quintus

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1. Personal Information

Name
Stuart Mickel
Organization(s)
Novartis Pharma AG, Basel Switzerland

2. Community Expertise

The Synaptic Leap community
Skills
Chemistry

3. Publications

Publications

Publications, Lectures & Patents:
Boron Chemistry as applied in the total synthesis of discodemoliide
Mickel Stuart
5th BASF Boron Conference, Hyderabas, India, February, 2008

Boron Chemistry as applied in the total synthesis of discodemoliide
Mickel Stuart
3rd BASF Boron Conference, Heildeberg Germany, November, 2007

Various lectures given at meetings and universities in Europe, the USA and Japan, by invitation from 2004 – present, dealing with the synthesis of discodermolide. See, for example, Pure and Applied Chemistry (2007), 79(4), 685-700

Alternative synthesis of aryl-octanoyl amide compounds.
Mickel, Stuart John. (Novartis AG, Switz.).
Application: GB 2005-21723 20051025. Priority:

Abstract

An alternative synthesis of certain 2(S), 4(S), 5(S), 7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amide compds. or pharmaceutically acceptable salts thereof which uses the synthetic pathway detailed in Schemes 1-4. Novel intermediates are used in the prepn. of the above target compd.

Alternative synthesis of aryl-octanoyl amide compounds.
Mickel, Stuart John. (Novartis AG, Switz.).
Application: GB 2005-21725 20051025.

Abstract

An alternative synthesis of 2(S), 4(S), 5(S), 7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amide compds. or pharmaceutically acceptable salts thereof which uses the synthetic pathway detailed in Schemes 1-3. Novel intermediates are used in the prepn. of the above target compd.

Alternative synthesis of aryl-octanoyl amide compounds.
Mickel, Stuart John. (Novartis AG, Switz
Application: GB 2005-21745 20051025. Priority:

Abstract

An alternative synthesis of certain 2(S), 4(S), 5(S), 7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amide compds. or pharmaceutically acceptable salts thereof which uses cyclooctadiene monoepoxide as a starting material. Novel intermediates are used in the prepn. of the above target compd.

Alternative synthesis of aryl-octanoyl amide compounds.
Mickel, Stuart John. (Novartis AG, Switz.).
Application: GB 2005-21751 20051025. Priority

Abstract

An alternative synthesis of certain 2(S), 4(S), 5(S), 7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amide compds. or pharmaceutically acceptable salts thereof which uses a beta-lactam as a starting material and follows the synthetic pathway defined in Schemes 1 and 2. Novel intermediates are used in the prepn. of the above target compd.

Alternative synthesis of aryl-octanoyl amide compounds.
Mickel, Stuart John. (Novartis AG, Switz.).
Application: GB 2005-21752 20051025. Priority

Abstract

An alternative synthesis of certain 2(S), 4(S), 5(S), 7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amide derivs. or pharmaceutically acceptable salts thereof utilizes an oxazolidinone compd. of formula (1a) and the reaction scheme defined in Scheme 1 therein. Novel intermediates are used in the prepn. of the above target compd.

Alternative synthesis of aryl-octanoyl amide compounds.
Mickel, Stuart John. (Novartis AG, Switz.).
Application: GB 2005-21748 20051025. Priority:

Abstract

An alternative synthesis of certain 2(S), 4(S), 5(S), 7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amide derivs. or pharmaceutically acceptable salts thereof which utilizes a palladium coupling reaction as defined in Scheme 1 therein. Novel intermediates are used in the prepn. of the above target compd.

Total synthesis of the marine natural product (+)-discodermolide in multigram quantities. Mickel, Stuart J.
Pure and Applied Chemistry (2007), 79(4), 685-700

Sythesis of renin inhibitors involving a cycloaddition reaction.
Mickel, Stuart John; Marterer, Wolfgang
WO 2007039183 A1

Process for preparation of chiral protected 2-aryl-5-hydroxymethyl-3-isopropylpyrrolidines from protected 2-amino-1-hydroxy-4-hydroxybenzyl-5-methylhexanes.
Mickel, Stuart John; Sedelmeier, Gottfried; Hirt, Hans; Schaefer, Frank; Foulkes, Michael.
WO 2006131304 A2 20061214

Process for alternative synthesis of aliskiren and intermediates.
Mickel, Stuart John, Sedelmeier, Gottfried; Rueeger, Heinrich.
WO 2006024501 A1 20060309

Adventures in Natural Product Synthesis: The large Scale Total Synthesis of the Marine Natrual Product (+)-Discodermolide
Mickel Stuart J. in Strategies and Tactics in Organic Synthesis, Volume 6,p269. Ed, Harmata M: Published Elesivier, Amsterdam 2006.

From deep-sea sponge to pilot plant: The large scale total synthesis of the marine natural product (+)-Discodermolide.
Mickel, Stuart J.
Abstracts, 37th Middle Atlantic Regional Meeting of the American Chemical Society, New Brunswick, NJ, United States, May 22-25, 2005 (2005)

From deep-sea sponge to pilot plant: The large scale total synthesis of the marine natural product (+)-Discodermolide.
Mickel, Stuart J..
Abstracts of Papers, 229th ACS National Meeting, San Diego, CA, United States, March 13-17, 2005 (2005
A Study of the Paterson Boron Aldol Reaction as Used in the Large-Scale Total Synthesis of the Anticancer Marine Natural Product (+)-Discodermolide.
Mickel, Stuart J.; Daeffler, Robert; Prikoszovich, Walter.
Organic Process Research & Development (2005), 9(1), 113-120.

Toward a commercial synthesis of (+)-discodermolide.
Mickel, Stuart J.
Current Opinion in Drug Discovery & Development (2004), 7(6), 869-881. Publisher: Thomson Scientific

Broad spectrum chemistry as practised by Novartis Process Research.
Mickel, Stuart J.; Fischer, Reto; Marterer, Wolfgang.
Chimia (2004), 58(9), 640-648.

Synthetic Analogues of the Microtubule-Stabilizing Agent (+)-Discodermolide: Preparation and Biological Activity.
Gunasekera, Sarath P.; Mickel, Stuart J.; Daeffler, Robert; Niederer, Daniel; Wright, Amy E.; Linley, Patricia; Pitts, Tara
Journal of Natural Products (2004), 67(5), 749-756.

Synthesis of discodermolide and analogs.
Florence, Gordon; Koch, Guido; Loiseleur, Olivier; Mickel, Stuart John; Paterson, Ian.
WO 2004009574 A1 20040129

Large-Scale Synthesis of the Anti-Cancer Marine Natural Product (+)-Discodermolide. Part 5: Linkage of Fragments C1-6 and C7-24 and Finale.
Mickel, Stuart J.; Niederer, Daniel; Daeffler, Robert; Osmani, Adnan; Kuesters, Ernst; Schmid, Emil; Schaer, Karl; Gamboni, Remo; Chen, Weichun; Loeser, Eric; Kinder, Frederick R., Jr.; Konigsberger, Kurt; Prasad, Kapa; Ramsey, Timothy M.; Repic, Oljan; Wang, Run-Ming; Florence, Gordon; Lyothier, Isabelle; Paterson, Ian.
Organic Process Research & Development (2004), 8(1), 122-130.

Large-Scale Synthesis of the Anti-Cancer Marine Natural Product (+)-Discodermolide. Part 4: Preparation of Fragment C7-24.
Mickel, Stuart J.; Sedelmeier, Gottfried H.; Niederer, Daniel; Schuerch, Friedrich; Seger, Manuela; Schreiner, Klaus; Daeffler, Robert; Osmani, Adnan; Bixel, Dominique; Loiseleur, Olivier; Cercus, Jacques; Stettler, Hans; Schaer, Karl; Gamboni, Remo; Bach, Andrew; Chen, Guang-Pei; Chen, Weichun; Geng, Peng; Lee, George T.; Loeser, Eric; McKenna, Joseph; Kinder, Frederick R., Jr.; Konigsberger, Kurt; Prasad, Kapa; Ramsey, Timothy M.; Reel, Noela; Repic, Oljan; Rogers, Larry; Shieh, Wen-Chung; Wang, Run-Ming; Waykole, Liladhar; Xue, Song; Florence, Gordon; Paterson, Ian.
Organic Process Research & Development (2004), 8(1), 113-121.

Large-Scale Synthesis of the Anti-Cancer Marine Natural Product (+)-Discodermolide. Part 3: Synthesis of Fragment C15-21.
Mickel, Stuart J.; Sedelmeier, Gottfried H.; Niederer, Daniel; Schuerch, Friedrich; Koch, Guido; Kuesters, E.; Daeffler, Robert; Osmani, Adnan; Seeger-Weibel, Manuela; Schmid, E.; Hirni, Alfred; Schaer, Karl; Gamboni, Remo; Bach, Andrew; Chen, Stephen; Chen, Weichun; Geng, Peng; Jagoe, Christopher T.; Kinder, Frederick R., Jr.; Lee, George T.; McKenna, Joseph; Ramsey, Timothy M.; Repic, Oljan; Rogers, Larry; Shieh, Wen-Chung; Wang, Run-Ming; Waykole, Liladhar.
Organic Process Research & Development (2004), 8(1), 107-112.

Large-Scale Synthesis of the Anti-Cancer Marine Natural Product (+)-Discodermolide. Part 2: Synthesis of Fragments C1-6 and C9-14.
Mickel, Stuart J.; Sedelmeier, Gottfried H.; Niederer, Daniel; Schuerch, Friedrich; Grimler, Dominique; Koch, Guido; Daeffler, Robert; Osmani, Adnan; Hirni, Alfred; Schaer, Karl; Gamboni, Remo; Bach, Andrew; Chaudhary, Apurva; Chen, Stephen; Chen, Weichun; Hu, Bin; Jagoe, Christopher T.; Kim, Hong-Yong; Kinder, Frederick R., Jr.; Liu, Yugang; Lu, Yansong; McKenna, Joseph; Prashad, Mahavir; Ramsey, Timothy M.; Repic, Oljan; Rogers, Larry; Shieh, Wen-Chung; Wang, Run-Ming; Waykole, Liladhar.
Organic Process Research & Development (2004), 8(1), 101-106

Large-Scale Synthesis of the Anti-Cancer Marine Natural Product (+)-Discodermolide. Part 1: Synthetic Strategy and Preparation of a Common Precursor.
Mickel, Stuart J.; Sedelmeier, Gottfried H.; Niederer, Daniel; Daeffler, Robert; Osmani, Adnan; Schreiner, Klaus; Seeger-Weibel, Manuela; Berod, Brigitte; Schaer, Karl; Gamboni, Remo; Chen, Stephen; Chen, Weichun; Jagoe, Christopher T.; Kinder, Frederick R., Jr.; Loo, Mauricio; Prasad, Kapa; Repic, Oljan; Shieh, Wen-Chung; Wang, Run-Ming; Waykole, Liladhar; Xu, David D.; Xue, Song.
Organic Process Research & Development (2004), 8(1), 92-100.

Ligands for expression cloning and isolation of GABAB receptors.
Froestl, Wolfgang; Bettler, Bernhard; Bittiger, Helmut; Heid, Jakob; Kaupmann, Klemens; Mickel, Stuart J.; Strub, Dietrich.
Farmaco (2003), 58(3), 173-183.

Ligands for expression cloning and isolation of GABAB receptors.
Froestl, Wolfgang; Bettler, Bernhard; Bittiger, Helmut; Heid, Jakob; Kaupmann, Klemens; Mickel, Stuart J.; Strub, Dietrich.
Farmaco (2001) 56(1-2), 101-105.

Ligands for the isolation of GABAB receptors .
Froestl, W.; Bettler, B.; Bittiger, H.; Heid, J.; Kaupmann, K.; Mickel, S. J.; Strub, D
Neuropharmacology (1999), 38(11), 1641-1646.

Morpholin-2-yl-phosphinic acids are potent GABAB receptor antagonists in rat brain.
Ong, Jennifer; Kerr, David I. B.; Bittiger, Helmut; Waldmeier, Peter C.; Baumann, Peter A.; Cooke, Nigel G.; Mickel, Stuart J.; Froestl, Wolfgang
European Journal of Pharmacology (1998), 362(1), 27-34

Cloning of rat and human metabotropic GABAB receptors and use of receptor-specific ligands.
Kaupmann, Klemens; Bettler, Bernhard; Bittiger, Helmut; Frostl, Wolfgang; Mickel, Stuart John. WO 9746675 A1 19971211

Chemistry of GABAB modulators.
Froestl, Wolfgang; Mickel, Stuart J.
USA. Editor(s): Enna, S. J.; Bowery, Norman G.
GABA Receptors (2nd Edition) (1997), 271-296. Publisher: Humana Press, Otowa,

Novel hydroxylated and alkoxylated N- and/or P-aralkylphosphinic acid derivatives.
Stampf, Philippe; Froestl, Wolfgang; Mickel, Stuart John; Zimmermann, Kaspar
WO 9711953 A1

Substituted phosphinic compounds and their use as pharmaceuticals.
Froestl, Wolfgang; Mickel, Stuart John; Cooke, Nigel Graham; Bennett, Stuart Norman Lile; Williams, Anne Rachel Burton
WO 9709335 A1

Expression cloning of GABAB receptors uncovers similarity to metabotropic glutamate receptors.
Kaupmann, Klemens; Huggel, Katharina; Heid, Jakob; Flor, Peter J.; Bischoff, Serge; Mickel, Stuart J.; McMaster, Gary; Angst, Christof; Bittiger, Helmut; Froestl, Wolfgang; Bettler, Bernhard
Nature (London) (1997), 386(6622), 239-246.

Potent, orally active GABAB receptor antagonists.
Froestl, W.; Mickel, S. J.; Schmutz, M.; Bittiger, H
Pharmacology Reviews and Communications (1996), 8(2-3, 3rd International GABAB Symposium, 1996), 127-133.

GABAB receptor antagonists: New tools and potential new drugs.
Froestl, W.; Mickel, S. J.; Mondadori, C.; Olpe, H. -R.; Pozza, M. F.; Waldmeier, P. C.; Bittiger, H.
Pharmacochemistry Library (1996), 24(Perspectives in Receptor Research), 253-270. Publisher: Elsevier

GABAB receptor antagonists: Potential therapeutic applications.
Bittiger, H.; Froestl, W.; Gentsch, C.; Jaekel, J.; Mickel, S. J.; Mondadori, C.; Olpe, H. R.; Schmutz, M
Editor(s): Tanaka, Chikako; Bowery, Norman G.
GABA: Receptors, Transporters and Metabolism (1996), 297-305

Determination of rat brain and plasma levels of the orally active GABAB antagonist 3-amino-propyl-n-butyl-phosphinic acid (CGP 36742) by a new GC/MS method.
Steulet, Anne-Francoise; Moebius, Hans-Joerg; Mickel, Stuart J.; Stoecklin, Kurt; Waldmeier, Peter C.
Biochemical Pharmacology (1996), 51(5), 613-19.

Phosphinic Acid Analogs of GABA. 2. Selective, Orally Active GABAB Antagonists.
Froestl, Wolfgang; Mickel, Stuart J.; von Sprecher, Georg; Diel, Peter J.; Hall, Roger G.; Maier, Ludwig; Strub, Dietrich; Melillo, Vito; Baumann, Peter A.; et al
Journal of Medicinal Chemistry (1995), 38(17), 3313-31.

Phosphinic Acid Analogs of GABA. 1. New Potent and Selective GABAB Agonists.
Froestl, Wolfgang; Mickel, Stuart J.; Hall, Roger G.; von Sprecher, Georg; Strub, Dietrich; Baumann, Peter A.; Brugger, Felix; Gentsch, Conrad; Jaekel, Joachim; et al.
Journal of Medicinal Chemistry (1995), 38(17), 3297-312.

GABA and glutamate release affected by GABAB receptor antagonists with similar potency: no evidence for pharmacologically different presynaptic receptors.
Waldmeier, Peter C.; Wicki, Peter; Feldtrauer, Jean-Jacques; Mickel, Stuart J.; Bittiger, Helmut; Baumann, Peter A.
British Journal of Pharmacology (1994), 113(4), 1515-21

Novel N-aralkyl and N-heteroaralkylaminoalkanephosphinic acids, preparations and nootropic and antiepileptic properties.
Mickel, Stuart John; Froestl, Wolfgang; Furet, Pascal.
EP 569333 A2 19931110

GABAB antagonists: Potential new drugs.
Bittiger, H.; Bernasconi, R.; Froestl, W.; Hall, R.; Jaekel, J.; Klebs, K.; Krueger, L.; Mickel, S. J.; Mondadori, C.;
Pharmacology Communications (1992), 2(1-2), 70-4.

Chemistry of new GABAB antagonists.
Froestl, W.; Mickel, S.J.; Von Sprecher, G.; Bittiger, H.; Olpe, H. R
Pharmacology Communications (1992), 2(1-2), 52-6.

3H-CGP 54 626: A potent antagonist radioligand for GABAB receptors.
Bittiger, H.; Reymann, N.; Froestl, W.; Mickel, S.J
Pharmacology Communications (1992), 2(1-2), 23.

Preparation and GABA antagonistic property of aminoalkanephosphinic acids and their salts.
Mickel, Stuart John
EP 543780 A2 19930526

The action of new potent GABAB receptor antagonists in the hemisected spinal cord preparation of the rat.
Brugger, Felix; Wicki, Urs; Olpe, Hans Rudolf; Froestl, Wolfgang; Mickel, Stuart.
European Journal of Pharmacology (1993), 235(1), 153-5.

GABAb antagonists: Novel CNS-active compounds.
Froestl, Wolgang; Furet, Pascal; Hall, Roger G.; Mickel, Stuart J.; Strub, Dieter; von Sprecher, Georg; Baumann, Peter A.; Bernasconi, Raymond; Brugger, Felix; et al
Editor(s): Testa, Bernard.
Perspect. Med. Chem. (1993), 259-72. Publisher: Verlag Helvetica Chim. Acta, Basel, Switz

The actions of orally active GABAB receptor antagonists on GABAergic transmission in vivo and in vitro.
Olpe, Hans Rudolf; Steinmann, Martin W.; Ferrat, Thomas; Pozza, Mario F.; Greiner, Karin; Brugger, Felix; Froestl, Wolfgang; Mickel, Stuart J.; Bittiger, Helmut
European Journal of Pharmacology (1993), 233(2-3), 179-86.

Preparation of (aminopropyl)phosphinates as GABAB antagonists. Baylis, Eric K.; Bittiger, Helmut; Froestl, Wolfgang; Hall, Roger G.; Maier, Ludwig; Mickel, Stuart J.; Olpe, Hans Rudolf.
Cont.-in-part of U.S. Ser. No. 378,887. US 5051524 Application: US 90-484716 19900226. Priority: GB 87-28483 19871204; US 88-275882 19881125; US 89-378887 19890712.

Preparation of (3-aminopropyl)phosphinates as antiepileptics.
Marescaux, Christian; Bernasconi, Raymond; Schmutz, Markus; Froestl, Wolfgang; Mickel, Stuart J.. EP 463560 A1 19920102

(γ )-2-Amino-2-thiazoline-4-ethanoic acid; a novel, specific GABAA receptor agonist.
Campbell, M. M.; Mickel, S. J.; Singh, G.
Bioorganic & Medicinal Chemistry Letters (1991), 1(5), 247-8.

Preparation of P-substituted propylphosphinic acid compounds as GABAB receptor antagonists.
Mickel, Stuart J.; Von Sprecher, Georg.
EP 402312 A2 19901212

Preparation of aminopropylphosphinic acids as GABA antagonists.
Baylis, Eric Keith; Bittiger, Helmut; Froestl, Wolfgang; Hall, Roger Graham; Maier, Ludwig; Mickel, Stuart John; Olpe, Hans Rudolf.
EP 319479 A2 19890607

Preparation, formulation, and testing of 3-aminopropylphosphinic acids as GABAB antagonists.
Baylis, Eric Keith; Bittiger, Helmut; Froestl, Wolfgang; Hall, Roger Graham; Maier, Ludwig; Mickel, Stuart John; Olpe, Hans Rudolf.
EP 319482 A2 19890607

4-Acetoxyazetidin-2-one: synthesis of a key beta-lactam intermediate by a [2 + 2] cycloaddition route [2-azetidinone, 4-(acetyloxy)-].
Mickel, Stuart J.; Hsiao, Chi Nung; Miller, Marvin J
Organic Syntheses (1987), 65 135-9.

4-Acetoxy-2-azetidinone: a useful heterocyclic synthon.
Mickel, Stuart.
Aldrichimica Acta (1985), 18(4), 95-9.

The synthesis of a new phosphorus-containing bicyclic β -lactam.
Campbell, Malcolm M.; Carruthers, Nicholas I.; Mickel, Stuart J.; Winton, Peter M
Journal of the Chemical Society, Chemical Communications (1984), (3), 200.

Aminophosphonic and aminophosphinic acid analogs of aspartic acid.
Campbell, Malcolm M.; Carruthers, Nicholas I.; Mickel, Stuart J
Tetrahedron (1982), 38(16), 2513-24.

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