EDITORIAL
| Continuous Processes in Small-Scale Manufacture Trevor Laird 927-927 |
| Full: PDF (45 K) |
HIGHLIGHTS FROM THE LITERATURE
| Some Items of Interest to Process R&D Chemists and Engineers Mark McLaughlin, Silvina García Rubio, Matthew Pfeiffer, Ulf Tilstam, Octavio Augusto Ceva Antunes, Trevor Laird*, Ganapati D. Yadav, and Andrei A. Zlota 928-939 |
| Full: PDF (273 K) |
HIGHLIGHTS FROM THE PATENTS
| A Review of U.S. Patents in the Field of Organic Process Development Published During June and July 2007 Keith Turner 940-950 |
| Full: PDF (318 K) |
FULL PAPERS
| Syntheses of 4,5-Disubstituted Oxazoles via Regioselective C-4 Bromination Bryan Li, Richard A. Buzon, and Zhijun Zhang 951-955  |
| Full: PDF (101 K) |
| Applicability of a Fiber-Supported Catalyst on a Buchwald–Hartwig Amination Reaction Henrik Christensen, Søren Kiil, Kim Dam-Johansen, and Ole Nielsen 956-965  |
| Full: PDF (586 K) |
| Scalable Reactor Design for Pharmaceuticals and Fine Chemicals Production. 2: Evaluation of Potential Scale-up Obstacles for Asymmetric Transfer Hydrogenation M. Zanfir and A. Gavriilidis 966-971  |
| Full: PDF (360 K) |
| Research and Development of an Efficient Synthesis of Hexahydrofuro[2,3-b]furan-3-ol Moiety—A Key Component of the HIV Protease Inhibitor Candidates Richard H. Yu, Richard P. Polniaszek, Mark W. Becker, Charles M. Cook, and Lok Him L. Yu 972-980  |
| Full: PDF (607 K) |
| pH Control in Aqueous Processes: N-4-Methylsulfonylphenylguanidine Lai C. Chan, Brian G. Cox, Angela Currie, James Muir, and Simon D. Yates 981-984  |
| Full: PDF (381 K) |
| The Synthesis of a 5HT2C Receptor Agonist Lindsay A. Hobson, William A. Nugent, Stephen R. Anderson, Subodh S. Deshmukh, James J. Haley III, Pingli Liu, Nicholas A. Magnus, Patrick Sheeran, James P. Sherbine, Benjamin R. P. Stone, and Jiang Zhu 985-995  |
| Full: PDF (200 K) |
| Development of a Scaleable Synthesis for 1,2-Bis(2-aminophenylthio)ethane (APO-Link) Used in the Production of Bismaleimide Resin Crystal G. Densmore, Hilary Wheeler, Rebecca Cohenour, Thomas W. Robison, Dawud Hasam, Blossom J. Cordova, Peter C. Stark, Edward N. Fuller, Charles J. Cook, and Holly A. Weber 996-1003  |
| Full: PDF (155 K) |
| An Expedient and Multikilogram Synthesis of a Naphthalenoid H3 Antagonist Yu-Ming Pu, Yi-Yin Ku, Timothy Grieme, Lawrence A. Black, Ashok V. Bhatia, and Marlon Cowart 1004-1009  |
| Full: PDF (206 K) |
| Synthesis of a 5-((Aryloxy)methyl)-3-(4-(trifluoromethyl)phenyl)[1,2,4]thiadiazole Derivative: A Promising PPARα,δ Agonist Michael Reuman, Zhiyong Hu, Gee-Hong Kuo, Xun Li, Ronald K. Russell, Lan Shen, Scott Youells, and Yongzheng Zhang 1010-1014  |
| Full: PDF (122 K) |
| Process Research and Development of an NK-1 Receptor Antagonist. Enantioselective Trifluoromethyl Addition to a Ketone in the Preparation of a Chiral Isochroman Stéphane Caron, Nga M. Do, Janice E. Sieser, Patrice Arpin, and Enrique Vazquez 1015-1024  |
| Full: PDF (226 K) |
| Ozonolysis of Acetic Acid 1-Vinyl-hexyl Ester in a Falling Film Microreactor Norbert Steinfeldt, Radwan Abdallah, Uwe Dingerdissen, and Klaus Jähnisch 1025-1031  |
| Full: PDF (226 K) |
| Development of a Scalable Synthesis of GSK183390A, a PPAR α/γ Agonist Lynette M. Oh, Huan Wang, Susan C. Shilcrat, Robert E. Herrmann, Daniel B. Patience, P. Grant Spoors, and Joseph Sisko 1032-1042  |
| Full: PDF (1004 K) |
| A Practical Synthesis of Enantiopure 7-Alkoxy-4-aryl-tetrahydroisoquinoline, a Dual Serotonin Reuptake Inhibitor/Histamine H3 Antagonist Xiaohu Deng, Jimmy T. Liang, Jing Liu, Heather McAllister, Carsten Schubert, and Neelakandha S. Mani 1043-1050  |
| Full: PDF (332 K) |
| A Scalable Process for the Synthesis of the Bcl Inhibitor Obatoclax Kenza Daïri, Yuxing Yao, Michael Faley, Sasmita Tripathy, Elise Rioux, Xavier Billot, Daniel Rabouin, Gerson Gonzalez, Jean-François Lavallée, and Giorgio Attardo 1051-1054  |
| Full: PDF (87 K) |
| Development of HIV-Integrase Inhibitor S-1360: Selection of the Protecting Group on the 1,2,4-Triazole Ring Sumio Shimizu, Takeshi Endo, Kenji Izumi, and Hidenori Mikamiyama 1055-1058  |
| Full: PDF (99 K) |
| One-Step Synthesis of 5-(4-Fluorobenzyl)-2-furyl Methyl Ketone: A Key Intermediate of HIV-Integrase Inhibitor S-1360 Kenji Izumi, Mikio Kabaki, Masaaki Uenaka, and Sumio Shimizu 1059-1061  |
| Full: PDF (72 K) |
| Discovery of the Decarboxylative Blaise Reaction and Its Application to the Efficient Synthesis of Ethyl 2,6-Dichloro-5-fluoronicotinoylacetate Jae Hoon Lee, Bo Seung Choi, Jay Hyok Chang, Sam Sik Kim, and Hyunik Shin 1062-1064  |
| Full: PDF (81 K) |
| Boric Acid Catalyzed Amidation in the Synthesis of Active Pharmaceutical Ingredients Ravi Kumar Mylavarapu, Kondaiah GCM, Naveenkumar Kolla, Raju Veeramalla, Purandhar Koilkonda, Apurba Bhattacharya, and Rakeshwar Bandichhor 1065-1068  |
| Full: PDF (89 K) |
| Optimized Synthesis of L-m-Tyrosine Suitable for Chemical Scale-Up Cara E. Humphrey, Markus Furegati, Kurt Laumen, Luigi La Vecchia, Thomas Leutert, J. Constanze D. Müller-Hartwieg, and Markus Vögtle 1069-1075  |
| Full: PDF (140 K) |
TECHNICAL NOTES
| Efficient Multikilogram Synthesis of 5-Bromo-2-cyclopropyl-1-methyl-1H-imidazole Rogelio P. Frutos, Sonia Rodríguez, Nitinchandra Patel, Joe Johnson, Anjan Saha, Dhileepkumar Krishnamurthy, and Chris H. Senanayake 1076-1078  |
| Full: PDF (73 K) |
| Process Development of the Synthetic Route to R116301 Michel Guillaume, Jef Cuypers, and Jul Dingenen 1079-1086  |
| Full: PDF (201 K) |
SPECIAL FEATURE SECTION: SAFETY OF CHEMICAL PROCESSES
SAFETY HIGHLIGHTS
| Safety Notables: Information from the Literature Gerald A. Weisenburger and Paul F. Vogt 1087-1090 |
| Full: PDF (67 K) |
CONCEPT ARTICLE
| How We Changed the Safety Culture Trevor A. Kletz 1091-1095  |
| Full: PDF (75 K) |
FULL PAPERS
| Explosion and Decomposition Characteristics of Hydrazoic Acid in the Gas Phase Jacques Wiss, Christian Fleury, Christoph Heuberger, Ulrich Onken, and Martin Glor 1096-1103  |
| Full: PDF (1907 K) |
| Development of a Scalable Process for the Synthesis of trans-2-Methylcyclopropanecarboxylic Acid Laurent Delhaye, Christophe Stevens, Alain Merschaert, Pieter Delbeke, Willy Briône, Ulf Tilstam, Alfio Borghese, Geoffroy Geldhof, Khalid Diker, Aurélie Dubois, Mario Barberis, and Luis Casarubios 1104-1111  |
| Full: PDF (2712 K) |
| Determination of Reaction Heat: A Comparison of Measurement and Estimation Techniques Gerald A. Weisenburger, Richard W. Barnhart, Jerry D. Clark, David J. Dale, Mike Hawksworth, Paul D. Higginson, Ying Kang, Donald J. Knoechel, Brian S. Moon, Stephen M. Shaw, Geraldine P. Taber, and Derek L. Tickner 1112-1125  |
| Full: PDF (1644 K) |
| Safety Aspects of a Cyanamide Reaction: Inherent Safe Design through Kinetic Modelling and Adiabatic Testing Wim Dermaut, Christine Fannes, and Johan Van Thienen 1126-1130  |
| Full: PDF (622 K) |
COMMUNICATIONS TO THE EDITOR
| Safety Evaluation of an Unexpected Incident with a Nitro Compound Rafael Barbas, Manuel Botija, Helena Camps, Anna Portell, Rafel Prohens, and Cristina Puigjaner 1131-1134  |
| Full: PDF (808 K) |
TECHNICAL NOTES
| Improvement of Process Safety and Efficiency of Grignard Reactions by Real-Time Monitoring Holger Kryk, Günther Hessel, and Wilfried Schmitt 1135-1140  |
| Full: PDF (932 K) |
| Cyclopentadiene: The Impact of Storage Conditions on Thermal Stability David J. am Ende, David C. Whritenour, and Jotham W. Coe 1141-1146  |
| Full: PDF (259 K) |
BOOK REVIEWS
| Analysis of Drug Impurities. R. J. Smith and M. L. Webb, Eds. Blackwell Publishing: Oxford. 2007. 275 + ix pp. £99.50. ISBN 1-4051-3358-6. 1147-1147 |
| Full: PDF (61 K) |
| Fine Chemicals–The Industry and the Business. By Peter Pollak. Wiley Interscience: Hoboken, NJ. 2007. 234 + xiii pp. £55.95. ISBN 978-0-470-05075-0. 1147-1148 |
| Full: PDF (61 K) |
| Methods and Reagents for Green Chemistry–An Introduction. P. Tundo, A. Perosa, F. Zecchini, Eds. Wiley Interscience: New York. 2007. 314 pp. £55.95. ISBN 978-0-471-75400-8. 1148-1149 |
| Full: PDF (61 K) |
| Boronic Acids. Hall, D. G., Ed. Wiley-VCH: Weinheim. 2005. 549 + xxv pages. EUR159. ISBN 978-3-527-30991-8. 1149-1149 |
| Full: PDF (61 K) |
| Encyclopedic Dictionary of Named Processes in Chemical Technology, 3rd ed. By Alan E. Comyns. CRC Press/Taylor and Francis: Boca Raton. 2007. £85. ISBN 978-0-8493-9163-7. 1149-1150 |
| Full: PDF (61 K) |
| Chirality in Drug Research, Volume 33. E. Francotte and W. Lindner, Eds. Wiley-VCH: Weinheim. 2006. 351 + xix pp. EUR139. ISBN 3-527-31076-2. 1150-1150 |
| Full: PDF (61 K) |
| Kirk-Othmer Concise Encyclopedia of Chemical Technology (2 Volumes), 5th ed. Wiley-Interscience: West Sussex, U.K. 2007. 2711 + xxv pages. £208. ISBN 978-0-470-04748-4. 1150-1150 |
| Full: PDF (61 K) |
| Organic Reactions in Water: Principles, Strategies and Applications. U. Marcus Lindström, Ed. Blackwell: London. 2007. 405 + xv pages. £99.50. ISBN 978-1-4051-3890-1. 1150-1151 |
| Full: PDF (61 K) |
| Catalysts for Fine Chemical Synthesis, Volume 5: Regio- and Stereo-Controlled Oxidations and Reductions. Stanley M. Roberts and John Whittall, Eds. Wiley: West Sussex, U.K. 2007. 312 + xxii pages. £100. ISBN 978-0-470-09022-0. 1151-1151 |
| Full: PDF (61 K) |
| Systematic Nomenclature of Organic, Organometallic and Coordination Chemistry. Ursula Bünzli-Trepp, Ed. CRC Press, Taylor and Francis Group: London, 2007. 636 + ix pages. £99. ISBN 978-1-4200-4615-1. 1151-1151 |
| Full: PDF (61 K) |