Green Chemisstry in Pharmaceuticals
Handbook from C.H.I.P.S.

Green Chemistry in the Pharmaceutical Industry
edited by Peter J. Dunn

Green Chemistry in the Pharmaceutical Industry covers all aspects of green chemistry in the pharmaceutical industry, from simple molecules to complex proteins, and from drug discovery to the fate of pharmaceuticals in the environment.

This handbook contains several convincing case studies from industry, such as Taxol, Pregabalin and Crestor, illustrating how this multidisciplinary approach has yielded efficient and environmentally-friendly processes. Finally, a section on technology and tools highlights the advantages of green chemistry.


Introduction to Green Chemistry, Organic Synthesis and Pharmaceuticals

  1. The Development of Organic Synthesis
  2. The Environmental Factor
  3. The Role of Catalysis
  4. Green Chemistry: Benign by Design
  5. Ibuprofen Manufacture
  6. The Question of Solvents: Alternative Reaction Media
  7. Biocatalysis: Green Chemistry Meets White Biotechnology

Green Chemistry Metrics

  1. Measuring Resource Usage
  2. Life Cycle Assessment (LCA)
  3. Measuring Chemistry and Process Efficiency
  4. Measuring Process Parameters and Emissions
  5. Real Time Analysis
  6. Operational Efficiency
  7. Measuring Energy
  8. Measuring the Toxicity of All the Substrates
  9. Measuring Degradation Potential
  10. Measuring the Inherent Safety of Lack of Inherent Safety

Solvent Use and Waste Issues

  1. Solvent and Process Greenness Scoring and Selection Tools
  2. Waste Minimization and Solvent Recovery

Environmental and Regulatory Aspects

  1. Historical Perspective
  2. Pharmaceuticals in the Environment
  3. Environmental Regulations

Synthesis of Sitagliptin, the Active Ingredient in Januvia and Janumet

  1. First-Generation Route
  2. Sitagliptin through Diastereoselective Hydrogenation of an Enamine. The PGA Enamine-Ester Route
  3. The Triazole Fragment
  4. Direct Preparation of Beta-Keto Amides
  5. Second-Generation Chiral Auxiliary Route. The PGA Enamine-Amide Route
  6. Prufication and Isolation of Sitagliptin (Pharmaceutical Form)
  7. The Final Manufacturing Route

The Development of Short, Efficient, Economic, and Sustainable chemoenzymatic Processes for Statin Side Chains

  1. Biocatalysis
  2. The Relevance of Statins
  3. Biocatalytic Routes to Statin Side Chains
  4. 2-Deoxy-D-Ribose 5-Phosphate Aldolase (DERA)-Based Routes to Statin Intermediates

The Taxol Story-Development of a Green Synthesis Via Plant Cell Fermentation

  1. Discovery and Early Development
  2. From Extraction of Taxol from Pacific Yew Tree Bark to Semi-Synthetic Taxol
  3. Taxol from Plant Cell Fermentation
  4. Comparison of Semi-Synthetic versus PCF Taxol Processes: The Environmental Impact
  5. Comparison of Semi-Synthetic versus PCF Taxol: Green Chemistry Principles

The Development of a Green, Energy Efficient, Chemoenzymatic Manufacturing Process of Pregabalin

  1. Process Routes to Pregabalin
  2. Biocatalytic Route to Pregabalin
  3. Green Chemistry Considerations

Green Processes for Peptide Mimetic Diabetic Drugs

  1. Green Chemistry Considerations in Peptide-like API manufacture
  2. Purification Process to Manufacture Amorphous API
  3. Preparation of Unnatural Amino Acids

The Development of an Environmentally Sustainable Process for Radafaxine

  1. Chemistry Process and the Dynamic Kinetic Resolution (DKR)
  2. Multicolumn Chromatography: Development of Route 4
  3. Environmental Assessment

Continuous Processing in the Pharmaceutical Industry

  1. Continuous Production of a Key Intermediate for Atorvastatin
  2. Continuous Process to Prepare Celecoxib
  3. Continuous Oxidation of Alcohols to Aldehydes
  4. Continuous Production of Bromonitromethane
  5. Continuous Production and Use of Diazomehtane
  6. A Snapshot of Some Further Continuous Processes Used in the Preparation of Pharmaceutical Agents

Preparataive and Industrial Scale Chromatography: Green and Integrated Processes

  1. Basic Principles of Chromatography
  2. Process Optimization to Reduce Eluent Consumption
  3. Use of a Green Solvent: Supercritical Carbon Dioxide
  4. Solvent Recycling Technologies
  5. Application Examples
  6. An Environmentally Friendly Solution for Each Separation

Dynamic Resolution of Chiral Amine Pharmaceuticals: Turning Waste Isomers into Useful Product

  1. Integration of Chiral Amine Resolution and Racemization
  2. Case StudiesM

Green Technologies in the Generic Pharmaceutical Industry

  1. 'Waste': Definition and Remedy
  2. Amidation
  3. Synthesis of Galanthamine
  4. Synthesis of Solefinacin
  5. Synthesis of Levetiracetam
  6. Synthesis of a Finasteride Intermediate
  7. Bromination
  8. Sulfoxidation in the Synthesis of Rabeprazole

Environmental Considerations in Biologics Manufacture

  1. Therapeutic Biologics
  2. Environmental Impact Considerations
  3. Overall Comparison
  4. Environmental Indices for Therapeutic Protein Manufacture
  5. Technologies with Potential Environmental Impact
  6. Single-Use Biologics Manufacture

Future Trends for Green Chemistry in the Pharmaceutical Industry

  1. Waste Minimization in Drug Discovery
  2. Greener Synthetic Methods in Primary Manufacturing
  3. Alternative Solvents in the Pharmaceutical Industry
  4. Green Chemistry in Secondary Pharmaceutical Operations
  5. Global Cooperation in Green Chemistry


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Green Chemistry in the Pharmaceutical Industry
edited by Peter J. Dunn
2010 • 388 pages • $179.00 + shipping
Texas residents please add 6.75 % sales tax

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