Volume 13; Issue 6

Organic Process Research & Development

Volume 13; Issue 6

1

Short and Efficient Process for the Synthesis of trans-4-Aminocyclohexanecarboxylic Acid Derivatives

Patil, Pankaj S., Mahajan, Ulhas S., Sonawane, Swapnil P., Gurjar, Mukund K.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 176 KB

english, 2009

2

Preparation and Characterization of Theophylline−Nicotinamide Cocrystal

Lu, Jie, Rohani, Sohrab

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 4.35 MB

english, 2009

3

Preparation of Saxagliptin, a Novel DPP-IV Inhibitor

Savage, Scott A., Jones, Gregory S., Kolotuchin, Sergei, Ramrattan, Shelly Ann, Vu, Truc, Waltermire, Robert E.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 279 KB

english, 2009

4

An Improved Synthetic Route for Preparative Process of Vardenafil

Tian, Guanghui, Liu, Zheng, Mao, Yongjun, Shen, Jingkang, Shen, Jingshan

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 213 KB

english, 2009

5

Polymorphism in Processes of Crystallization in Solution: A Practical Review

Mangin, Denis, Puel, Francois, Veesler, Stephane

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 3.01 MB

english, 2009

6

The Solubility of Beclomethasone-17,21-dipropionate in Selected Organic Solvents: Experimental Measurement and Thermodynamic Modeling

Bakhbakhi, Yousef, Charpentier, Paul, Rohani, Sohrab

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 150 KB

english, 2009

7

A Novel Chiral Resolving Reagent, Bis(( S )-Mandelic acid)-3-nitrophthalate, for Amlodipine Racemate Resolution: Scalable Synthesis and Resolution Process

Lee, Hong Woo, Shin, Sung Jae, Yu, Hosung, Kang, Sung Kwon, Yoo, Choong Leol

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 172 KB

english, 2009

8

New and Improved Manufacturing Process for Valsartan

.N, Senthil Kumar, Reddy, Shankar B., Sinha, Brajesh Kumar, Mukkanti, Kagga, Dandala, Ramesh

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 427 KB

english, 2009

9

Particle Engineering Strategies via Crystallization for Pulmonary Drug Delivery

Ragab, Doaa M., Rohani, Sohrab

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 1.86 MB

english, 2009

10

Evaluation and Establishment of a Cleaning Protocol for the Production of Vanisal Sodium and Aspirin Using a Continuous Oscillatory Baffled Reactor

Ricardo, Caldeira, Xiongwei, Ni

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 3.19 MB

english, 2009

11

A Scalable Zinc Activation Procedure Using DIBAL-H in a Reformatsky Reaction

Girgis, Michael J., Liang, Jessica K., Du, Zhengming, Slade, Joel, Prasad, Kapa

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 1.62 MB

english, 2009

12

Formation of 2-Trifluoromethylphenyl Grignard Reagent via Magnesium−Halogen Exchange: Process Safety Evaluation and Concentration Effect

Tang, Wenjun, Sarvestani, Max, Wei, Xudong, Nummy, Laurence J., Patel, Nitinchandra, Narayanan, Bikshandarkoil, Byrne, Denis, Lee, Heewon, Yee, Nathan K., Senanayake, Chris H.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 1.41 MB

english, 2009

13

An Improved Process for Pioglitazone and Its Pharmaceutically Acceptable Salt †

Madivada, Lokeswara Rao, Anumala, Raghupathi Reddy, Gilla, Goverdhan, Alla, Sampath, Charagondla, Kavitha, Kagga, Mukkanti, Bhattacharya, Apurba, Bandichhor, Rakeshwar

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 183 KB

english, 2009

14

A Practical Solid Form Screen Approach To Identify a Pharmaceutical Glutaric Acid Cocrystal for Development

Li, Zhibin, Yang, Bing-Shiou, Jiang, Mo, Eriksson, Magnus, Spinelli, Earl, Yee, Nathan, Senanayake, Chris

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 1.50 MB

english, 2009

15

Synthesis of the NK1 Receptor Antagonist GW597599. Part 3: Development of a Scalable Route to a Key Chirally Pure Arylpiperazine Urea, A Happy End

Guercio, Giuseppe, Bacchi, Sergio, Perboni, Alcide, Leroi, Corinne, Tinazzi, Francesco, Bientinesi, Ilaria, Hourdin, Marie, Goodyear, Michael, Curti, Stefano, Provera, Stefano, Cimarosti, Zadeo

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 667 KB

english, 2009

16

Turning DSC Charts of Polymorphs into Phase Diagrams: A Tutorial Paper †

Threlfall, Terence L.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 1.75 MB

english, 2009

17

The Challenges of Developing an API Crystallization Process for a Complex Polymorphic and Highly Solvating System. Part I

Chekal, Brian P., Campeta, Anthony M., Abramov, Yuriy A., Feeder, Neil, Glynn, Paul P., McLaughlin, Robert W., Meenan, Paul A., Singer, Robert A.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 2.40 MB

english, 2009

18

Crystallisation from Water-in-Oil Emulsions As a Route to Spherical Particulates: Glycine and the Hydrochloride Salts of Glutamic Acid and Ephedrine

Chadwick, K., Davey, R. J., Mughal, R., Marziano, I.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 6.08 MB

english, 2009

19

Attrition-Enhanced Deracemization in the Synthesis of Clopidogrel - A Practical Application of a New Discovery

van der Meijden, Maarten W., Leeman, Michel, Gelens, Edith, Noorduin, Wim L., Meekes, Hugo, van Enckevort, Willem J. P., Kaptein, Bernard, Vlieg, Elias, Kellogg, Richard M.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 121 KB

english, 2009

20

Scalable Process for the Premix of Esomeprazole †

Reddy, Lekkala Amarnath, Malakondaiah, Golla China, Reddy, Alieti Sanjay, Bhaskar, Boluguddu Vijaya, Himabindu, Vurimidi, Bhattacharya, Apurba, Bandichhor, Rakeshwar

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 95 KB

english, 2009

21

Efficient Synthesis of 1,4-Diaryl-5-methyl-1,2,3-triazole, A Potential mGluR1 Antagonist, and the Risk Assessment Study of Arylazides

Tsuritani, Takayuki, Mizuno, Hiroo, Nonoyama, Nobuaki, Kii, Satoshi, Akao, Atsushi, Sato, Kimihiko, Yasuda, Nobuyoshi, Mase, Toshiaki

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 365 KB

english, 2009

22

Process Development and Scale Up of a Glycine Antagonist

Banks, Adam, Breen, Gary F., Caine, Darren, Carey, John S., Drake, Christopher, Forth, Michael A., Gladwin, Asa, Guelfi, Simone, Hayes, Jerome F., Maragni, Paolo, Morgan, David O., Oxley, Paul, Perbon

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 427 KB

english, 2009

23

Development of a Scalable Synthetic Process for DG-051B, A First-in-Class Inhibitior of LTA4H

Enache, Livia A., Kennedy, Isaac, Sullins, David W., Chen, Wei, Ristic, Dragan, Stahl, Glenn L., Dzekhtser, Sergey, Erickson, Robert A., Yan, Changren, Muellner, Frank W., Krohn, Michael D., Winger, J

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 374 KB

english, 2009

24

Removal of Heavy Metals from Organic Reaction Mixtures: Preparation and Application of Functionalized Resins(1)

Barbaras, Damien, Brozio, Jörg, Johannsen, Ib, Allmendinger, Thomas

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 1.48 MB

english, 2009

25

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

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 1.33 MB

english, 2009

26

A Low-Waste Process To Sertraline By Diastereomeric Crystal Resolution and Waste Isomer Racemisation

Blacker, A. John, Brown, Stuart, Clique, Blandine, Gourlay, Brian, Headley, Catherine E., Ingham, Stephen, Ritson, Dougal, Screen, Thomas, Stirling, Matthew J., Taylor, David, Thompson, Gary

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 531 KB

english, 2009

27

Why Do Organic Compounds Crystallise Well or Badly or Ever so Slowly? Why Is Crystallisation Nevertheless Such a Good Purification Technique? †

Hursthouse, Michael B., Huth, L. Susanne, Threlfall, Terence L.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 2.19 MB

english, 2009

28

A Convenient and Stable Synthon for Ethyl Azide and Its Evaluation in a [3 + 2]-Cycloaddition Reaction under Continuous-Flow Conditions

Tinder, Rob, Farr, Roger, Heid, Richard, Zhao, Ralph, Rarig, Randy S., Storz, Thomas

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 3.38 MB

english, 2009

29

Development of Manufacturing Processes for a New Family of 2,6-Dihaloaryl 1,2,4-Triazole Insecticides

Hull, John W., Romer, Duane R., Adaway, Timothy J., Podhorez, David E.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 147 KB

english, 2009

30

A Practical Approach for Using Solubility to Design Cooling Crystallisations

Muller, Frans L., Fielding, Mark, Black, Simon

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 234 KB

english, 2009

31

Practical Diastereoselective Synthesis and Scale-up Study of (+)-2-((1 R ,2 R ,3 R ,5 S )-2-Amino-6,6-dimethylbicyclo[3.1.1]hept-3-yl)ethanol: A Key Intermediate of the Novel Prostaglandin D 2 Receptor Antagonist S-5751

Hida, Takemasa, Mitsumori, Susumu, Honma, Tsunetoshi, Hiramatsu, Yoshiharu, Hashizume, Hiroshi, Okada, Tetsuo, Kakinuma, Makoto, Kawata, Kyozo, Oda, Katsuo, Hasegawa, Aiko, Masui, Toshiaki, Nogusa, Hi

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 243 KB

english, 2009

32

A Novel Crystallization Methodology To Ensure Isolation of the Most Stable Crystal Form

Cote, Aaron, Zhou, George, Stanik, Mary

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 2.03 MB

english, 2009

33

Practical Enantioselective Synthesis of a 3-Aryl-3-trifluoromethyl-2-aminopropanol Derivative

Alimardanov, Asaf, Nikitenko, Antonia, Connolly, Terrence J., Feigelson, Gregg, Chan, Anita W., Ding, Zhixian, Ghosh, Mousumi, Shi, Xinxu, Ren, Jianxin, Hansen, Eric, Farr, Roger, MacEwan, Michael, Ta

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 576 KB

english, 2009

34

Safety Notables: Information from the Literature

Barnhart, Richard W., Dale, David J., Ironside, Michael D., Vogt, Paul F.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 122 KB

english, 2009

35

The Resolution of 2-Hydroxy-5,5-dimethyl-4-phenyl-1,3,2-dioxaphosphorinan 2-Oxide (Phencyphos) by Preferential Crystallization

Leeman, Michel, Querniard, Florian, Vries, T. R., Kaptein, Bernard, Kellogg, Richard M.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 289 KB

english, 2009

36

Continuous Crystallization of Pharmaceuticals Using a Continuous Oscillatory Baffled Crystallizer

Lawton, Simon, Steele, Gerry, Shering, Phil, Zhao, Lihua, Laird, Ian, Ni, Xiong-Wei

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 2.56 MB

english, 2009

37

The Discovery and Development of a Safe, Practical Synthesis of ABT-869

Kruger, Albert W., Rozema, Michael J., Chu-Kung, Alexander, Gandarilla, Jorge, Haight, Anthony R., Kotecki, Brian J., Richter, Steven M., Schwartz, Albert M., Wang, Zhe

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 191 KB

english, 2009

38

Endoscopy-Based in Situ Bulk Video Imaging of Batch Crystallization Processes

Simon, Levente L., Nagy, Zoltan K., Hungerbuhler, Konrad

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 1.87 MB

english, 2009

39

Book Review of Green Catalysis Green Catalysis . Edited by Paul T. Anastas . Wiley-VCH : Weinheim . Three volumes. 2009 . 1082 pp. €499. ISBN 978-3-52731577-2 .

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 33 KB

english, 2009

40

Green N -Methylation of Electron Deficient Pyrroles with Dimethylcarbonate

Laurila, Michael L., Magnus, Nicholas A., Staszak, Michael A.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 161 KB

english, 2009

41

Special Polymorphism and Crystallisation Feature Section

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 31 KB

english, 2009

42

Special Safety Feature Section

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 30 KB

english, 2009

43

Book Review of Catalysis of Organic Reactions Catalysis of Organic Reactions . Edited by Michael L. Prunier . CRC Press/Taylor Francis : Boca Raton, FL . 2009 . 549 + xxvi pp. $169.95. ISBN 978-1-4200-7076-7 .

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 34 KB

english, 2009

44

Development of a Scalable Synthesis of Dipeptidyl Peptidase-4 Inhibitor ABT-279

McDermott, Todd S., Bhagavatula, Lakshmi, Borchardt, Thomas B., Engstrom, Kenneth M., Gandarilla, Jorge, Kotecki, Brian J., Kruger, Albert W., Rozema, Michael J., Sheikh, Ahmad Y., Wagaw, Seble H., Wi

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 313 KB

english, 2009

45

Practical Segregation of Incompatible Reagents in the Organic Chemistry Laboratory

Wiener, John J. M., Grice, Cheryl A.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 2.64 MB

english, 2009

46

Crystallization Behavior of Polymorphic Mixtures of MPPO

Nakata, Yoshitaka, Kiyosawa, Youko, Kagara, Kooji, Matsuoka, Masakuni

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 4.82 MB

english, 2009

47

An Efficient Laboratory Automation Concept for Process Chemistry

Bernlind, Christian, Urbaniczky, Csaba

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 4.91 MB

english, 2009

48

Seeded Batch Cooling Crystallization with Temperature Cycling for the Control of Size Uniformity and Polymorphic Purity of Sulfathiazole Crystals

Bakar, Mohd R. Abu, Nagy, Zoltan K., Rielly, Chris D.

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 7.09 MB

english, 2009

49

An Efficient Synthesis of a Cyclic Ether Key Intermediate for 9-Membered Masked Enediyne Using an Automated Synthesizer

Tanaka, Yoshikazu, Fuse, Shinichiro, Tanaka, Hiroshi, Doi, Takayuki, Takahashi, Takashi

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 3.00 MB

english, 2009

50

Polymorphic Crystallization and Transformation of the Anti-Viral/HIV Drug Stavudine

Lu, Jie, Rohani, Sohrab

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 4.81 MB

english, 2009

51

The Effect of Temperature and Solvent Composition on Transformation of β- to α-Glycine As Monitored in Situ by FBRM and PVM

Dang, Leping, Yang, Huaiyu, Black, Simon, Wei, Hongyuan

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 2.70 MB

english, 2009

52

A Continuously Operated Bimembrane Reactor Process for the Biocatalytic Production of (2 R ,5 R )-Hexanediol

Schroer, Kirsten, Lütz, Stephan

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 314 KB

english, 2009

53

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

McLaughlin, Mark, García Rubio, Silvina, Tilstam, Ulf, Laird, Trevor, Zlota, Andrei

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 864 KB

english, 2009

54

An Efficient Kilogram-Scale Synthesis of N , N ′-Bis(4,6-disubstituted 1,3,5-triazin-2-yl)-4-aminophenetylamine

Duceppe, Jean-Simon, Perron, Valérie, Cloutier, Josée, Penney, Christopher, Zacharie, Boulos

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 318 KB

english, 2009

55

Online Reaction Monitoring and Evaluation of Kinetic Parameters for Dilute Reactions Using Refractive Index Measurements

Tjahjono, Martin, Widjaja, Effendi, Garland, Marc

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 187 KB

english, 2009

56

Solvent Effects on the Crystallization and Preferential Nucleation of Carbamazepine Anhydrous Polymorphs: A Molecular Recognition Perspective

Kelly, Ron C., Rodríguez-Hornedo, Naír

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 2.85 MB

english, 2009

57

Pilot-Plant Preparation of an α v β 3 Integrin Antagonist. Part 3. Process Research and Development of a Diisopropylcarbodiimide and Catalytic 1-Hydroxybenzotriazole Peptide Coupling †

Clark, Jerry D., Anderson, D. Keith, Banaszak, David V., Brown, Derek B., Czyzewski, Ann M., Edeny, Albert D., Forouzi, Puneh S., Gallagher, Donald J., Iskos, V. H., Kleine, H. Peter, Knable, Carl M.,

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 2.37 MB

english, 2009

58

Some Thoughts on Generic API Manufacture

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 44 KB

english, 2009

59

A Rapid Method for Screening Crystallization Conditions and Phases of an Active Pharmaceutical Ingredient

Detoisien, Thibaud, Forite, Maxime, Taulelle, Pascal, Teston, Joël, Colson, Didier, Klein, Jean Paul, Veesler, Stéphane

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 3.59 MB

english, 2009

60

Book Review of Flash Chemistry: Fast Organic Synthesis in Microsystems Flash Chemistry: Fast Organic Synthesis in Microsystems . Edited by Jun-ichi Yoshida . Wiley : New York . 2009 . 244 + ix pp. €94.90. ISBN 978-0-470-03586-3 .

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 34 KB

english, 2009

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