Chirality in Drug Compounds

May 18-19, 2009 • Philadelphia, PA

Benefits of Attending:• Achieve efficacy of pharmaceutical

compounds• Increase percentage yield• Discover new chiral structures to expand

research options• Minimize research costs• Reduce time to market• Drive efficiency and cut waste

Presenting Companies Include:Bristol-Myers Squibb

Cornerstone Pharmaceuticals

Johnson & Johnson

Lundbeck Research USA

Pfizer

Pharmacopeia

Rigel Pharmaceuticals

Sapphire Therapeutics, Inc.

University of the Sciences in Philadelphia

Drug CompoundsChirality in

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Register by 3/13/2009 for theAll-Access Pass and Save $898

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Techniques to obtain the molecule with the right pharmalogical profile

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Media Partners:

Sponsors:

Who Should AttendThis conference is designed scientistsfrom both pharmaceuticals and academiawith a focus in:

Sponsorship andExhibition OpportunitiesSponsorships and Exhibits are excellentopportunities for your company to showcaseits products and services to high-level, targeteddecision makers attending the conference.Pharma IQ and Chirality in DrugCompounds will help companies like yoursachieve sales, marketing and brandingobjectives by setting aside a limited number ofevent sponsorships and exhibit spaces – all ofwhich are custom-tailored to help yourcompany create a platform to maximize itsexposure at the event.

For more information on Sponsoring andExhibiting at Chirality in Drug Compounds,please contact Thomas Boccard at 1-866-232-8660 or [email protected].

Conferences and Webinars available:Visit us at www.iqpc.com and see what otherexciting and information-packed conferencesand webinars being offered by theInternational Quality & Productivity Center.

About the Organizer: Pharma IQ, thepharmaceutical divisionof IQPC, provides a

forum to address thecritical issues facing the pharmaceuticalindustry today. Pharma IQ utilizes workshop,conference and training course formats tofacilitate a learning environment forpharmaceutical professional working in allareas of drug development from Discovery toPost-Marketing.

• Discovery • Green Chemistry • Research & Development • Chemical Engineering• Biotransformation • Organic Chemistry • Biochemistry• Analytic Chemistry

Dear Colleague,

In the current cost-conscious health care environment, the pharmaceuticalindustry must take full advantage of available resources to providedesperately needed new product opportunities. Scientists operating withinthis environment must increase their awareness and utilization of an array ofnew technologies in cooperative partnerships to compete successfully intoday’s market. These technologies not only accelerate time to the desireddecision point, but also offer long-term opportunities for superior efficiencyduring commercial route development and manufacturing.

The necessity to analyze and purify chiral compounds has increased.

As demanded by the FDA, chiral pharmaceuticals should be developed andreach the market as single enantiomer products. This fact makes robustchiral separation methods essential for product quality control analysis,because the unwanted enantiomer is often the most critical productimpurity.

Here’s a rundown at what you’ll experience at Chirality in Drug Compounds:• Discover new research - the opportunities to encounter cutting-edgescience are endless • Advance your career while enhancing your skills• Make Connections - network through unparalleled opportunities • Learn how your peers are successfully utilizing technology

I look forward to greeting you in Philadelphia!

Sincerely,

Michelle CardinalSr. Conference DirectorIQPC-NY

2 1-800-882- 8684 • www.iqpc.com/us/chirality

May 18-19, 2009 • Philadelphia, PA


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2:00 Registration for Main Conference

2:30 Chairperson’s Opening Remarks

2:40 Opening Keynote: Importance of Chirality in DrugsThe importance of chirality in drugs and other pharmaceuticalproducts cannot be understated. Modern synthetic methods nowallow the use of asymmetric reactions with chiral catalysts or reagentsto obtain desired isomers. Powerful separations techniques have alsobeen developed to achieve the same goal. These create newopportunities in drug discovery and development. This openingkeynote will cover:• Importance of chirality • Enantiomeric consideration and the revolutionary changes to drug

development • Effects of chirality on intellectual property

Adeboye Adejare, PhDProfessor & Chair, Department of Pharmaceutical Sciences,Philadelphia College of PharmacyUniversity of the Sciences in Philadelphia

3:40 Panel: Preparative Chromatography for ChiralResolutions of Pharmaceutical Intermediates inDrug Discovery and Development StagesChromatographic technology has been widely used for theenantiomer resolution in early stages of drug discovery anddevelopment. Supercritical fluid chromatography (SFC) is usedpredominately in drug discovery stage due to its rapid sample turnaround and less organic solvent usage. Other technologies such assimulated moving bed (SMB), steady state recycling (SSR), and batchHPLC are also used in the drug development stage. The selection and

application of these technologies are depended on selectivity, samplesolubility, sample size, and system availability. Examples, pros andcons of these technologies are discussed

Tony YanPrincipal ScientistPfizer Global R&D

Bob DepiantaScientist Pfizer Global R&D

Jim BradowScientistPfizer Global R&D

Laurence PhilippeAssociate Research FellowPfizer Global R&D

4:30 Asymmetric Hydrogenation for Early Stage DrugDevelopmentNew techniques for phase-transfer hydrogenation as well asinexpensive parallel pressure reactors have revolutionized reactionscreening to deliver maximum speed and efficiency. Newhydrogenation technologies and approaches that provide thepotential for accelerated discovery of chiral route opportunities usinghydrogenation will be a focal point.

Christopher A. TelehaResearch FellowJohnson & Johnson

5:15 Close of Day One

Monday, May 18, 2009

Main Conference Day One

Monday, May 18, 2009

Pre-Conference Workshops


Workshop A 8:00 Workshop Registration

8:30 – 11:00

Approaches to Diastereomeric Crystallization to SeparateEnantiomers from Racemic MixturesOptical resolution through diastereomeric crystallization chemically separatesenantiomers from racemic mixture by producing a salt. Because of the experimentalconsistency and easy adoption to manufacturing scale, it provides the most rapid andcost-effective access to high-purity chiral drug intermediates and robust large-scaleindustrial processes. This workshop will include discussions on:• Rapid process optimization using high-throughput screening• Resolution of neutral racemates• Resolution of molecules with multiple chiral centers• Going from bench-top to scale-upIt will also focus on the “Green Chemistry” aspects like:• Minimizing the amount of chemicals• Avoiding the use of toxic chemicals• Solvent-less reactions• Reuse of chemicals Heightened proficiency with modern techniques and added familiarity with pertinentexamples of industrial application will convey greater expertise to practitioners of chiraldrug synthesis.

Niteen A. Vaidya, PhDCTO ChiroSolve Inc.

Workshop B 11:00 Workshop Registration

11:30 – 2:00 (Lunch will be served)

Enzymatic Biotransformation: Practical Tools forDrug Synthesis Enzymatic synthesis has left the realm of whole-cell fermentationand voluminous processing to enter an era of isolatedcommercial biocatalysts performing as reagents, therebybecoming more accessible and usable by today’s laboratoryscientists. The first step in enabling their use is a generalunderstanding of the available catalysts, their ease of use, andtheir relative likelihood of success. The second step is theincorporation of this new understanding in route design anddevelopment for application toward API synthesis.• Achieve high success rates with enzymes as reagents in

retrosynthesis• Create user-friendly biotransformation in the laboratory setting• Optimize enzyme reactions• Design strategies for basic enzyme engineering• Navigate regulatory implications of biotransformation

Workshop leader is to be announced. Please check thewebsite at www.iqpc.com/us/chirality for updates andannouncements.

8:00 Registration & Coffee

8:30 Chairperson’s Recap of Day One

8:45 Marfey’s Reagent: Past, Present, & FutureUses for the Pre-column Derivatizing Reagentfor the Separation of Enantiomeric Isomers ofAmino Acids & Amine CompoundsThe present abstract describes characteristics and applicationof Marfey’s reagent (MR) including general synthesis of thereagent and diastereomers along with advantages,disadvantages and the required precautions. Applications, andcomparison with other derivatizing agents, for the resolutionof complex mixtures of DL-amino acids, amines and non-proteinogenic amino acids, peptides/amino acids.

Deepak Gupta, PhDSenior ScientistCornerstone Pharmaceuticals

9:45 Building a Highly Automated 5 Pump (3Gradient, 2 Isocratic), 4 Detector (2 UV, ELSD& MS) Super-Critical Fluid Chromatography(SFC) System For Chiral Purification In DrugDiscovery When building our gradient SFC/MS based chiral purificationplatform for drug discovery, Lundbeck Research designedspecifications based solely on the existing practices of themedicinal chemists and business need. Specifically, theyconcluded that we must routinely inject ≥100 mg and yield 10 gper day of high purity (95-99% ee) for any number of compounds(1-100). These specifications tend to require gradient operationand significantly exceed those of the off the shelf instrumentationmore commonly used in this setting, particularly with regard tomass per injection for many compounds. Hear how they set outto find better ways to use the available instruments and ultimatelymeet their business need.

Mark Hayward, PhDAssociate Director, Analytical Chemistry Department, DiscoveryAutomation DepartmentLundbeck Research

10:45 Networking Break

11:30 Chiral Supercritical Fluid Chromatography inDrug Discovery: from Analytical toMultigram-Scale• Higher throughput with higher flow rate and shorter cycle

time• Less solvent consumption/disposal cost• Less packaging time after preparative separations• Solubility issues minimized • Higher efficiency than HPLC, ideal for challenging separations

Dauh-Rurng WuPrincipal ScientistBristol-Myers Squibb

12:30 Networking Lunch

1:45 Practical Approaches to ChiralChromatography by Supercritical FluidChromatographic (SFC) TechniquesEnantiopure drug compounds are essential for toxicity andefficacy studies since chirality can influence or exhibitsubstantially different chemical and toxicological effects. Chiralchromatography is broadly used as a rapid tool to separate andisolate these pure enantiomers and SFC has emerged as thepreferred technique to support the various stages of drugdevelopment. The scope of this presentation highlights somereal-world uses of SFC for analysis and purification of chirallyactive pharmaceutical compounds.

Christine Aurigemma Principal Scientist Pfizer Global R&D

2:45 A Parallel Normal Phase Gradient ScreenApproach to Rapid Chiral MethodDevelopment • The Normal Phase Parallel Gradient Screen Approach allows

the user to simultaneously screen multiple chiral stationaryphases and solvent combinations in a shorter time

• The parallel approach increases the speed of methoddevelopment by at least a factor of five

• The gradient approach further extends the success of themethod for a wide range of molecules to achieve a directlyscaleable, rapid isocratic chiral separation method

Douglas MooreAssociate Research Scientist IIBristol-Myers Squibb

Michael Hicks, PhDSenior Investigator IBristol-Myers Squibb

3:45 Networking Break

4:15 Super-Critical Fluid Chromatography (SFC)with Tandem Mass Spectrometry (MS/MS) toEvaluate the Disposition of Individual Stereo-Isomers of DrugsFrequently, candidate compounds in drug discovery anddevelopment programs are chiral. Separations formeasurement of these compounds are typically done withnormal phase LC (NP-LC) or supercritical fluid chromatography(SFC). Mass spectrometry (MS) can dramatically enhancesensitivity and specificity of detection which can be of highvalue for samples coming from in vitro and in vivo studies.However, only SFC (not NP-LC) can be easily interfaced with aMS. Hear how Lundbeck Research • Coupled analytical-scale SFC with both single-quadrupole

(SFC/MS) and triple-quadrupole (SFC/MS/MS) massspectrometers while comparing the benefits of each

• Used this combination to take advantage of the low viscosityin SFC for fast chiral separations simultaneously with thehigh sensitivity and specificity of MS (or MS/MS)

Mark Hayward, PhDAssociate Director, Analytical Chemistry Department, DiscoveryAutomation DepartmentLundbeck Research

5:15 Close of Conference

Tuesday, May 19, 2009

Main Conference Day Two


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About Our SponsorsAvantium Technologies’ core competency resides in solid statepharmaceutical chemistry and crystal engineering for smallmolecules. We provide fast-paced, high-throughput

crystallization services to the pharmaceutical industry. We support yourchemical and pharmaceutical development efforts from pre-clinical stages toNDA and help accelerate the APIs time-to-market. Key service elements:• Identification, characterization, selection of and recommendations for optimal

polymorphs, salts and co-crystals + scale-ups • Amorphous API stabilization via solid dispersions • Comprehensive form space identification: define & safeguard IP rights for

Phase II and molecules • Comprehensive solubility screening programs • Crystallization process development optimization, enantiomer separation via

chiral resolution. Website: www.avantium.com

Chirality in Drug Compounds



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Chirality in Drug Compounds