Chemi S.p.a.

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Chem Spa

Mauro Anibaldi

Lorenzo De Ferra

Maurizio Zenoni

Stefano Turchetta

Ettore Ammirati

Paolo Brandi

Stefano Servi

Giorgio Berardi

Fabrizio Cocchi

Ezio Fasoli

Daniele Scorretti

A process for the purification of L-&#x3b1;-glycerophosphorylcholine is described, wherein L-&#x3b1;-glycerophosphorylcholine is crystallized from DMSO or from a mixture of DMSO with at least another solvent, preferably selected from water, alcohol, halogenated solvents, ethers, esters and/or amides. Such a process allows to obtain L-&#x3b1;-glycerophosphorylcholine having a purity greater than 99.5%, preferably greater than 99.7%, even more preferably greater than or equal to 99.9%. A method for determining the purity of L-&#x3b1;-glycerophosphorylcholine is also described, comprising the elution of L-&#x3b1;-glycerophosphorylcholine through an HPLC column having an amino stationary phase, and subsequent detection of L-&#x3b1;-glycerophosphorylcholine itself, and any impurity thereof, by means of an Evaporative Light Scattering Detector type.

Process for the purification of L-&#x3b1;-glycerophosphorylcholine

Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.

Process for the synthesis of azacitidine and decitabine

The document describes a process for the preparation of N-Acyl-Phosphatidyl-Ethanolamine of formula (I) on an industrial scale, In which R, Rand Rare, independently from each other, saturated, monounsaturated or polyunsaturated acyls C-C, pure or mixed together, and X&#x2550;OH or OM, where M=alkaline metal or alkaline earth, ammonium or alkylammonium. The process in question allows the conversion of lecithin of synthetic or natural origin into N-Acyl-Phosphatidyl-Ethanolamine of formula (I) of high purity, using a limited molar excess of the reagent N-acyl-ethanolamine, where the acyl is as defined above for the formula (I) through reaction of transphosphatidylation in the presence of the enzyme phospholipase D and in conditions suitable for production on an industrial scale. 

Process for the production of N-acyl-phosphatidyl-ethanolamine

Described is a new process for producing temozolomide, comprising the reaction between 5-aminoimidazole-4-carboxamide and N-succinimidyl-N'-methyl carbamate and the subsequent reaction of the thus obtained carbamoyl 5-aminoimidazole-4-carboxamide with sodium nitrite. Temozolomide is then purified by chromatography on adsorbent polymeric resin and subsequent crystallization from water and acetone.

Process for preparing temozolomide

Process for preparing lysophosphatidylcholine by selective monoacylation of glycerophosphorylcholine (1), in the presence of an acylating agent and of a dialkyltin derivative, according to the following diagram:  The process is particularly simple and has high overall yields.

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Patrica, Italy

Mauro Anibaldi