Synthetic Chemistry
Capabilities and Services 

About the cover:  A molecular model of a transmembrane protein

With more than 20 years of experience in synthesis, medicinal chemistry, and drug product advancement, Southwest Research Institute (SwRI) provides comprehensive services ranging from drug idea conception through phase II clinical trials.

SwRI offers synthesis and medicinal chemistry services for laboratory and pilot plant as well as expert capabilities in drug formulation and drug delivery through microencapsulation. Because of these capabilities, the Institute can partner with clients at any phase including development and commercialization. The SwRI research model favors a problem-solving and project management approach, which focuses on client deliverables.

SwRI scientists use top-of-the-line molecular modeling systems for applying computational methods to aid in understanding protein and ligand interactions and new compound designs.

Laboratory-Scale Synthesis

To support client needs in all stages of early drug discovery, SwRI provides custom synthesis of compounds for multiple drug discovery applications. Institute personnel offer extensive experience in synthesis and medicinal chemistry strategies, drug design, synthetic route design, and execution. Institute staff members offer a variety of services, including:

• Provide synthesis on milligram to 50+gram scale
• Follow established synthetic routes, design new synthetic routes, or trouble-shoot existing synthetic routes
• Provide custom intermediate/template or monomer/reagent synthesis
• Prepare analog synthesis
• Produce synthesis of metabolites or standards
• Develop molecular modeling studies for compound design and for pharmacophore development and screening (Accelyrs System®)

At SwRI, experienced chemists perform multistep synthesis of target compounds using a large variety of synthesis techniques and expertise. The Synthesis and Medicinal Chemistry laboratories at SwRI can handle a diverse range of reaction scale, and has larger scale walk-in hoods and equipment.

Process Research Capabilities and Services

To support client needs in all stages of process development and technology transfer, SwRI provides process research and kilo-scale current Good Manufacturing Practices (cGMP) and noncGMP custom synthesis services for a wide range of drug development applications, including:

• Kilogram-scale facility
• Synthesis route and process development
• Process technology transfer
• Regulatory assistance
• cGMP API synthesis
• Chiral resolution
• Polymorph screening
• Cryogenic and ambient milling and micronization
• Spray drying and disk atomization

SwRI chemists determine the molecular structure of synthetic intermediates, using a Varian Unity/Inova 400 with a liquids probe (ATB), a nanoprobe (inverse ¹H, ¹³C), and a solids probe (CP/MAS).

Experience in Drug Research and Development

Institute staff members have extensive experience in helping develop and market new and innovative drugs. For more than 20 years, SwRI chemists have aided clients with a wide range of requirements, including:

• Multiple start-ups and technical transfers
• Polymorph control
• Preclinical drug supply management and process development
• Chemistry, Manufacturing, and Controls (CMC) strategy, including more than 10 Investigational New Drug (IND) applications and 15 CMCs filed
• Process improvement
• Department of Energy requirements
• cGMP operation

Expert Synthetic Knowledge

Institute scientists have worked with a wide range of synthetic compounds, including:

• Bicyclic amines
• Heterocyclic compounds
• Asymmetric synthesis
• pyrrolo[2,3-d]pyrimidines
• thieno[2,3-d]pyrimidines
• beta-lactams
• Synthetic molecular sensors
• Carbohydrate synthesis

SwRI Facilities and Equipment

The Institute has almost two million square feet of office, laboratories, test facilities and other state-of-the-art facilities and equipment, such as:

• 12- to 200-liter glass reactors (from –70 to 200°C)
• Stirred Teflon®-lined pressure filter
• Multiple synthesis/medicinal chemistry lab and hood set-ups
• Walk-in hoods and glassware for large-scale chemistry
• 316 stainless steel centrifuge
• Support tanks and receivers
• 20-liter rotary evaporator
• Vacuum and forced air drying equipment
• Three pilot plants
• Jet mill, ball-mill, co-mill facilities
• Specialty equipment, including:

• 400-MHz Varian nuclear magnetic resonance apparatus
• HPLC/MS, GC
• HPLC/DAD
• Hydrogenation capabilities
   

This brochure was originally published in February 2007. For more information about Synthetic Chemistry, contact Dr. Stan McHardy, Phone (210) 522-2669, Chemical and Pharmaceutical Synthesis Section, or Dr. Joseph McDonough, Phone (210) 522-3670, Synthesis and Drug Delivery Section, Chemistry and Chemical Engineering Division, Southwest Research Institute, P.O. Drawer 28510, San Antonio, Texas 78228-0510, Fax (210) 522-4632.

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