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Fabio Bertozzi


Research Line

D3 PharmaChemistry


IIT Central Research Labs Genova


+39 010 2896 235
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Fabio Bertozzi was educated at the University of Pisa (Italy) where he graduated in Chemistry and Pharmaceutical Technology in 1998. During his studies, he joined an Erasmus internship at Center of Chemistry and Chemical Engineering at the University of Lund (Sweden), under the supervision of Prof. T. Frejd.

He received his Ph.D. in Organic Chemistry at the University of Pisa (Italy) in 2002, in the lab of Prof. F. Macchia and Prof. P. Crotti. The research work was focused on the development of new catalytic asymmetric methodologies using organometallic reagents (organozinc and Grignard reagents) in combination with unsaturated small-ring heterocycles.

During his Ph.D., he had a graduate internship at Department of Organic and Molecular Inorganic Chemistry, University of Groningen (The Netherlands) in the lab of Prof. B.L. Feringa, working on the development of novel catalytic asymmetric reactions employing organometallic reagents.

In 2002, Dr. Bertozzi joined ACADIA Pharmaceuticals, Copenhagen (Denmark), for a to post-doctoral fellowship aiming at the development of a novel and synthetic useful one-pot methodology for the synthesis of drug-like structures by a metal-iodide promoted three-component reaction.

In 2003, Dr. Bertozzi became Scientist in the Drug Discovery group at Acadia Pharmaceuticals, where he worked on different early stage projects on the hit confirmation/lead determination process in the field of CNS related diseases. He was also responsible for setting up a High Throughput Medicinal Chemistry lab/group for the design and synthesis of libraries of compounds.

In 2007, Dr. Bertozzi held the position of Research Scientist in the Department of Medicinal Chemistry at ACADIA Pharmaceuticals, coordinating an advanced research 5-HT program, aiming at the nomination of a new clinical candidate. He contributed to the chemistry efforts in the design, synthesis, purification of compounds for testing, coordinating of the communication between chemistry and other departments (bioscience, DMPK, In-vivo, toxicology).

Dr. Bertozzi holds 1 issued patent and has published 14 original papers in leading international journals.

Dr. Bertozzi joined IIT in November 2009, where he currently holds a Team Leader position in the Drug Discovery and Development unit.

Selected Publications

A New Diastereo- and Enantioselective Copper-Catalyzed Conversion of Alkynyl Epoxides into a-Allenic Alcohols.Bertozzi, F.; Crotti, P.; Macchia, F.; Pineschi, M.; Arnold, A.; Feringa, B.L. Tetrahedron Letters 1999, 40, 4893-4896.

A New Catalytic and Enantioselective Desymmetrization of Symmetrical Methylidene Cycloalkene Oxides.Bertozzi, F.; Crotti, P.; Macchia, F.; Pineschi, M.; Arnold, A.; Feringa, B.L. Organic Letters 2000, 2, 933-936.

Temporary in Situ Aluminum and Zinc Tethering in Diels-Alder Reactions. Bertozzi, F.; Olsson, R.; Frejd, T. Organic Letters 2000, 2, 1283-1286.

Highly Enantioselective Regiodivergent and Catalytic Parallel Kinetic Resolution. Bertozzi, F.; Crotti, P.; Macchia, F.; Pineschi, M.; Feringa, B.L. Angewandte Chemie, Int. Ed.2001, 40, 930-932.


A Multigram, Catalytic and Enantioselective Synthesis of Optically Active 4-Methyl-2-Cyclohexen-1-one: a Useful Chiral Building Block. Bertozzi, F.; Crotti, P.; Macchia, F.; Pineschi, M.; Feringa, B.L. Synthesis 2001, 3, 483-486.


Unprecedented Catalytic Enantioselective Trapping of Arene Oxides with Dialkylzinc Reagents.Bertozzi, F.; Crotti, P.; Del Moro, F.; Macchia, F.; Pineschi, M.; Feringa, B.L. Chemical Communications 2001, 2606-2607.


Copper Phosphoramidite Catalyzed Enantioselective Ring-Opening of Oxabicyclic Alkenes: Remarkable Reversal of Stereocontrol. Bertozzi, F.; Pineschi, M.; Macchia, F.; Arnold, A.; Minnaard, A.; Feringa, B.L. Organic Letters 2002, 4, 2703-2705.


A Novel Metal-Iodide Promoted Three-Component Synthesis of Substituted Pyrrolidines.Bertozzi, F.; Gustafsson, M.; Olsson, R. Organic Letters 2002, 4, 3147-3150.


A One-Pot Three-Component Reaction for the Synthesis of a-(Aminoethyl)-a,b-Enones. Bertozzi, F.; Gustafsson, M.; Olsson, R. Organic Letters 2002, 4, 4333-4336.


A Combinatorial Scaffold Approach Based upon a Multicomponent Reaction. Bertozzi, F.; Gundersen, B.V.; Gustafsson, M.; Olsson, R. Organic Letters 2003, 5, 1551-1554.


Copper-Catalyzed Addition of Organometallic Reagents to Vinyl Diepoxides. A Novel Entry to Oxabridged Systems and to Substituted Allylic Alcohols. Bertozzi, F.; Crotti, P.; Del Moro, F.; Di Bussolo,V.; Macchia,F.; Pineschi, M. Eur. J. Org. Chem. 2003, 1264-1270.


Treating Neuropathic Pain with Neuropeptide FF Receptor 2 Agonists. Scully, A.L.; Davis, R.E.; Vanover, K.E.; Gardell, L.R.; Lameh, J.; Kelly, N.M.; Bertozzi, F. PCT Int. Appl. (2005) WO2005031000A220050407.


Discovery of Selective Nonpeptidergic Neuropeptide FF2 Receptor Agonists. Gaubert, G.; Bertozzi, F.; Kelly, N.M.; Pawlas, J.; Scully, A.L.; Nash, N.R.; Gardell, L.R.; Lameh, J.; Olsson R. J. Med. Chem. 2009, 52, 6511-6514.


Synthesis, Structure-Activity Relationships, and Characterization of Novel Nonsteroidal and Selective Androgen Receptor Modulators. Schlienger, N.; Lund, B.W.; Pawlas, J.; Badalassi, F.; Bertozzi, F.; Lewinsky, R.; Fejzic, A.; Thygesen, M.B.; Tabatabaei, A.; Risso Bradley, S.; Gardell, L.R.; Piu, F.; Olsson, R. J. Med. Chem. 2009, 52, 7186–7191.


Neuropeptide FF Receptors have opposing Modulatory Effects on Nociception. Lameh, J.; Bertozzi, F.; Kelly, N.M.; Jacobi, P.M.; Nguyen, D.; Bajpai, A.; Gaubert, G.; Olsson, R.; Gardell, L.R. J. Pharm. Exper. Therap. 2010, 334, 244-254.


Armirotti, A.; Romeo, E.; Ponzano, S.; Mengatto, L.; Dionisi, M.; Karacsonyi, C.; Bertozzi, F.; Garau, G.; Tarozzo, G.; Reggiani, A.; Bandiera, T.; Tarzia, G.; Mor, M.; Piomelli, D.b-lactones inhibit N-acylethanolamine acid amidase by S-acylation of the catalytic N-terminal cysteine. ACS Med. Chem. Lett. 2012, 3, 422-426.



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