Organic Process Research and Development Table of Contents: 2008, vol. 12, No. 6


Safety of Chemical Processes 08
Editorial

The Impact of Process Chemists and Engineers on Green Chemistry
NealG.  Anderson
1019-1020
Full: PDF (56 K)

Highlights from the Literature

Some Items of Interest to Process R&D Chemists and Engineers
Mark McLaughlinSilvina GarcíaRubioMatthew PfeifferUlf TilstamOctavio Augusto Ceva AntunesAndrei A. ZlotaTrevor Laird
1021-1030
Full: PDF (249 K)

Highlights from the Patents

A Review of U.S. Patents in the Field of Organic Process Development Published During June and July 2008
Keith Turner
1031-1040
Full: PDF (278 K)

Concept Article

Kepner-Tregoe Decision Analysis as a Tool to Aid Route Selection. Part 1
Jeremy S. Parker and Jonathan D. Moseley
1041-1043

Full: PDF (45 K)

Full Papers

Kepner-Tregoe Decision Analysis as a Tool To Aid Route Selection. Part 2. Application to AZD7545, a PDK Inhibitor
Jonathan D. Moseley, David Brown, Catherine R. Firkin, Shelley L. Jenkin, Bharti Patel and Evan W. Snape
1044-1059

Full: PDF (295 K)
Kepner-Tregoe Decision Analysis as a Tool To Aid Route Selection. Part 3. Application to a Back-Up Series of Compounds in the PDK Project
Jeremy S. Parker, John F. Bower, Paul M. Murray, Bharti Patel and Pere Talavera
1060-1077

Full: PDF (1635 K)
Scale-Up of Microwave-Promoted Reactions to the Multigram Level Using a Sealed-Vessel Microwave Apparatus
Matthew D. Bowman, Jason R. Schmink, Cynthia M. McGowan, Chad M. Kormos and Nicholas E. Leadbeater
1078-1088

Full: PDF (502 K)
Green Chemistry with a Novel 5.8-GHz Microwave Apparatus. Prompt One-Pot Solvent-Free Synthesis of a Major Ionic Liquid: The 1-Butyl-3-methylimidazolium Tetrafluoroborate System
Satoshi Horikoshi, Tomofumi Hamamura, Masatsugu Kajitani, Masahiro Yoshizawa-Fujita and Nick Serpone
1089-1093

Full: PDF (708 K)
Development of a Bulk Enabling Route to Maraviroc (UK-427,857), a CCR-5 Receptor Antagonist
Sarah J. Haycock-Lewandowski, Alexander Wilder and Jens Åhman
1094-1103

Full: PDF (197 K)
Process Research and Scale-up of a Commercialisable Route to Maraviroc (UK-427,857), a CCR-5 Receptor Antagonist
Jens Åhman, Melissa Birch, Sarah J. Haycock-Lewandowski, James, Long and Alexander Wilder
1104-1113

Full: PDF (963 K)
A Convergent Process for the Preparation of Adamantane 11-β-HSD-1 Inhibitors
Calvin L. Becker, Kenneth M. Engstrom, Francis A. Kerdesky, John C. Tolle, Seble H. Wagaw and Weifeng Wang
1114-1118

Full: PDF (103 K)
Enzymatic Preparation of a d-Amino Acid from a Racemic Amino Acid or Keto Acid
Ronald L. Hanson, Brian L. Davis, Steven L. Goldberg, Robert M. Johnston, William L. Parker, Thomas P. Tully, Michael A. Montana and Ramesh N. Patel
1119-1129

Full: PDF (182 K)
Practical Electrochemical Iodination of Aromatic Compounds
Kazuhide Kataoka, Yuji Hagiwara, Koji Midorikawa, Seiji Suga and Jun-ichi Yoshida
1130-1136

Full: PDF (680 K)
A Practical Synthesis of a Diazepinylbenzoic Acid, a Retinoid X Receptor Antagonist
Xinglong Jiang, George T. Lee, Kapa Prasad and Oljan Repič
1137-1141

Full: PDF (144 K)
Improved Process for the Preparation of 6-Chloro-5-(2-chloroethyl)oxindole
Durgesh V. Nadkarni and James F. Hallissey
1142-1145

Full: PDF (91 K)
Syntheses of a Triad of Flt3 Kinase Inhibitors: From Bench to Pilot Plant
Wen-Chung Shieh, Joe McKenna, Joseph A. Sclafani, Song Xue, Michael Girgis, James Vivelo, Branko Radetich and Kapa Prasad
1146-1155

Full: PDF (230 K)
Friedel−Crafts Benzoylation of Anisole in Ionic Liquids: Catalysis, Separation, and Recycle Studies
Christopher Hardacre, Paul Nancarrow, David W. Rooney and Jillian M. Thompson
1156-1163

Full: PDF (426 K)
A Practical Synthesis of a Chiral Analogue of FTY720
Xinglong Jiang, Baoqing Gong, Kapa Prasad and Oljan Repič
1164-1169

Full: PDF (132 K)
Large-Scale Asymmetric Synthesis of the 3,6,7,8-Tetrahydrochromeno[7,8-d]imidazole BYK 405879: A Promising Candidate for the Treatment of Acid-Related Diseases
Andreas M. Palmer, Matthias Webel, Christian Scheufler, Dieter Haag and Bernd Müller
1170-1182

Full: PDF (251 K)
Preparation of a HMG-CoA Reductase Inhibitor via an Optimized Imidazole-Forming Condensation Reaction
Daniel M. Bowles, Gary L. Bolton, David C. Boyles, Timothy T. Curran, Richard H. Hutchings, Scott D. Larsen, Jonathan M. Miller, William K. C. Park, Kurtis G. Ritsema, David C. Schineman and Markus Tamm
1183-1187

Full: PDF (120 K)
Synthesis of the NK1 Receptor Antagonist GW597599. Part 1: Development of a Scalable Route to a Key Chirally Pure Arylpiperazine
Giuseppe Guercio, Sergio Bacchi, Michael Goodyear, Antonella Carangio, Francesco Tinazzi and Stefano Curti
1188-1194

Full: PDF (793 K)
A Large Scale Process for the Preparation of Thymitaq
Håkan Malmgren, Birthe Bäckström, Ellen Sølver and Johan Wennerberg
1195-1200

Full: PDF (111 K)
A Rapid, Large-Scale Synthesis of a Potent Cholecystokinin (CCK) 1R Receptor Agonist
Jeffrey T. Kuethe, Karla G. Childers, Guy R. Humphrey, Michel Journet and Zhihui Peng
1201-1208

Full: PDF (178 K)
Removal of Soluble Palladium Complexes from Reaction Mixtures by Fixed-Bed Adsorption
Michael J. Girgis, Laura E. Kuczynski, Sonia M. Berberena, Caitlin A. Boyd, Pamela L. Kubinski, Megerle L. Scherholz, Donald E. Drinkwater, Xiaoxuan Shen, Stanislaw Babiak and Brian G. Lefebvre
1209-1217

Full: PDF (1359 K)
Scalable Reactor Design for Pharmaceuticals and Fine Chemicals Production. 3. A Novel Gas−Liquid Reactor for Catalytic Asymmetric Transfer Hydrogenation with Simultaneous Acetone Stripping
Xiuyan Sun and Asterios Gavriilidis
1218-1222

Full: PDF (1021 K)
Polymorphic Transformation of Pravastatin Sodium Monitored Using Combined Online FBRM and PVM
Chun-Yan Jia, Qiu-Xiang Yin, Mei-Jing Zhang, Jing-Kang Wang and Zhong-Hua Shen
1223-1228

Full: PDF (704 K)
Isolation, Synthesis, and Characterization of Impurities and Degradants from the Clofarabine Process
Bruce G. Anderson, William E. Bauta, William R. Cantrell, Jr., Tracy Engles and Dennis P. Lovett
1229-1237

Full: PDF (172 K)
Calcium Pantothenate. Part 3.(1) Process for the Biologically Active Enantiomer of the Same via Selective Crystallization and Racemization
Ludwik Synoradzki, Halina Hajmowicz, Jerzy Wisialski, Arkadiusz Mizerski and Tomasz Rowicki
1238-1244

Full: PDF (762 K)
Practical Synthesis of a HIV Integrase Inhibitor
Yong-Li Zhong, Brenda Pipik, Jaemoon Lee, Yoshinori Kohmura, Shigemitsu Okada, Kazunobu Igawa, Chie Kadowaki, Akihiro Takezawa, Shinji Kato, David A. Conlon, Hua Zhou, Anthony O. King, Robert A. Reamer, Donald R. Gauthier, Jr. and David Askin
1245-1252

Full: PDF (178 K)
Development of a Suitable Process for the Preparation of a TNF-α Converting Enzyme Inhibitor, WAY-281418
Youchu Wang, Maria Papamichelakis, Warren Chew, John Sellstedt, Razzak Noureldin, Sam Tadayon and Sylvain DaigneaultRocco J. Galante and Jerry Sun
1253-1260

Full: PDF (186 K)

Technical Notes

Practical Amination of Nitropyridones by Silylation
Robert A. Singer and Michaël Doré
1261-1264

Full: PDF (96 K)

Communications to the Editor

Mild and Selective Synthesis of an Aryl Boronic Ester by Equilibration of Mixtures of Boronic and Borinic Acid Derivatives
Vanessa F. Hawkins, Mark C. Wilkinson and Matthew Whiting
1265-1268

Full: PDF (88 K)
An Efficient Approach to 3-Bromo-6-chloro-phenanthrene-9,10-dione
John Limanto, Benjamin T. Dorner, Frederick W. Hartner and Lushi Tan
1269-1272

Full: PDF (94 K)
A Facile Two-Step Synthesis of 3-Fluoro-6-methoxyquinoline
Bryan Li, Zhijun Zhang and Michael Mangano
1273-1275

Full: PDF (80 K)

Editorial

Safety Special Issue
Trevor Laird
1276-1276
Full: PDF (31 K)
Safety Notables: Information from the Literature
Gerald A. WeisenburgerPaul F. Vogt
1277-1282
Full: PDF (76 K)

Letter to the Editor

SAFETY IS NO ACCIDENT!
Seemon Pines
1283-1284
Full: PDF (39 K)

Technical Notes

Diazidomethane Explosion
Raymond E. Conrow and W. Dennis Dean
1285-1286

Full: PDF (53 K)

Full Papers

Selection of the Proper Calorimetric Test Strategy in Reactive Chemicals Hazard Evaluation
David J. Frurip
1287-1292

Full: PDF (224 K)
A Practical Method For Stabilizing Lithiated Halogenated Aromatic Compounds
Thimma Rawalpally, Yaohui Ji, Ashish Shankar, William Edwards, Joshua Allen, Yong Jiang, Thomas P. Cleary and Michael E. Pierce
1293-1298

Full: PDF (767 K)
Measurement of Gas Flow Rates from Small-Scale Reactions
Gerald A. Weisenburger, Richard W. Barnhart and Gregory S. Steeno
1299-1304

Full: PDF (846 K)
Management of Change for Laboratories and Pilot Plants
Neal Langerman
1305-1306

Full: PDF (44 K)
A Catalyzed and Highly Selective Ester Reduction in the Synthesis of an N-Acylpyrrolidine: Safe Design through Reaction Calorimetry and Modeling
Roy C. Flanagan, Shiping Xie and Alan Millar
1307-1312

Full: PDF (1214 K)

Book Reviews

Book Review of Computational Organic Chemistry
Eddy M. E. Viseux
1313-1313
Full: PDF (54 K)
Book Review of Asymmetric Organic Synthesis with Enzymes

1313-1314
Full: PDF (54 K)
Book Review of Theilheimer’s Synthetic Methods of Organic Chemistry, Vol. 72

1314-1314
Full: PDF (54 K)
Book Review of The Management of Chemical Process Development in the Pharmaceutical Industry
John Knight
1314-1315
Full: PDF (54 K)
Book Review of Process Chemistry in the Pharmaceutical Industry, Vol. 2
W. J. Watson
1315-1315
Full: PDF (54 K)
Book Review of High-Throughput Analysis in the Pharmaceutical Industry

1315-1315
Full: PDF (54 K)
Book Review of Process Systems Engineering: Volumes 3 and 4: Supply Chain Optimization - parts I and II

1315-1315
Full: PDF (54 K)
Book Review of Pharmaceutical Pre-Approval Inspections: A Guide to Regulatory Success (Drugs and the Pharmaceutical Sciences, Vol. 181, 2nd ed.)
Derek Robinson
1316-1316
Full: PDF (54 K)