Table of Contents

January 2003
Volume 7, Issue 1
Pages 1-122

Editorial

May Organic Process Research & Development Keep Growing!

p 1
Publication Date (Web): December 19, 2002 (Editorial)
DOI: 10.1021/op025614y

Highlights From The Literature

Trevor LairdStephen A. HermitageUlf Tilstam
pp 2–9
Publication Date (Web): December 31, 2002 (Editorial)
DOI: 10.1021/op0256136

Articles

Process Design and Scale-Up of the Synthesis of 2,2‘:5‘,2‘ ‘-Terthienyl

B. J. J. Smeets, R. H. Meijer, J. Meuldijk, J. A. J. M. Vekemans, and L. A. Hulshof*
pp 10–16
Publication Date (Web): November 05, 2002 (Article)
DOI: 10.1021/op020044n

O-Methylation of Dihydroxybenzenes with Methanol in the Vapour Phase over Alkali-Loaded SiO2 Catalysts:  A Kinetic Analysis

Rajaram Bal, S. Mayadevi,* and S. Sivasanker
pp 17–21
Publication Date (Web): November 01, 2002 (Article)
DOI: 10.1021/op020054o

An Improved Process for the N-Alkylation of Indoles Using Chiral N-Protected 2-Methylaziridines

Paul R. Giles,* Mark Rogers-Evans, Milan Soukup, and John Knight
pp 22–24
Publication Date (Web): November 14, 2002 (Article)
DOI: 10.1021/op020078v

Trifluoroacetic Acid-Mediated Cleavage of a Triethylsilyl Protecting Group:  Application in the Final Step of the Semisynthetic Route to Paclitaxel (Taxol)

Ambarish K. Singh,* Raymond E. Weaver, Gerald L. Powers, Victor W. Rosso, Chenkou Wei, David A. Lust, Atul S. Kotnis, F. Taha Comezoglu, Mark Liu, Kenneth S. Bembenek, Bich D. Phan, Dale J. Vanyo, Merrill L. Davies, Rachel Mathew, Venkatapuram A. Palaniswamy, Wen-Sen Li, Kumar Gadamsetti, Ciro J. Spagnuolo, and William J. Winter
pp 25–27
Publication Date (Web): November 05, 2002 (Article)
DOI: 10.1021/op020221k

Rapid, Continuous Solution-Phase Peptide Synthesis:  Application to Peptides of Pharmaceutical Interest

Louis A. Carpino,* Shahnaz Ghassemi, Dumitru Ionescu, Mohamed Ismail, Dean Sadat-Aalaee,§ George A. Truran, E. M. E. Mansour, Gary A. Siwruk,§ John S. Eynon,§ and Barry Morgan§
pp 28–37
Publication Date (Web): December 10, 2002 (Article)
DOI: 10.1021/op0202179

The Development of a Practical and Reliable Large-Scale Synthesis of 2,6-Diamino-4-bromopyridine

Matthias Nettekoven* and Christian Jenny§
pp 38–43
Publication Date (Web): December 03, 2002 (Article)
DOI: 10.1021/op020085j

Heterogeneous Rh/C-Catalyzed Direct Reductive Coupling of Haloaryls to Biaryls in Water

Sudip Mukhopadhyay,* Ashutosh V. Joshi, Liat Peleg, and Yoel Sasson*
pp 44–46
Publication Date (Web): January 03, 2003 (Article)
DOI: 10.1021/op020080m

Controlled Detritylation of Antisense Oligonucleotides

Achim H. Krotz,* Bethany McElroy, Anthony N. Scozzari, Douglas L. Cole, and Vasulinga T. Ravikumar
pp 47–52
Publication Date (Web): January 01, 2003 (Article)
DOI: 10.1021/op020068u

A New Approach to Rapid Parallel Development for Four Neurokinin Antagonists. Part 1.

Jonathan D. Moseley* and William O. Moss
pp 53–57
Publication Date (Web): December 17, 2002 (Article)
DOI: 10.1021/op020064p

A New Approach to Rapid Parallel Development of Four Neurokinin Antagonists. Part 2. Synthesis of ZD6021 Cyano Acid

Jonathan D. Moseley,* William O. Moss, Matthew J. Welham, Claire L. Ancell, John Banister, Sharon A. Bowden, Glenn Norton, and Maureen J. Young
pp 58–66
Publication Date (Web): December 17, 2002 (Article)
DOI: 10.1021/op020065h

A New Approach to the Rapid Parallel Development of Four Neurokinin Antagonists. Part 3. Assembly of Neurokinin Antagonists

Jeremy S. Parker,* Sharon A. Bowden, Catherine R. Firkin, Jonathan D. Moseley, Paul M. Murray, Matthew J. Welham, Richard Wisedale, Maureen J. Young, and William O. Moss
pp 67–73
Publication Date (Web): December 17, 2002 (Article)
DOI: 10.1021/op020066+

A New Route for Manufacture of 3-Cyano-1-naphthalenecarboxylic Acid

I. W. Ashworth, M. C. Bowden, B. Dembofsky, D. Levin,* W. Moss,§ E. Robinson, N. Szczur, and J. Virica
pp 74–81
Publication Date (Web): December 17, 2002 (Technology Report)
DOI: 10.1021/op025571l

Lecture Transcripts

Process Development on the Enantioselective Enzymatic Hydrolysis of S-Ethyl 2-Ethoxy-3-(4-hydroxyphenyl)propanoate

Heinz-Josef Deussen,* Magali Zundel, Marine Valdois, Søren Vig Lehmann, Volker Weil, Carsten Mailand Hjort, Peter Rahbek Østergaard, Erik Marcussen, and Søren Ebdrup
pp 82–88
Publication Date (Web): December 13, 2002 (Summary of Lecture Transcript)
DOI: 10.1021/op0256035

Technical Notes

Industrially Viable Syntheses of Highly Enantiomerically Enriched 1-Aryl Alcohols via Asymmetric Hydrogenation

David Chaplin, Paul Harrison, Julian P. Henschke, Ian C. Lennon, Graham Meek, Paul Moran, Christopher J. Pilkington, James A. Ramsden,* Simon Watkins, and Antonio Zanotti-Gerosa
pp 89–94
Publication Date (Web): December 10, 2002 (Technical Note)
DOI: 10.1021/op025585r

Nitration of Phenol and Substituted Phenols with Dilute Nitric Acid Using Phase-Transfer Catalysts

Ashutosh V. Joshi, Mubeen Baidoosi, Sudip Mukhopadhyay, and Yoel Sasson*
pp 95–97
Publication Date (Web): December 11, 2002 (Technical Note)
DOI: 10.1021/op0200120

A Facile Synthesis of 1,4-Dialkoxy-2,5-diiodobenzenes:  Reaction of Dialkoxybenzenes with Iodine Monochloride in Alcoholic Solvents

Koji Wariishi, Sin-ichi Morishima, and Yoshio Inagaki*
pp 98–100
Publication Date (Web): December 07, 2002 (Technical Note)
DOI: 10.1021/op025566h

Technology Reports

A Practical Synthesis of the PDE4 Inhibitor, SB-207499, from a Cyclohexanone Precursor

Neil F. Badham,* Jian-Hao Chen, Paul G. Cummings, Philip C. Dell'Orco,§ Ann M. Diederich, Ann M. Eldridge, Wilford L. Mendelson, Robert J. Mills, Vance J. Novack, Mark A. Olsen, Abu M. Rustum, Kevin S. Webb, and Shawn Yang
pp 101–108
Publication Date (Web): October 30, 2002 (Technology Report)
DOI: 10.1021/op025584z

Solid/Liquid Palladium-Catalyzed Coupling of Haloaryls Using Alcohols as Reducing Agents:  Kinetics and Process Optimization

Diana Gitis, Sudip Mukhopadhyay, Gadi Rothenberg,§ and Yoel Sasson*
pp 109–114
Publication Date (Web): December 19, 2002 (Technology Report)
DOI: 10.1021/op015519+

Development of a Scaleable Route for the Production of cis-N-Benzyl-3-methylamino-4-methylpiperidine

David H. Brown Ripin,* Stefan Abele, Weiling Cai, Todd Blumenkopf,§ Jeffrey M. Casavant,§ Jonathan L. Doty,§ Mark Flanagan,§ Christian Koecher, Klaus W. Laue, Keith McCarthy, Cliff Meltz, Mike Munchhoff,§ Kees Pouwer, Bharat Shah, Jianmin Sun,§ John Teixeira, Ton Vries, David A. Whipple,§ and Glenn Wilcox
pp 115–120
Publication Date (Web): December 02, 2002 (Technology Report)
DOI: 10.1021/op025599x

Book Reviews

Advanced Drying Technologies By T. Kudra and A. S. Mujumdar. Marcel Dekker:  New York. 2002. 459 pp. $175.00. ISBN 0-8247-9618-7.

Kees van 't Land
pp 121–122
Publication Date (Web): December 04, 2002 (Book Review)
DOI: 10.1021/op010102p

Additions & Corrections

A New Route for the Preparation of 5-Hydroxyisophthalic Acid

Mark Gelmont, Oded Arad, and Jakob Oren
p 121
Publication Date (Web): November 20, 2002 (Addition/Correction)
DOI: 10.1021/op0200930