Apotex Pharmachem Inc.

Brantford Chemicals Inc.

Syntex (u.s.a.) Inc.

Acic (canada) Inc.

Stephen E Horne

Gamini Weeratunga

K S Keshava Murthy

Daqing Che

Bhaskar Reddy Guntoori

Zhi-Xian Wang

Teng Jiam Liak

Elena Bejan

Arlindo Lucas Castelhano

Allan W Rey

Keshava Ks Murthy

Fan Wang

Carlos Zetina-Rocha

Derrick L Clive

Derek John Norris

Zhengyu Yuan

Svetoslav S Bratovanov

Alexander Krantz

Yajun Zhao

Lotfi Derdour

Laura Kaye Montemayor

Jian Jeffrey Chen

Steven Lee Bender

Judith Gail Deal

Bruno K Radatus

Probal Kanti Datta

Jaipal Reddy Nagireddy

Paul David Cannon

Sammy Chris Duncan

David A Stradiotto

Ks Keshava Murthy

Keshava K S Murthy

Mohamed Ibrahim Zaki

Martin Ehlert

Chandrawansha B W Senanayake

Gurijala V Reddy

Shawn Young

Hal Van Wart

Abbulu Kante

Matthew A Buck

Bogdan M Comanita

Laura Kaye McConachie

A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.

Process for the preparation of esomeprazole and salts thereof

A process for the preparation of an acid addition salt of an organic base comprising exposing the organic base in solid form to a gaseous acid, with the proviso that ziprasidone, its acid addition salts and intermediates thereof are excluded.

Preparation of acid addition salts of amine bases by solid phase&#x2014;gas phase reactions

An industrially acceptable process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3')quiniclidine from a cis/trans mixture of isomers. Treatment of the mixture with an organic sulfonic acid generates a less soluble acid addition salt that is enriched in the cis-isomer. Recrystallization or pulping using various organic solvents allows for enrichment of the cis-isomer by filtration. These new sulfonic acid salts of the cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3&#x2032;)quiniclidine prepared according to the present invention could be further converted into the hydrochloride salt by any known procedures such as treatment with a base and then hydrochloric acid salt formation or exchange of the sulfonic acid salt with hydrochloric acid.

Process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3')quiniclidine hydrochloride

An industrially acceptable process for the preparation of 2-methylspiro(1,3-oxathiolane-5,3')quiniclidine. The cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3&#x2032;)quiniclidine is known generally as Cevimeline.

Process for the preparation of 2-methylspiro(1,3-oxathiolane-5,3')quiniclidine

The present invention relates to a new and useful amorphous form of ziprasidone hydrochloride (5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride) and preparations thereof.

Amorphous ziprasidone hydrochloride (5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride) and processes to produce the same

A process for the preparation and purification of Eplerenone is described wherein hydroxylated impurities are removed using a novel derivatization procedure.

Process for the preparation and purification of eplerenone

A process for the preparation of aminoalkyl phenyl carbamate compounds of Formula I, wherein Rand Rindependently are hydrogen or a Calkyl; Rand Rare the same or different and each is a Calkyl; or Rand Rtogether with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; Rand Rindependently are hydrogen, linear, branched or cyclic Calkyl; or Rand Rtogether with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; the carbon centre designated '*' can be racemic or enantiomerically enriched in the (R)- or (S)- configuration; and pharmaceutically acceptable acid addition salts thereof.

Process for the preparation of phenylcarbamates

A process is provided for preparing pharmaceutical grade atorvastatin hemicalcium salt comprising:  

Process for producing atorvastatin hemicalcium

A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester comprising:

Preparation of atorvastatin

The present invention relates to new and useful processes for the preparation of the anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride.

Preparation of an anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride (ziprasidone hydrochloride)

A process for the preparation of a polypeptide designated in the present invention as 1, composed of the following amino acid units in the structure, namely: L-alanine, L-glutamic acid, L-lysine and L-tyrosine randomly arranged in the polypeptide 1, or pharmaceutically acceptable salts thereof, comprising the steps of:   

Process for the preparation of polypeptide 1

Preparation of chiral 1,2,3,4-tetrahydro-6,7-dialkoxy-3-isoquinolinecarboxylic acid and derivatives

This invention relates to the preparation of 3-sulfonamido-4-arylaminopyridines by heating a 3-sulfonamido-4-aminopyridine with an aryl halide in the presence of an alkaline compound, a copper-containing agent and in the presence of a polar protic solvent.

Preparation of derivative of 3-sulfonamido-4-phenylaminopyridine

Matrix metalloprotease inhibitors

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Burlington, Canada

Stephen E Horne