Ranbaxy Laboratories, Inc.

Other

Rakesh Kumar Arora

Yatendra Kumar

Jag Mohan Khanna

Kaptan Singh

Neera Tiwari

Shailendra Kumar Singh

Arun Malhotra

Jag M Khanna

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.

Amorphous form of cefpodoxime proxetil

A process for the manufacture of 7-acylamino-3-hydroxy-cephem-4-carboxylate-1-oxide in E-rotamer form (Formula III), comprises reacting a 7-acylamino-3-exomethylenecepham-4-carboxylate-1-oxide with ozone in an inert organic solvent in the presence of a catalytic amount of an organic or inorganic base at a temperature ranging from about -80.degree. C. to about +20.degree. C. The E-rotamer (wherein the 3-hydroxy group is strongly hydrogen bonded to the carbonyl of the 4-ester group) exhibits different chemical and physical properties from and is more thermodynamically stable than, the Z-rotamer (wherein there is no hydrogen bonding between the 3-hydroxy group and the carbonyl of the 4-ester group).

E-rotamers of 3-hydroy cephem derivatives

A process for converting cephalosporin p-nitrobenzyl ester (Formula I) to the corresponding cephalosporin free acid (Formula II) comprising treating the cephalosporin p-nitrobenzyl ester with a metal selected from the group consisting of iron, magnesium, aluminum, and tin, and with hydrochloric acid in a mixture of water and a water-miscible organic solvent. Preferably, the metal is iron in the form of a fine powder, and the reaction is carried out at a temperature in the range of 30.degree.-50.degree. C.

Process for P-nitrobenzyl ester cleavage in cephalosporin

A process for the manufacture of 7-acylamino-3-hydroxycephem-4-carboxylate-1-oxide in E-rotamer form (Formula III), comprises reacting a 7-acylamino-3-exomethylenecepham-4-carboxylate-1-oxide with ozone in an inert organic solvent in the presence of a catalytic amount of an organic or inorganic base at a temperature ranging from about -80.degree. C. to about +20.degree. C. The E-rotamer (wherein the 3-hydroxy group is strongly hydrogen bonded to the carbonyl of the 4-ester group) exhibits different chemical and physical properties from and is more thermodynamically stable than, the Z-rotamer (wherein there is no hydrogen bonding between the 3-hydroxy group and the carbonyl of the 4-ester group).

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Haryana, India

Rakesh Kumar Arora