Volume 14; Issue 1

Organic Process Research & Development

Volume 14; Issue 1

1

Process Development and Pilot-Scale Synthesis of New Cyclization Conditions of Substituted Phenylacetamides to Tetrahydroisoquinoline-2-ones Using Eaton’s Reagent

Ulysse, Luckner G., Yang, Qiang, McLaws, Mark D., Keefe, Daniel K., Guzzo, Peter R., Haney, Brian P.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 636 KB

english, 2010

2

Exploring the Scope for Scale-Up of Organic Chemistry Using a Large Batch Microwave Reactor

Schmink, Jason R., Kormos, Chad M., Devine, William G., Leadbeater, Nicholas E.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 1.83 MB

english, 2010

3

Investigation of Synthetic Routes to a Key Benzopyran Intermediate of a 5HT4 Agonist

Rassias, Geracimos, Stevenson, Neil G., Curtis, Neil R., Northall, John M., Gray, Matthew, Prodger, Jeremy C., Walker, Andrew J.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 309 KB

english, 2010

4

Routes for the Synthesis of (2S)-2-Methyltetrahydropyran-4-one from Simple Optically Pure Building Blocks

Anderson, Kevin R., Atkinson, Stéphanie L. G., Fujiwara, Takahiro, Giles, Melvyn E., Matsumoto, Takaji, Merifield, Eric, Singleton, John T., Saito, Takao, Sotoguchi, Tsukasa, Tornos, James A.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 460 KB

english, 2010

5

Synthesis of an Antibacterial Compound Containing a 1,4-Substituted 1H-1,2,3-Triazole: A Scaleable Alternative to the “Click” Reaction

Job, Gabriel E., Johnson, Graham, Lou, Rongliang, Martynow, Jacek G., Reeve, Maxwell M., Hanselmann, Roger

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 439 KB

english, 2010

6

Green Chemistry Articles of Interest to the Pharmaceutical Industry

Andrews, Ian, Cui, Jian, DaSilva, Jimmy, Dudin, Leo, Dunn, Peter, Hayler, John, Hinkley, Bill, Hughes, David, Kaptein, Bernard, Lorenz, Kurt

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 515 KB

english, 2010

7

Sonogashira Reactions with Propyne: Facile Synthesis of 4-Hydroxy-2-methylbenzofurans from Iodoresorcinols

Berliner, Martin A., Cordi, Eric M., Dunetz, Joshua R., Price, Kristin E.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 854 KB

english, 2010

8

Quaternary Chiral Center via Diastereoselective Enolate Amination Enables the Synthesis of an Anti-inflammatory Agent†

Magnus, Nicholas A., Campagna, Silvio, Confalone, Pat N., Savage, Scott, Meloni, David J., Waltermire, Robert E., Wethman, Robert G., Yates, Mathew

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 845 KB

english, 2010

9

Practical and Scalable Process for the Preparation of 4-Amino-1,3-dimethylpyrazole Hydrochloride

Graham, Stephen R., Brown, Peter J., Ford, J. Gair

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 106 KB

english, 2010

10

Practical Aspects of Carbon−Carbon Cross-Coupling Reactions Using Heteroarenes

Slagt, Vincent F., de Vries, André H. M., de Vries, Johannes G., Kellogg, Richard M.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 1.55 MB

english, 2010

11

Development of an Efficient Process Towards the Benzimidazole BYK308944: A Key Intermediate in the Synthesis of a Potassium-Competitive Acid Blocker

Webel, Matthias, Palmer, Andreas Marc, Scheufler, Christian, Haag, Dieter, Müller, Bernd

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 1.24 MB

english, 2010

12

Improved Synthesis of the Selective Rho-Kinase Inhibitor 6-Chloro- N 4-{3,5-difluoro-4-[(3-methyl-1 H -pyrrolo[2,3- b ]pyridin-4-yl)oxy]phenyl}pyrimidin-2,4-diamine

Schirok, Hartmut, Paulsen, Holger, Kroh, Walter, Chen, Gang, Gao, Ping

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 419 KB

english, 2010

13

Instantaneous, Facile and Selective Synthesis of Tetrabromobisphenol A using Potassium Tribromide: An Efficient and Renewable Brominating Agent

Kumar, Lalit, Sharma, Vivek, Mahajan, Tanu, Agarwal, D. D.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 157 KB

english, 2010

14

Understanding and Controlling the Formation of an Impurity during the Development of Muraglitazar, a PPAR Dual Agonist

Ye, Qingmei, Huang, Yande, Rusowicz, Andrew, Palaniswamy, Venkatapuram A., Raglione, Thomas V.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 230 KB

english, 2010

15

A Multidisciplinary Approach Toward the Rapid and Preparative-Scale Biocatalytic Synthesis of Chiral Amino Alcohols: A Concise Transketolase-/ω-Transaminase-Mediated Synthesis of (2 S ,3 S )-2-Aminopentane-1,3-diol

Smith, Mark E. B., Chen, Bing H., Hibbert, Edward G., Kaulmann, Ursula, Smithies, Kirsty, Galman, James L., Baganz, Frank, Dalby, Paul A., Hailes, Helen C., Lye, Gary J., Ward, John M., Woodley, John

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 400 KB

english, 2010

16

“Dark” Singlet Oxygenation of β-Citronellol: A Key Step in the Manufacture of Rose Oxide

Alsters, Paul L., Jary, Walther, Nardello-Rataj, Véronique, Aubry, Jean-Marie

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 323 KB

english, 2010

17

The Development of a New Manufacturing Route to the Novel Anticonvulsant, SB-406725A

Walker, Matthew D., Andrews, Benjamin I., Burton, Andrew J., Humphreys, Luke D., Kelly, Gary, Schilling, Mark B., Scott, Peter W.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 181 KB

english, 2010

18

Practical Application of Oxidation Using a Novel Na 2 WO 4 −H 2 O 2 System under Neutral Conditions for Scale-Up Manufacturing of 12α-Hydroxy-3-oxooleanano-28,13-lactone: Key Intermediate of Endothelin A Receptor Antagonist S-0139

Hida, Takemasa, Fukui, Yuuki, Kawata, Kyozo, Kabaki, Mikio, Masui, Toshiaki, Fumoto, Masataka, Nogusa, Hideo

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 3.11 MB

english, 2010

19

Industrial Oxidations with Organocatalyst TEMPO and Its Derivatives

Ciriminna, Rosaria, Pagliaro, Mario

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 532 KB

english, 2010

20

Comparison of Large-Scale Routes to Manufacture Chiral exo -2-Norbornyl Thiourea

Caille, Seb, Boni, Jerome, Cox, Geoffrey B., Faul, Margaret M., Franco, Pilar, Khattabi, Saab, Klingensmith, Liane M., Larrow, Jay F., Lee, James K., Martinelli, Michael J., Miller, Larry M., Moniz, G

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 1.55 MB

english, 2010

21

Development of a Biocatalytic Process as an Alternative to the (−)-DIP-Cl-Mediated Asymmetric Reduction of a Key Intermediate of Montelukast

Liang, Jack, Lalonde, James, Borup, Birthe, Mitchell, Vesna, Mundorff, Emily, Trinh, Na, Kochrekar, D. A., Nair Cherat, Ramachandran, Pai, G. Ganesh

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 822 KB

english, 2010

22

A Review of U.S. Patents in the Field of Organic Process Development Published During August and September 2009

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 683 KB

english, 2010

23

Translating High-Temperature Microwave Chemistry to Scalable Continuous Flow Processes

Damm, Markus, Glasnov, Toma N., Kappe, C. Oliver

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 154 KB

english, 2010

24

Hydrogen Peroxide Oxidation of Phosphite Triesters in Oligonucleotide Syntheses

Cvetovich, Raymond J.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 74 KB

english, 2010

25

Oxidation of Hexafluoropropylene with Oxygen to Hexafluoropropylene Oxide

Wróblewska, Agnieszka, Milchert, Eugeniusz, Meissner, Egbert

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 216 KB

english, 2010

26

Development of a Practical Biocatalytic Process for ( R )-2-Methylpentanol

Gooding, Owen W., Voladri, Rama, Bautista, Abigail, Hopkins, Thutam, Huisman, Gjalt, Jenne, Stephan, Ma, Steven, Mundorff, Emily C., Savile, Megan M., Truesdell, Susan J., Wong, John W.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 523 KB

english, 2010

27

An Improved Process for the Production of Lansoprazole: Investigation of Key Parameters That Influence the Water Content in Final API †

Gangula, Srinivas, Elati, Chandrasekhar R., Neredla, Anitha, Baddam, Sudhakar R., Neelam, Uday Kumar, Bandichhor, Rakeshwar, Dongamanti, Ashok

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 1.56 MB

english, 2010

28

Implementation of a High-Temperature Claisen Approach for Early Phase Delivery of a Benzopyran Derivative

Walker, Andrew J., Adolph, Sven, Connell, Richard B., Laue, Klaus, Roeder, Michael, Rueggeberg, Carsten J., Hahn, Dirk Uwe, Voegtli, Kurt, Watson, John

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 287 KB

english, 2010

29

Lipase-Catalyzed Polycondensation in Water: A New Approach for Polyester Synthesis

Duwensee, Julia, Wenda, Stefanie, Ruth, Wolfgang, Kragl, Udo

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 3.76 MB

english, 2010

30

A Practical and Efficient Synthesis of (3 R ,4 S )-1-Benzyl-4-phenylpyrrolidine-3-carboxylic acid via an Aziridinium Ion Intermediate

Ohigashi, Atsushi, Kikuchi, Takashi, Goto, Shunsuke

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 280 KB

english, 2010

31

Special Oxidation Chemistry Feature Section

Lathbury, David

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 31 KB

english, 2010

32

Efficient Production of Enantiomerically Pure Chiral Amines at Concentrations of 50 g/L Using Transaminases

Truppo, Matthew D., Rozzell, J. David, Turner, Nicholas J.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 377 KB

english, 2010

33

Development of an Extremely Efficient Oxidative Chlorination Reaction: The Value of Routine Data Collection

Barnwell, Neil, Cornwall, Philip, Horner, Daniel, Knott, Jason, Liddon, John

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 1.93 MB

english, 2010

34

Polymorphism - Still Unpredictable?

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 51 KB

english, 2010

35

Highly Enantioselective Reduction of a Small Heterocyclic Ketone: Biocatalytic Reduction of Tetrahydrothiophene-3-one to the Corresponding ( R )-Alcohol

Liang, Jack, Mundorff, Emily, Voladri, Rama, Jenne, Stephan, Gilson, Lynne, Conway, Aaron, Krebber, Anke, Wong, John, Huisman, Gjalt, Truesdell, Susan, Lalonde, James

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 219 KB

english, 2010

36

Some Items of Interest to Process R&D Chemists and Engineers

McLaughlin, Mark, Pfeiffer, Matthew, Tilstam, Ulf, Zlota, Andrei A., Laird, Trevor

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 288 KB

english, 2010

37

Straightforward Enzymatic Process Based on HNL CLEA-Catalysis towards Cyanohydrin Derivatives

Cabirol, Fabien L., Lim, Angela E. C., Hanefeld, Ulf, Sheldon, Roger A.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 603 KB

english, 2010

38

Optimisation of Permanganate Oxidation and Suzuki−Miyaura Coupling Steps in the Synthesis of a Na v 1.8 Sodium Channel Modulator

Fray, M. Jonathan, Gillmore, Adam T., Glossop, Melanie S., McManus, David J., Moses, Ian B., Praquin, Céline F.B., Reeves, Keith A., Thompson, Lisa R.

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 359 KB

english, 2010

39

Direct Oxidation of Cyclohexene with Inert Polymeric Membrane Reactor

Buonomenna, Maria G., Golemme, Giovanni, De Santo, Maria P., Drioli, Enrico

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 3.43 MB

english, 2010

40

Development of a Multikilogram Synthesis of a Chiral Epoxide Precursor to a CCR1 Antagonist. Use of in Situ Monitoring for Informed Optimisation via Fragile Intermediates

Ainge, Debra, Booker, James E. M., Pedge, Nicholas, Sinclair, Rhona, Sleigh, Chris, Štefinović, Marijan, Vaz, Luis-Manuel, Way, Edward

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 1016 KB

english, 2010

41

Book Review: Dynamic Stereochemistry of Chiral Compounds - Principles and Applications Dynamic Stereochemistry of Chiral Compounds - Principles and Applications . Edited by Christian Wolf . RSC Publishing : Cambridge, U.K. 2008 . 512 + xx pp. £49.95. ISBN 9780854042463 .

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 29 KB

english, 2010

42

Selection of a Purification Process for the Removal and Recycling of Cesium Catalyst after Polyol Production

Rodríguez, Juan F., Villajos, María Teresa, Devic, Anne Chloe, Ramos, María Jesús, Gabaldón, Ana María, de Lucas, Antonio

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 1.36 MB

english, 2010