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On the mechanism of an asymmetric alpha,beta-unsaturated carboxylic acid hydrogenation: application to the synthesis of a PGD2 receptor antagonist

Tellers, David M ; Mcwilliams, J Christopher ; Humphrey, Guy ; Journet, Michel ; Dimichele, Lisa ; Hinksmon, Joseph ; Mckeown, Arlene E ; Rosner, Thorsten ; Sun, Yongkui ; Tillyer, Richard D

Journal of the American Chemical Society, 27 December 2006, Vol.128(51), pp.17063-73 [Peer Reviewed Journal]

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Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor

Labrecque, Pascale ; Roy, Sébastien J ; Fréchette, Louis ; Iorio-Morin, Christian ; Gallant, Maxime A ; Parent, Jean-Luc

PloS one, 2013, Vol.8(6), pp.e65767 [Peer Reviewed Journal]

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Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans

Cheng, Kang ; Wu, Tsuei-Ju ; Wu, Kenneth K ; Sturino, Claudio ; Metters, Kathleen ; Gottesdiener, Keith ; Wright, Samuel D ; Wang, Zhaoyin ; O'Neill, Gary ; Lai, Eseng ; Waters, M Gerard

Proceedings of the National Academy of Sciences of the United States of America, 25 April 2006, Vol.103(17), pp.6682-7 [Peer Reviewed Journal]

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Thromboxane A2/prostaglandin H2 receptor antagonists. A new therapeutic principle

Patscheke, H

Stroke, December 1990, Vol.21(12 Suppl), pp.IV139-42 [Peer Reviewed Journal]

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Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists

Brescia, Marc-Raleigh ; Rokosz, Laura L ; Cole, Andrew G ; Stauffer, Tara M ; Lehrach, John M ; Auld, Douglas S ; Henderson, Ian ; Webb, Maria L

Bioorganic & medicinal chemistry letters, 01 March 2007, Vol.17(5), pp.1211-5 [Peer Reviewed Journal]

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Discovery of new chemical leads for prostaglandin D2 receptor antagonists

Torisu, Kazuhiko ; Kobayashi, Kaoru ; Iwahashi, Maki ; Egashira, Hiromu ; Nakai, Yoshihiko ; Okada, Yutaka ; Nanbu, Fumio ; Ohuchida, Shuichi ; Nakai, Hisao ; Toda, Masaaki

Bioorganic & medicinal chemistry letters, 06 September 2004, Vol.14(17), pp.4557-62 [Peer Reviewed Journal]

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2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists

Sandham, David A ; Aldcroft, Clive ; Baettig, Urs ; Barker, Lucy ; Beer, David ; Bhalay, Gurdip ; Brown, Zarin ; Dubois, Gerald ; Budd, David ; Bidlake, Louise ; Campbell, Emma ; Cox, Brian ; Everatt, Brian ; Harrison, David ; Leblanc, Catherine J ; Manini, Jodie ; Profit, Rachael ; Stringer, Rowan ; Thompson, Katy S ; Turner

Bioorganic & medicinal chemistry letters, 01 August 2007, Vol.17(15), pp.4347-50 [Peer Reviewed Journal]

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Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2

Hattori, Kouji ; Okitsu, Osamu ; Tabuchi, Seiichiro ; Taniguchi, Kiyoshi ; Nishio, Mie ; Koyama, Satoshi ; Seki, Jiro ; Sakane, Kazuo

Bioorganic & medicinal chemistry letters, 01 July 2005, Vol.15(13), pp.3279-83 [Peer Reviewed Journal]

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Discovery of a potent and selective prostaglandin D2 receptor antagonist, (3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopentabindol-3-yl-acetic acid (MK-0524)

Sturino, Claudio F ; O'Neill, Gary ; Lachance, Nicolas ; Boyd, Michael ; Berthelette, Carl ; Labelle, Marc ; Li, Lianhai ; Roy, Bruno ; Scheigetz, John ; Tsou, Nancy ; Aubin, Yves ; Bateman, Kevin P ; Chauret, Nathalie ; Day, Stephen H ; Lévesque, Jean-François ; Seto, Carmai ; Silva

Journal of medicinal chemistry, 22 February 2007, Vol.50(4), pp.794-806 [Peer Reviewed Journal]

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Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4

Hattori, Kouji ; Takamura, Fujiko ; Tanaka, Akira ; Takasugi, Hisashi ; Taniguchi, Kiyoshi ; Nishio, Mie ; Koyama, Satoshi ; Seki, Jiro ; Sakane, Kazuo

Bioorganic & medicinal chemistry letters, 01 July 2005, Vol.15(13), pp.3284-7 [Peer Reviewed Journal]

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Specific PGF(2alpha) receptor (FP) antagonism and human uterine contractility in vitro

Friel, Anne M ; O'Reilly, Michael W ; Sexton, Donal J ; Morrison, John J

BJOG : an international journal of obstetrics and gynaecology, August 2005, Vol.112(8), pp.1034-42 [Peer Reviewed Journal]

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Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists

Robarge, Michael J ; Bom, David C ; Tumey, L Nathan ; Varga, Norbert ; Gleason, Elizabeth ; Silver, Daniel ; Song, Jianping ; Murphy, Steven M ; Ekema, George ; Doucette, Chris ; Hanniford, Doug ; Palmer, Marc ; Pawlowski, Gary ; Danzig, Joel ; Loftus, Margaret ; Hunady, Karen ; Sherf, Bruce A ; Mays, Robert W ; Stricker-Krongrad, Alain ; Brunden

Bioorganic & medicinal chemistry letters, 15 March 2005, Vol.15(6), pp.1749-53 [Peer Reviewed Journal]

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A practical synthesis for the core structure of a family of selective prostaglandin D2 receptor antagonists

Campos, Kevin R ; Journet, Michel ; Cai, Dongwei ; Kowal, Jason J ; Lee, Sandra ; Larsen, Robert D ; Reider, Paul J

The Journal of organic chemistry, 21 March 2003, Vol.68(6), pp.2338-42 [Peer Reviewed Journal]

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Identification of an indole series of prostaglandin D2 receptor antagonists

Sturino, Claudio F ; Lachance, Nicolas ; Boyd, Michael ; Berthelette, Carl ; Labelle, Marc ; Li, Lianhai ; Roy, Bruno ; Scheigetz, John ; Tsou, Nancy ; Brideau, Christine ; Cauchon, Elizabeth ; Carriere, Marie-Claude ; Denis, Danielle ; Greig, Gillian ; Kargman, Stacia ; Lamontagne, Sonia ; Mathieu, Marie-Claude ; Sawyer, Nicole ; Slipetz, Deborah ; O'Neill

Bioorganic & medicinal chemistry letters, 01 June 2006, Vol.16(11), pp.3043-8 [Peer Reviewed Journal]

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15
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Synthesis and in vitro evaluation of a selective antagonist and the corresponding radioligand for the prostaglandin D2 receptor CRTH2

Ulven, Trond ; Gallen, Michael J ; Nielsen, Mads C ; Merten, Nicole ; Schmidt, Carola ; Mohr, Klaus ; Tränkle, Christian ; Kostenis, Evi

Bioorganic & medicinal chemistry letters, 01 November 2007, Vol.17(21), pp.5924-7 [Peer Reviewed Journal]

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16
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Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis

Beaulieu, Christian ; Wang, Zhaoyin ; Denis, Danielle ; Greig, Gillian ; Lamontagne, Sonia ; O'Neill, Gary ; Slipetz, Deborah ; Wang, Jennifer

Bioorganic & medicinal chemistry letters, 21 June 2004, Vol.14(12), pp.3195-9 [Peer Reviewed Journal]

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17
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Asymmetric synthesis of a prostaglandin D2 receptor antagonist

Campos, Kevin R ; Journet, Michel ; Lee, Sandra ; Grabowski, Edward J J ; Tillyer, Richard D

The Journal of organic chemistry, 07 January 2005, Vol.70(1), pp.268-74 [Peer Reviewed Journal]

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18
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AL-8810: a novel prostaglandin F2 alpha analog with selective antagonist effects at the prostaglandin F2 alpha (FP) receptor

Griffin, B W ; Klimko, P ; Crider, J Y ; Sharif, N A

The Journal of pharmacology and experimental therapeutics, September 1999, Vol.290(3), pp.1278-84 [Peer Reviewed Journal]

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19
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Metabolic activation of indole-containing prostaglandin D2 receptor 1 antagonists: impacts of glutathione trapping and glucuronide conjugation on covalent binding

Lévesque, Jean-François ; Day, Stephen H ; Chauret, Nathalie ; Seto, Carmai ; Trimble, Laird ; Bateman, Kevin P ; Silva, José M ; Berthelette, Carl ; Lachance, Nicolas ; Boyd, Michael ; Li, Lianhai ; Sturino, Claudio F ; Wang, Zhaoyin ; Zamboni, Robert ; Young, Robert N ; Nicoll-Griffith, Deborah A

Bioorganic & medicinal chemistry letters, 01 June 2007, Vol.17(11), pp.3038-43 [Peer Reviewed Journal]

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20
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Discovery of potent CRTh2 (DP2) receptor antagonists

Birkinshaw, Timothy N ; Teague, Simon J ; Beech, Claire ; Bonnert, Roger V ; Hill, Stephen ; Patel, Anil ; Reakes, Sara ; Sanganee, Hitesh ; Dougall, Iain G ; Phillips, Tim T ; Salter, Sylvia ; Schmidt, Jerzy ; Arrowsmith, Elizabeth C ; Carrillo, Juan J ; Bell, Fiona M ; Paine, Stuart W ; Weaver, Richard

Bioorganic & medicinal chemistry letters, 15 August 2006, Vol.16(16), pp.4287-90 [Peer Reviewed Journal]

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21
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Discovery of orally active prostaglandin D2 receptor antagonists

Torisu, Kazuhiko ; Kobayashi, Kaoru ; Iwahashi, Maki ; Nakai, Yoshihiko ; Onoda, Takahiro ; Nagase, Toshihiko ; Sugimoto, Isamu ; Okada, Yutaka ; Matsumoto, Ryoji ; Nanbu, Fumio ; Ohuchida, Shuichi ; Nakai, Hisao ; Toda, Masaaki

Bioorganic & medicinal chemistry letters, 04 October 2004, Vol.14(19), pp.4891-5 [Peer Reviewed Journal]

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22
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Discovery of a new class of potent, selective, and orally active prostaglandin D2 receptor antagonists

Torisu, Kazuhiko ; Kobayashi, Kaoru ; Iwahashi, Maki ; Nakai, Yoshihiko ; Onoda, Takahiro ; Nagase, Toshihiko ; Sugimoto, Isamu ; Okada, Yutaka ; Matsumoto, Ryoji ; Nanbu, Fumio ; Ohuchida, Shuichi ; Nakai, Hisao ; Toda, Masaaki

Bioorganic & medicinal chemistry, 15 October 2004, Vol.12(20), pp.5361-78 [Peer Reviewed Journal]

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23
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Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2

Armer, Richard E ; Ashton, Mark R ; Boyd, Edward A ; Brennan, Chris J ; Brookfield, Frederick A ; Gazi, Lucien ; Gyles, Shân L ; Hay, Philip A ; Hunter, Michael G ; Middlemiss, David ; Whittaker, Mark ; Xue, Luzheng ; Pettipher, Roy

Journal of medicinal chemistry, 06 October 2005, Vol.48(20), pp.6174-7 [Peer Reviewed Journal]

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24
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Development of prostaglandin D2 receptor antagonist: discovery of highly potent antagonists

Torisu, Kazuhiko ; Kobayashi, Kaoru ; Iwahashi, Maki ; Nakai, Yoshihiko ; Onoda, Takahiro ; Nagase, Toshihiko ; Sugimoto, Isamu ; Okada, Yutaka ; Matsumoto, Ryoji ; Nanbu, Fumio ; Ohuchida, Shuichi ; Nakai, Hisao ; Masaaki Toda, Hisao

Bioorganic & medicinal chemistry, 01 September 2004, Vol.12(17), pp.4685-700 [Peer Reviewed Journal]

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25
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Delay of preterm birth in sheep by THG113.31, a prostaglandin F2alpha receptor antagonist

Hirst, Jonathan J ; Parkington, Helena C ; Young, I Ross ; Palliser, Hannah K ; Peri, Krishna G ; Olson, David M

American journal of obstetrics and gynecology, July 2005, Vol.193(1), pp.256-66 [Peer Reviewed Journal]

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26
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Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism

Wang, Yingcai ; Fu, Zice ; Schmitt, Michael ; Wang, Xuemei ; Shen, Wang ; Rickel, Erika ; Martin, Tod ; Budelsky, Alison ; Marshall, Derek ; Collins, Tassie ; Tang, H Lucy ; Medina, Julio C ; Liu, Jiwen Jim

Bioorganic & medicinal chemistry letters, 01 January 2012, Vol.22(1), pp.367-70 [Peer Reviewed Journal]

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27
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Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits

Ulven, Trond ; Receveur, Jean-Marie ; Grimstrup, Marie ; Rist, Øystein ; Frimurer, Thomas M ; Gerlach, Lars-Ole ; Mathiesen, Jesper Mosolff ; Kostenis, Evi ; Uller, Lena ; Högberg, Thomas

Journal of medicinal chemistry, 16 November 2006, Vol.49(23), pp.6638-41 [Peer Reviewed Journal]

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28
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Synthesis and in vitro platelet aggregation and TP receptor binding studies on bicyclic 5,8-ethanooctahydroisoquinolines and 5,8-ethanotetrahydroisoquinolines

Saha, Shankar L ; Roche, Victoria F ; Pendola, Kathleen ; Kearley, Mark ; Lei, Longping ; Romstedt, Karl J ; Herdman, Mark ; Shams, Gamal ; Kaisare, Vivek ; Feller, Dennis R

Bioorganic & medicinal chemistry, August 2002, Vol.10(8), pp.2779-93 [Peer Reviewed Journal]

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29
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Discovery of a new class of potent, selective, and orally bioavailable CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases

Crosignani, Stefano ; Page, Patrick ; Missotten, Marc ; Colovray, Véronique ; Cleva, Christophe ; Arrighi, Jean-François ; Atherall, John ; Macritchie, Jackie ; Martin, Thierry ; Humbert, Yves ; Gaudet, Marilène ; Pupowicz, Doris ; Maio, Maurizio ; Pittet, Pierre-André ; Golzio, Lucia ; Giachetti

Journal of medicinal chemistry, 10 April 2008, Vol.51(7), pp.2227-43 [Peer Reviewed Journal]

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30
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Identification of 2-(2-(1-naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido4,3-bindol-5(2H)-yl)acetic acid (setipiprant/ACT-129968), a potent, selective, and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist

Fretz, Heinz ; Valdenaire, Anja ; Pothier, Julien ; Hilpert, Kurt ; Gnerre, Carmela ; Peter, Oliver ; Leroy, Xavier ; Riederer, Markus A

Journal of medicinal chemistry, 27 June 2013, Vol.56(12), pp.4899-911 [Peer Reviewed Journal]

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31
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Discovery of new orally active prostaglandin D2 receptor antagonists

Iwahashi, Maki ; Naganawa, Atsushi ; Kinoshita, Atsushi ; Shimabukuro, Atsushi ; Nishiyama, Toshihiko ; Ogawa, Seiji ; Matsunaga, Yoko ; Tsukamoto, Kohki ; Okada, Yutaka ; Matsumoto, Ryoji ; Nambu, Fumio ; Oumi, Rie ; Odagaki, Yoshihiko ; Katagi, Jun ; Yano, Koji ; Tani, Kousuke ; Nakai, Hisao ; Toda, Masaaki

Bioorganic & medicinal chemistry, 15 November 2011, Vol.19(22), pp.6935-48 [Peer Reviewed Journal]

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32
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Azaindoles as potent CRTH2 receptor antagonists

Simard, Daniel ; Leblanc, Yves ; Berthelette, Carl ; Zaghdane, M Helmi ; Molinaro, Carmela ; Wang, Zhaoyin ; Gallant, Michel ; Lau, Stephen ; Thao, Trinh ; Hamel, Martine ; Stocco, Rino ; Sawyer, Nicole ; Sillaots, Susan ; Gervais, Francois ; Houle, Robert ; Lévesque, Jean-François

Bioorganic & medicinal chemistry letters, 15 January 2011, Vol.21(2), pp.841-5 [Peer Reviewed Journal]

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33
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The 3D Structure of Human DP Prostaglandin G-Protein-Coupled Receptor Bound to Cyclopentanoindole Antagonist, Predicted Using the DuplexBiHelix Modification of the GEnSeMBLE Method

Shankar, Vishnu ; Goddard, William A ; Kim, Soo-Kyung ; Abrol, Ravinder ; Liu, Fan

Journal of chemical theory and computation, 13 March 2018, Vol.14(3), pp.1624-1642 [Peer Reviewed Journal]

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34
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Isoquinoline derivatives as potent CRTH2 receptor antagonists: synthesis and SAR

Nishikawa-Shimono, Rie ; Sekiguchi, Yoshinori ; Koami, Takeshi ; Kawamura, Madoka ; Wakasugi, Daisuke ; Watanabe, Kazuhito ; Wakahara, Shunichi ; Matsumoto, Kayo ; Takayama, Tetsuo

Bioorganic & medicinal chemistry letters, 01 May 2012, Vol.22(9), pp.3305-10 [Peer Reviewed Journal]

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35
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Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold

Valdenaire, Anja ; Pothier, Julien ; Renneberg, Dorte ; Riederer, Markus A ; Peter, Oliver ; Leroy, Xavier ; Gnerre, Carmela ; Fretz, Heinz

Bioorganic & medicinal chemistry letters, 15 February 2013, Vol.23(4), pp.944-8 [Peer Reviewed Journal]

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36
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CRTH2 antagonist MK-7246: a synthetic evolution from discovery through development

Molinaro, Carmela ; Bulger, Paul G ; Lee, Ernest E ; Kosjek, Birgit ; Lau, Stephen ; Gauvreau, Danny ; Howard, Melissa E ; Wallace, Debra J ; O'Shea, Paul D

The Journal of organic chemistry, 02 March 2012, Vol.77(5), pp.2299-309 [Peer Reviewed Journal]

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