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.

Contents

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

8. Measuring Resource Usage
9. Life Cycle Assessment (LCA)
10. Measuring Chemistry and Process Efficiency
11. Measuring Process Parameters and Emissions
12. Real Time Analysis
13. Operational Efficiency
14. Measuring Energy
15. Measuring the Toxicity of All the Substrates
16. Measuring Degradation Potential
17. Measuring the Inherent Safety of Lack of Inherent Safety

Solvent Use and Waste Issues

18. Solvent and Process Greenness Scoring and Selection Tools
19. Waste Minimization and Solvent Recovery

Environmental and Regulatory Aspects

20. Historical Perspective
21. Pharmaceuticals in the Environment
22. Environmental Regulations

Synthesis of Sitagliptin, the Active Ingredient in Januvia and Janumet

23. First-Generation Route
24. Sitagliptin through Diastereoselective Hydrogenation of an Enamine. The PGA Enamine-Ester Route
25. The Triazole Fragment
26. Direct Preparation of Beta-Keto Amides
27. Second-Generation Chiral Auxiliary Route. The PGA Enamine-Amide Route
28. Prufication and Isolation of Sitagliptin (Pharmaceutical Form)
29. The Final Manufacturing Route

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

30. Biocatalysis
31. The Relevance of Statins
32. Biocatalytic Routes to Statin Side Chains
33. 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

34. Discovery and Early Development
35. From Extraction of Taxol from Pacific Yew Tree Bark to Semi-Synthetic Taxol
36. Taxol from Plant Cell Fermentation
37. Comparison of Semi-Synthetic versus PCF Taxol Processes: The Environmental Impact
38. Comparison of Semi-Synthetic versus PCF Taxol: Green Chemistry Principles

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

39. Process Routes to Pregabalin
40. Biocatalytic Route to Pregabalin
41. Green Chemistry Considerations

Green Processes for Peptide Mimetic Diabetic Drugs

42. Green Chemistry Considerations in Peptide-like API manufacture
43. Purification Process to Manufacture Amorphous API
44. Preparation of Unnatural Amino Acids

The Development of an Environmentally Sustainable Process for Radafaxine

45. Chemistry Process and the Dynamic Kinetic Resolution (DKR)
46. Multicolumn Chromatography: Development of Route 4
47. Environmental Assessment

Continuous Processing in the Pharmaceutical Industry

48. Continuous Production of a Key Intermediate for Atorvastatin
49. Continuous Process to Prepare Celecoxib
50. Continuous Oxidation of Alcohols to Aldehydes
51. Continuous Production of Bromonitromethane
52. Continuous Production and Use of Diazomehtane
53. A Snapshot of Some Further Continuous Processes Used in the Preparation of Pharmaceutical Agents

Preparataive and Industrial Scale Chromatography: Green and Integrated Processes

54. Basic Principles of Chromatography
55. Process Optimization to Reduce Eluent Consumption
56. Use of a Green Solvent: Supercritical Carbon Dioxide
57. Solvent Recycling Technologies
58. Application Examples
59. An Environmentally Friendly Solution for Each Separation

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

60. Integration of Chiral Amine Resolution and Racemization
61. Case StudiesM

Green Technologies in the Generic Pharmaceutical Industry

62. 'Waste': Definition and Remedy
63. Amidation
64. Synthesis of Galanthamine
65. Synthesis of Solefinacin
66. Synthesis of Levetiracetam
67. Synthesis of a Finasteride Intermediate
68. Bromination
69. Sulfoxidation in the Synthesis of Rabeprazole

Environmental Considerations in Biologics Manufacture

70. Therapeutic Biologics
71. Environmental Impact Considerations
72. Overall Comparison
73. Environmental Indices for Therapeutic Protein Manufacture
74. Technologies with Potential Environmental Impact
75. Single-Use Biologics Manufacture

Future Trends for Green Chemistry in the Pharmaceutical Industry

76. Waste Minimization in Drug Discovery
77. Greener Synthetic Methods in Primary Manufacturing
78. Alternative Solvents in the Pharmaceutical Industry
79. Green Chemistry in Secondary Pharmaceutical Operations
80. Global Cooperation in Green Chemistry

Index

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