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Critical Assessment of Pharmaceutical ProcessesA Rationale for Changing the Synthetic Route

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Mike Butters,*^† David Catterick,*^‡ Andrew Craig,^‡ Alan Curzons,^‡ David Dale,^§ Adam Gillmore,*^§ Stuart P. Green,^§ Ivan Marziano,^§ Jon-Paul Sherlock,^† and Wesley White^†

AstraZeneca, Process R&D, Avlon/Charnwood, Avlon Works, Severn Road, Hallen, Bristol BS10 7ZE, U.K., GlaxoSmithKline, Synthetic Chemistry, Old Powder Mills, Tonbridge, Kent TN11 9AN, U.K., and Pfizer, Chemical R&D, PGR&D, Ramsgate Road, Sandwich, Kent CT13 9NJ, U.K.

Chem. Rev., 2006, 106 (7), pp 3002–3027

DOI: 10.1021/cr050982w

Publication Date (Web): March 8, 2006

Section:

Pharmaceuticals

1. Introduction
2. Criteria for Process Assessment
- 2.1. Safety Issues2.1.1. Potential Safety Issues and Their Significance
2.1.2. Prediction and Assessment of Safety Issues
2.1.3. Options To Manage Safety Issues
2.1.4. Designing a Safer New Route
- 2.2. Environmental Issues
2.2.1. Potential Environmental Issues and Their Significance
2.2.2. Prediction and Assessment of Environmental Issues
2.2.3. Options To Manage Environmental Issues
2.2.4. Designing a New “Greener” Route
- 2.3. Legal Issues
2.3.1. Potential Legal Issues and Their Significance
2.3.2. Prediction and Assessment of Legal Issues Associated with Regulated Substances
2.3.3. Prediction and Assessment of Legal Issues Associated with Patent Infringement
2.3.4. Options To Manage Patent Issues
2.3.5. Designing a New Route with Freedom To Operate
- 2.4. Economic Issues
2.4.1. Potential Economic Issues and Their Significance
2.4.2. Prediction and Assessment of Economic Issues
2.4.3. Options To Manage Economic Issues
2.4.4. Designing a Cost-Effective New Route
- 2.5. Control Issues
2.5.1. Potential Control Issues and Their Significance
2.5.2. Prediction and Assessment of Control Issues
2.5.3. Options To Manage Control Issues
2.5.4. Designing a New Route with Adequate Control Measures
- 2.6. Throughput Issues
2.6.1. Potential Throughput Issues and Their Significance
2.6.2. Prediction and Assessment of Throughput Issues
2.6.3. Options To Manage Throughput Issues
2.6.4. Designing a New Route with High Throughput
3. Interrelationships between Process Issues
4. Conclusions
5. Acknowledgments
6. References

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