Ilex Products, Inc.

Genzyme Corporation

Dennis P Lovett

William E Bauta

William R Cantrell, Jr

Jose Puente

Brian D Burke

Brian E Schulmeier

The present invention for the stereoselective preparation of 2-deoxy-&#x3b2;-D-adenine nucleosides wherein a blocked 2-deoxy-&#x3b1;-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative.

Process for preparing purine nucleosides

The present invention provides a process for the preparation of homophthlate esters useful in the preparation of homophthalic anhydride reactants.

Process for preparing homophthalate derivatives

The present invention provides for the preparation &bgr;-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and solvent. The present invention also provides for the stereoselective preparation of 2-deoxy-&bgr;-D-adenine nucleosides wherein a blocked 2-deoxy-&agr;-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. The forgoing aspects of the present invention are utilized in the preparation of a clofarabine composition wherein the ratio of &bgr; to &agr;-anomer is at least 99:1.

The present invention provides a process from preparing isocoumarin-3-yl derivatives comprising reacting a homophthalic anhydride derivative with a carbonyl compound, wherein the carbonyl group is substituted with an acyl activating group, in the presence of a reaction medium comprising a solvent and a base. The invention also encompasses a process for the preparation of homophthalate esters useful in the preparation of homophthalic anhydride reactants as well as an integrated process wherein the twp reactions are carried out sequentially to afford the desired isocoumarin derivative.

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San Antonio, TX, United States of America

Dennis P Lovett