Acic (canada) Inc.

Brantford Chemicals Inc.

Apotex Pharmachem Inc.

Bruno K Radatus

Khashayar Karimian

Keshava Ks Murthy

K S Keshava Murthy

Gamini Weeratunga

Anand Daljeet

Allan W Rey

Stephen E Horne

Yajun Zhao

Derek John Norris

Gurijala V Reddy

Chandrawansha B W Senanayake

Kanwarpal S Swidhu

Kanwar Pal Sidhu

Tania E Nish

Ks Keshava Murthy

A process for the industrial scale manufacture of 4-(4-fluorophenyl)-N-alkylnipecotinate esters by the addition of 4-fluorophenylmagnesium halide in tetrahydrofuran to 3,4-unsaturated-3-piperidine esters.

Preparation of 4-(4-fluorophenyl)-N-alkylnipecotinate esters, 4-(4-fluorophenyl)-N-arylnipecotinate esters and 4-(4-fluorophenyl)-N-aralkylnipecotinate esters

There are disclosed novel Stavudine solvates as follows: Stavudine NN-dimethyllacetamide solvates; Stavudine NN-dimethylacrylamide solvates and Stavudine NN-dimethylpropionamide solvates and processes for producing Stavudine NN-dimethylacetamide solvates, Stavudine NN dimethylacrylamide solvates and Stavudine NN dimethylpropionamide solvates which results in pure Stavudine.

Process for the preparation of substantially pure stavudine and related intermediates useful in the preparation thereof

1,3-oxathiolan-5-ones useful in the production of antiviral nucleoside analogues

Process for the manufacture of related intermediates including cistofur

A process from preparing 5-halogenated 2,3-O-cyclocytidine derivatives comprising reacting 2,3-O-cyclocytidine with a halogenating reagent, preferably N-bromosuccinimide, in the presence of an acid such as acetic or trifluoroacetic.

Process for preparing halogenated 2,3-O-cyclocytidine derivatives

Compounds of Formula IV: ##STR1## are described. In the compounds of Formula IV, R.sup.6 is selected from a trifluoromethyl group, a C.sub.1 -C.sub.6 alkyl group and a C.sub.6 -C.sub.9 aryl group, and R.sup.1 is selected from hydrogen, trityl, methoxytrityl, dimethoxytrityl, acetyl, a C2-C6 alkylacyl group, a C6-C9 arylacyl group, allyl, 2,2,2-trichloroethyl, phosphates and salts thereof, tosyl and mesyl. The above organosulfonyl salts of 2,3'-O-cyclocytidine are intermediates in the preparation of 1-(B-D-xylopentofuranose)cytosine, an inhibitor of DNA synthesis.

Organosulfonyl salts of 2,3'-O-cyclocytidine

A 5'-halo-2,3'-O-cyclocytidine of Formula I: ##STR1## wherein: X is a bromide, chloride, or iodide; Y is halide, sulfate, acetate, tosyl, mesyl, benzoate, and phosphate; R.sup.1 is hydrogen; and R.sup.2 is a hydroxy protecting group. Pharmaceutical compositions containing the above compounds exhibit antineoplastic activity.

5-halo-2,3'-O-cyclocytidines

Process for the production of an improved form of Form 1 Ranitidine Hydrochloride having improved filtration and drying characteristics, said process comprising in a substantially anhydrous hydroxylic solvent, comprising at least one alkanol solvent having 3-4 carbon atoms, adding anhydrous hydrogen chloride gas to Ranitidine free base wherein said substantially anhydrous hydroxylic solvent has the characteristics that it solubilizes the Ranitidine free base and hydrogen chloride gas, and subsequently recovering the improved form of Form 1 Ranitidine Hydrochloride.

Form of form 1 Ranitidine

A composition of a 1:1 molar complex of guanidine and 3'-azido-3'-deoxythymidine (AZT) which is generated at about pH above 9 and disrupted by pH below about 9. This complex is a useful intermediate in the purification of AZT.

Complex of guanidine and AZT

A process for making Fluconazole comprising the steps of: ##STR1##

Methods for the manufacture of fluconazole

Process for preparing 2,3'-O-cyclocytidine

A process for recovering 3'-azido-3'-deoxythymidine (AZT) or a salt thereof from a mixture of chemicals involving the reaction of the AZT with guanidine to form a salt precipitate. The salt precipitate is then acidified to pH of less than about 9 to yield free AZT, which can then be crystallized from solution. 3'-Azido-3'-deoxythymidine and its salts, also known as AZT and Zidovudine, is used in the treatment of AIDS patients.

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Brantford, Canada

Bruno K Radatus