonyl&rsqb;oxy&rsqb;ethyl ester, is described.

Growing community of inventors

Gurgaon, India

Kaptan Singh