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1

Development of a Fit-for-Purpose Large-Scale Synthesis of an Oral PARP Inhibitor

Wallace, Debra J., Baxter, Carl A., Brands, Karel J. M., Bremeyer, Nadine, Brewer, Sarah E., Desmond, Richard, Emerson, Khateeta M., Foley, Jennifer, Fernandez, Paul, Hu, Weifeng, Keen, Stephen P., Mu

Journal:

Organic Process Research & Development

Year:

2011

Language:

english

File:

PDF, 981 KB

english, 2011

2

Reaction Development and Mechanistic Study of a Ruthenium Catalyzed Intramolecular Asymmetric Reductive Amination en Route to the Dual Orexin Inhibitor Suvorexant (MK-4305)

Strotman, Neil A., Baxter, Carl A., Brands, Karel M. J., Cleator, Ed, Krska, Shane W., Reamer, Robert A., Wallace, Debra J., Wright, Timothy J.

Journal:

Journal of the American Chemical Society

Year:

2011

Language:

english

File:

PDF, 1.24 MB

english, 2011

3

ChemInform Abstract: Observations on the DDQ Oxidation of 1-Acyldihydropyridines — A Synthetic Application.

Debra J. Wallace, Andrew D. Gibb, Ian F. Cottrell, Derek J. Kennedy, Karel M. J. Brands, Ulf H. Dolling

Journal:

Year:

2002

File:

PDF, 31 KB

2002

4

Efficient One-Pot Synthesis of the 2-Aminocarbonylpyrrolidin-4-ylthio-Containing Side Chain (I) of the New Broad-Spectrum Carbapenem Antibiotic Ertapenem.

Karel M. J. Brands, et al. et al.

Journal:

Year:

2002

File:

PDF, 27 KB

2002

5

Practical Asymmetric Synthesis of Aprepitant (I), a Potent Human NK-1 Receptor Antagonist, via a Stereoselective Lewis Acid Catalyzed trans Acetalization Reaction.

Matthew Zhao, James M. McNamara, Guo-Jie Ho, Khateeta M. Emerson, Zhiguo J. Song, David M. Tschaen, Karel M. J. Brands, Ulf-H Dolling, Edward J. J. Grabowski, Paul J. Reider

Journal:

Year:

2003

File:

PDF, 67 KB

2003

6

A Practical Synthesis of Lithium 3-Fluoropyridine-2-carboxylate.

Khateeta M. Emerson, Robert D. Wilson, Michael S. Ashwood, Derek J. Kennedy, David Hands, Karel M. J. Brands, Ian F. Cottrell, Ulf-H. Dolling

Journal:

Year:

2004

File:

PDF, 80 KB

2004

7

Regioselective Synthesis of 1,3,5-Substituted Pyrazoles from Acetylenic Ketones and Hydrazines.

Brian C. Bishop, Karel M. J. Brands, Andrew D. Gibb, Derek J. Kennedy

Journal:

Year:

2004

File:

PDF, 128 KB

2004

8

An Efficient One-Pot Synthesis of Annulated Pyridines Utilizing a Directed ortho-Metalation/Transmetalation Approach.

Antony J. Davies, Karel M. J. Brands, Cameron J. Cowden, Ulf-H. Dolling, David R. Lieberman

Journal:

Year:

2004

Language:

english

File:

PDF, 109 KB

english, 2004

9

Expedient Diels—Alder Assembly of 4-Aryl-4-phenylsulfonyl Cyclohexanones.

Jeremy P. Scott, Deborah C. Hammond, Elizabeth M. Beck, Karel M. J. Brands, Antony J. Davies, Ulf-H. Dolling, Derek J. Kennedy

Journal:

Year:

2004

File:

PDF, 146 KB

2004

10

An Efficient and General Synthesis of 3-Substituted Propionaldehydes Using the Suzuki—Miyaura Coupling.

Cameron J. Cowden, Deborah C. Hammond, Brian C. Bishop, Karel M. J. Brands, Antony J. Davies, Ulf-H. Dolling, Sarah E. Brewer

Journal:

Year:

2004

File:

PDF, 24 KB

2004

11

Preparation, Thermal Stability and Carbonyl Addition Reactions of 2,5-Difluorophenyl Lithium and 2,5-Difluorophenyl Grignard.

Jeremy P. Scott, Sarah E. Brewer, Antony J. Davies, Karel M. J. Brands

Journal:

Year:

2004

File:

PDF, 16 KB

2004

12

Syntheses of Morpholine-2,3-diones and 2-Hydroxymorpholin-3-ones: Intermediates in the Synthesis of Aprepitant.

Todd D. Nelson, Jonathan D. Rosen, Karel M. J. Brands, Bridgette Craig, Mark A. Huffman, James M. McNamara

Journal:

Year:

2005

File:

PDF, 16 KB

2005

13

An efficient one-pot synthesis of annulated pyridines utilising a directed ortho-metallation/transmetallation approach

Antony J. Davies, Karel M.J. Brands, Cameron J. Cowden, Ulf-H. Dolling, David R. Lieberman

Journal:

Tetrahedron Letters

Year:

2004

Language:

english

File:

PDF, 253 KB

english, 2004

14

Expedient Diels–Alder assembly of 4-aryl-4-phenylsulfonyl cyclohexanones

Jeremy P. Scott, Deborah C. Hammond, Elizabeth M. Beck, Karel M.J. Brands, Antony J. Davies, Ulf-H. Dolling, Derek J. Kennedy

Journal:

Tetrahedron Letters

Year:

2004

Language:

english

File:

PDF, 256 KB

english, 2004

15

An efficient and general synthesis of 3-substituted propionaldehydes using the Suzuki–Miyaura coupling

Cameron J Cowden, Deborah C Hammond, Brian C Bishop, Karel M.J Brands, Antony J Davies, Ulf-H Dolling, Sarah E Brewer

Journal:

Tetrahedron Letters

Year:

2004

Language:

english

File:

PDF, 253 KB

english, 2004

16

Syntheses of morpholine-2,3-diones and 2-hydroxymorpholin-3-ones: intermediates in the synthesis of aprepitant

Todd D. Nelson, Jonathan D. Rosen, Karel M.J. Brands, Bridgette Craig, Mark A. Huffman, James M. McNamara

Journal:

Tetrahedron Letters

Year:

2004

Language:

english

File:

PDF, 270 KB

english, 2004

17

Practical routes to the triarylsulfonyl chloride intermediate of a β3 adrenergic receptor agonist

Norihiro Ikemoto, Jinchu Liu, Karel M.J Brands, James M McNamara, Paul J Reider

Journal:

Year:

2003

Language:

english

File:

PDF, 208 KB

english, 2003

18

Synthesis of the “tricyclic heart” of manzamines

Karel M.J. Brands, Upendra K. Pandit

Journal:

Tetrahedron Letters

Year:

1989

Language:

english

File:

PDF, 265 KB

english, 1989

19

Intestinal nodular lymphoid hyperplasia in patients with common variable immunodeficiency: Local accumulation of B and CD8(+) lymphocytes

Paul Brande, Karel Geboes, Gaston Vantrappen, André Eeckhout, Simonne Vertessen, Erik A. M. Stevens, Jan L. Ceuppens

Journal:

Journal of Clinical Immunology

Year:

1988

Language:

english

File:

PDF, 1.32 MB

english, 1988

20

Synthesis of the homochiral “tricyclic heart” of manzamine A

Karel M.J. Brands, Arthur A.P. Meekel, Upendra K. Pandit

Journal:

Year:

1991

Language:

english

File:

PDF, 1.56 MB

english, 1991

21

Development of a Scaleable Synthesis of a Partial Nicotinic Acid Receptor Agonist

Wilson, Robert D., Cleator, Ed, Ashwood, Michael S., Bio, Matthew M., Brands, Karel M. J., Davies, Antony J., Dolling, Ulf-H., Emerson, Khateeta M., Gibb, Andrew D., Hands, David

Journal:

Organic Process Research & Development

Year:

2009

Language:

english

File:

PDF, 497 KB

english, 2009

22

Efficient Synthesis of NK1 Receptor Antagonist Aprepitant Using a Crystallization-Induced Diastereoselective Transformation†

Brands, Karel M. J., Payack, Joseph F., Rosen, Jonathan D., Nelson, Todd D., Candelario, Alexander, Huffman, Mark A., Zhao, Matthew M., Li, Jing, Craig, Bridgette, Song, Zhiguo J.

Journal:

Journal of the American Chemical Society

Year:

2003

Language:

english

File:

PDF, 138 KB

english, 2003

23

Crystallization-Induced Diastereomer Transformations†

Brands, Karel M. J., Davies, Antony J.

Journal:

Chemical Reviews

Year:

2006

Language:

english

File:

PDF, 585 KB

english, 2006

24

A Practical Synthesis of Lithium 3-Fluoropyridine-2-carboxylate

Emerson, Khateeta M., Wilson, Robert D., Ashwood, Michael S., Kennedy, Derek J., Hands, David, Brands, Karel M. J., Cottrell, Ian F., Dolling, Ulf-H

Journal:

Synthetic Communications

Year:

2003

Language:

english

File:

PDF, 161 KB

english, 2003

25

Continuous ST-segment monitoring associated with infarct size and left ventricular function in the GUSTO-I trial

Karel G.M. Moons, Peter Klootwijk, Simon H. Meij, Gerrit-Anne van Es, Taco Baardman, Timo Lenderink, Marcel van den Brand, J.Dik F. Habbema, Diederick E. Grobbee, Maarten L. Simoons

Journal:

American Heart Journal

Year:

1999

Language:

english

File:

PDF, 201 KB

english, 1999

26

Practical Asymmetric Synthesis of a γ-Secretase Inhibitor Exploiting Substrate-Controlled Intramolecular Nitrile Oxide−Olefin Cycloaddition

Scott, Jeremy P., Oliver, Steven F., Brands, Karel M. J., Brewer, Sarah E., Davies, Antony J., Gibb, Andrew D., Hands, David, Keen, Stephen P., Sheen, Faye J., Reamer, Robert A., Wilson, Robert D., Do

Journal:

Journal of Organic Chemistry

Year:

2006

Language:

english

File:

PDF, 131 KB

english, 2006

27

Process Development and Large-Scale Synthesis of a c-Met Kinase Inhibitor

Stewart, Gavin W., Brands, Karel M. J., Brewer, Sarah E., Cowden, Cameron J., Davies, Antony J., Edwards, John S., Gibson, Andrew W., Hamilton, Simon E., Katz, Jason D., Keen, Stephen P., Mullens, Pet

Journal:

Organic Process Research & Development

Year:

2010

Language:

english

File:

PDF, 505 KB

english, 2010

28

Practical Asymmetric Synthesis of Aprepitant, a Potent Human NK-1 Receptor Antagonist, via a Stereoselective Lewis Acid-Catalyzed Trans Acetalization Reaction

Zhao, Matthew M., McNamara, James M., Ho, Guo-Jie, Emerson, Khateeta M., Song, Zhiguo J., Tschaen, David M., Brands, Karel M. J., Dolling, Ulf-H, Grabowski, Edward J. J., Reider, Paul J., Cottrell, Ia

Journal:

Journal of Organic Chemistry

Year:

2002

Language:

english

File:

PDF, 111 KB

english, 2002

29

The First Large-Scale Synthesis of MK-4305: A Dual Orexin Receptor Antagonist for the Treatment of Sleep Disorder

Baxter, Carl A., Cleator, Ed, Brands, Karel M. J., Edwards, John S., Reamer, Robert A., Sheen, Faye J., Stewart, Gavin W., Strotman, Neil A., Wallace, Debra J.

Journal:

Organic Process Research & Development

Year:

2011

Language:

english

File:

PDF, 1.21 MB

english, 2011

30

Understanding the Origin of Unusual Stepwise Hydrogenation Kinetics in the Synthesis of the 3-(4-Fluorophenyl)morpholine Moiety of NK 1 Receptor Antagonist Aprepitant

Brands, Karel M. J., Krska, Shane W., Rosner, Thorsten, Conrad, Karen M., Corley, Edward G., Kaba, Mahmoud, Larsen, Robert D., Reamer, Robert A., Sun, Yongkui, Tsay, Fuh-Rong

Journal:

Organic Process Research & Development

Year:

2006

Language:

english

File:

PDF, 156 KB

english, 2006

31

Practical Synthesis of the New Carbapenem Antibiotic Ertapenem Sodium

Williams, J. Michael, Brands, Karel M. J., Skerlj, Renato T., Jobson, Ronald B., Marchesini, George, Conrad, Karen M., Pipik, Brenda, Savary, Kimberly A., Tsay, Fuh-Rong, Houghton, Peter G., Sidler, D

Journal:

Journal of Organic Chemistry

Year:

2005

Language:

english

File:

PDF, 162 KB

english, 2005

32

Mild Aryl Ether Formation in the Semisynthesis of the Novel Macrolide Immunosuppressant L-732,531

Brands, Karel M. Jos, Dolling, Ulf-H., Jobson, Ronald B., Marchesini, George, Reamer, Robert A., Williams, J. Michael

Journal:

Journal of Organic Chemistry

Year:

1998

Language:

english

File:

PDF, 142 KB

english, 1998

33

Thermal Hazard Evaluation of 4-Methoxybenzyl Chloride (PMB-Cl)

Brewer, Sarah E., Vickery, Thomas P., Bachert, Donald C., Brands, Karel M. J., Emerson, Khateeta M., Goodyear, Adrian, Kumke, Kathleen J., Lam, Thientu, Scott, Jeremy P.

Journal:

Organic Process Research & Development

Year:

2005

Language:

english

File:

PDF, 74 KB

english, 2005

34

A Novel Crystallization-Induced Diastereomeric Transformation Based on a Reversible Carbon−Sulfur Bond Formation. Application to the Synthesis of a γ-Secretase Inhibitor

Davies, Antony J., Scott, Jeremy P., Bishop, Brian C., Brands, Karel M. J., Brewer, Sarah E., DaSilva, Jimmy O., Dormer, Peter G., Dolling, Ulf-H., Gibb, Andrew D., Hammond, Deborah C., Lieberman, Dav

Journal:

Journal of Organic Chemistry

Year:

2007

Language:

english

File:

PDF, 137 KB

english, 2007

35

A Practical Synthesis of a γ-Secretase Inhibitor

Scott, Jeremy P., Lieberman, David R., Beureux, Olivier M., Brands, Karel M. J., Davies, Antony J., Gibson, Andrew W., Hammond, Deborah C., McWilliams, Chris J., Stewart, Gavin W., Wilson, Robert D.,

Journal:

Journal of Organic Chemistry

Year:

2007

Language:

english

File:

PDF, 138 KB

english, 2007

36

Efficient One-Pot Synthesis of the 2-Aminocarbonylpyrrolidin-4-ylthio-Containing Side Chain of the New Broad-Spectrum Carbapenem Antibiotic Ertapenem

Brands, Karel M. J., Jobson, Ronald B., Conrad, Karen M., Williams, J. Michael, Pipik, Brenda, Cameron, Mark, Davies, Antony J., Houghton, Peter G., Ashwood, Michael S., Cottrell, Ian F., Reamer, Robe

Journal:

Journal of Organic Chemistry

Year:

2002

Language:

english

File:

PDF, 83 KB

english, 2002

37

Development of a Phase Transfer Catalyzed Asymmetric Synthesis for an Estrogen Receptor Beta Selective Agonist

Scott, Jeremy P., Ashwood, Michael S., Brands, Karel M. J., Brewer, Sarah E., Cowden, Cameron J., Dolling, Ulf-H., Emerson, Khateeta M., Gibb, Andrew D., Goodyear, Adrian, Oliver, Steven F., Stewart,

Journal:

Organic Process Research & Development

Year:

2008

Language:

english

File:

PDF, 168 KB

english, 2008

38

Practical Asymmetric Synthesis of a Non-Peptidic α v β 3 Antagonist

Keen, Stephen P., Cowden, Cameron J., Bishop, Brian C., Brands, Karel M. J., Davies, Antony J., Dolling, Ulf H., Lieberman, David R., Stewart, Gavin W.

Journal:

Journal of Organic Chemistry

Year:

2005

Language:

english

File:

PDF, 214 KB

english, 2005

39

A Practical and Scaleable Synthesis of 1 R ,5 S -Bicyclo[3.1.0]hexan-2-one: The Development of a Catalytic Lithium 2,2,6,6-Tetramethylpiperidide (LTMP) Mediated Intramolecular Cyclopropanation of ( R )-1,2-Epoxyhex-5-ene

Alorati, Anthony D., Bio, Matthew M., Brands, Karel M. J., Cleator, Ed, Davies, Antony J., Wilson, Robert D., Wise, Chris S.

Journal:

Organic Process Research & Development

Year:

2007

Language:

english

File:

PDF, 57 KB

english, 2007

40

Federsel, Hans Jürgen, Brands, Karel M. J.

Journal:

Organic Process Research & Development

Year:

2007

Language:

english

File:

PDF, 13 KB

english, 2007

41

The conformational bias of aryl, arylsulfonyl geminally substituted tertiary carbon centers: applications in substrate-based stereocontrol

Scott, Jeremy P., Mullens, Peter R., Brewer, Sarah E., Brands, Karel M. J., Chilenski, Jennifer R., Davies, Antony J., Gibb, Andrew D., Lieberman, David R., Oliver, Steven F., Dolling, Ulf-H.

Journal:

Organic & Biomolecular Chemistry

Year:

2006

Language:

english

File:

PDF, 169 KB

english, 2006

42

[AIP NOISE AND FLUCTUATIONS: 20th International Conference on Noice and Fluctuations (ICNF-2009) - Pisa (Italy) (14–19 June 2009)] AIP Conference Proceedings - Universal oscillations of high-order cumulants

Flindt, Christian, Fricke, Christian, Hohls, Frank, Novotný, Tomáš, Netočný, Karel, Brandes, Tobias, Haug, Rolf J., Macucci, Massimo, Basso, Giovanni

Year:

2009

Language:

english

File:

PDF, 904 KB

english, 2009

43

Observations on the DDQ Oxidation of 1-Acyldihydropyridines - A Synthetic Application

Wallace, Debra J., Gibb, Andrew D., Cottrell, Ian F., Kennedy, Derek J., Brands, Karel M. J., Dolling, Ulf H.

Journal:

Year:

2001

Language:

english

File:

PDF, 98 KB

english, 2001

44

Preparation, Thermal Stability and Carbonyl Addition Reactions of 2,5-Difluorophenyl Lithium and 2,5-Difluorophenyl Grignard

Scott, Jeremy P., Brewer, Sarah E., Davies, Antony J., Brands, Karel M.

Journal:

Year:

2004

Language:

english

File:

PDF, 94 KB

english, 2004

45

Synthesis of an Optically Active Tricyclic Intermediate for Manzamines

K. Pandit, Upendra, M. J. Brands, Karel

Journal:

Year:

1990

Language:

english

File:

PDF, 99 KB

english, 1990

46

Development of a General Protocol to Prepare 2H-1, 3-Benzoxazine Derivatives

Qi, Ji, Oliver, Steven F., Xiao, Wensong, Song, Licheng, Brands, Karel M. Jos

Journal:

Organic Process Research & Development

Year:

2017

Language:

english

File:

PDF, 530 KB

english, 2017

47

Increased Mortality Among Patients With vs Without Cirrhosis and Autoimmune Hepatitis

van den Brand, Floris F., van der Veen, Koen S., de Boer, Ynto S., van Gerven, Nicole M., Lissenberg-Witte, Birgit I., Beuers, Ulrich, van Erpecum, Karel J., van Buuren, Henk R., den Ouden, Jannie W.,

Journal:

Clinical Gastroenterology and Hepatology

Year:

2018

Language:

english

File:

PDF, 679 KB

english, 2018