List of works - Giovanni Piersanti

A novel one-pot approach of hexahydropyrrolo[2,3-b]indole nucleus by a cascade addition/cyclization strategy: synthesis of (+/-)-esermethole.

scientific article published on September 2010

A simple, modular synthesis of C4-substituted tryptophan derivatives

scientific article published on 01 October 2016

An improved synthesis of cis-4-phenyl-2-propionamidotetralin (4-P-PDOT): a selective MT(2) melatonin receptor antagonist

scientific article published on 13 November 2007

Concise and Convergent Enantioselective Total Syntheses of (+)- and (-)-Fumimycin

scientific article published on 06 September 2019

Conformation by NMR of two tetralin-based receptor ligands

scientific article

Correlation between energetics of collisionally activated decompositions, interaction energy and biological potency of carbamate FAAH inhibitors

scientific article published on 01 December 2007

Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies

scientific article

Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors.

scientific article

Diastereo- and enantioselective hydrogenation of a challenging enamide derived from 4-phenyl-2-tetralone: an appealing shortcut towards enantiopure cis-2-aminotetraline derivatives

scientific article published in March 2010

Direct B-alkyl Suzuki-Miyaura cross-coupling of 2-halopurines. Practical synthesis of ST1535, a potent adenosine A2A receptor antagonist.

scientific article published in August 2010

Direct preparation of unsymmetrical difunctionalized cyclen derivatives by an Ugi multicomponent reaction

scientific article published on 01 January 2009

Direct, One-Pot Reductive Alkylation of Anilines with Functionalized Acetals Mediated by Triethylsilane and TFA. Straightforward Route for Unsymmetrically Substituted Ethylenediamine

scientific article published on 22 December 2010

Direct, regioselective, and chemoselective preparation of novel boronated tryptophans by Friedel-Crafts alkylation

scientific article published on 30 December 2011

Divergent synthesis of novel 9-deazaxanthine derivatives via late-stage cross-coupling reactions.

scientific article

Enantioselective total synthesis of (-)-acylfulvene and (-)-irofulven

scientific article published on 01 September 2006

Enantioselective total synthesis of (-)-acylfulvene and (-)-irofulven.

scientific article published on December 2009

Facile synthesis of @-tide beta-strand peptidomimetics: improved assembly in solution and on solid phase

scientific article published on 01 November 2004

Iridium-catalyzed direct synthesis of tryptamine derivatives from indoles: exploiting n-protected β-amino alcohols as alkylating agents.

scientific article published on 26 February 2015

Iron-Catalyzed Direct C3-Benzylation of Indoles with Benzyl Alcohols through Borrowing Hydrogen

scientific article published on 26 July 2017

New branched macrocyclic ligand and its side-arm, two urea-based receptors for anions: synthesis, binding studies and crystal structure

New family of polyamine macrocycles containing 2,5-diphenyl[1,3,4]oxadiazole as a signaling unit. Synthesis, acid-base and spectrophotometric properties

scientific article

Observations in the Synthesis of the Core of the Antitumor Illudins via an Enyne Ring Closing Metathesis Cascade

scientific article published on September 2009

Organocatalytic Aza-Friedel-Crafts/Lactonization Domino Reaction of Naphthols and Phenols with 2-Acetamidoacrylate to Naphtho- and Benzofuranones Bearing a Quaternary Center at the C3 Position

scientific article published on 17 September 2018

Palladium(II)-Catalyzed Cross-Dehydrogenative Coupling (CDC) of N-Phthaloyl Dehydroalanine Esters with Simple Arenes: Stereoselective Synthesis of Z-Dehydrophenylalanine Derivatives

scientific article published on 20 May 2016

Palladium(II)-Catalyzed Intramolecular Oxidative C-H/C-H Cross-Coupling Reaction of C3,N-Linked Biheterocycles: Rapid Access to Polycyclic Nitrogen Heterocycles

scientific article published on 17 January 2017

Potent, Metabolically Stable 2-Alkyl-8-(2H-1,2,3-triazol-2-yl)-9H-adenines as Adenosine A2A Receptor Ligands

scientific article published on 07 May 2015

Switchable reactivity of acylated alpha, beta-dehydroamino ester in the Friedel-Crafts alkylation of indoles by changing the Lewis acid

scientific article published on 18 June 2008

Synthesis and Structure-Activity Relationships of FAAH Inhibitors: Cyclohexylcarbamic Acid Biphenyl Esters with Chemical Modulation at the Proximal Phenyl Ring

scientific article published on 01 January 2006

Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.

scientific article published on 24 June 2013

Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand 4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone.

scientific article published on 18 November 2011

Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.

scientific article published on 29 May 2008

Synthesis of (-)-epi-indolactam V by an intramolecular Buchwald-Hartwig C-N coupling cyclization reaction.

scientific article published on 25 July 2013

Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.

scientific article published on 16 January 2013

Synthesis of (±)-cis-clavicipitic acid by a Rh(I)-catalyzed intramolecular imine reaction

scientific article published on 14 March 2014

Synthesis of 2-substituted tryptophans via a C3- to C2-alkyl migration.

scientific article published on 26 August 2014

Synthesis of Tryptamine Derivatives via a Direct, One-Pot Reductive Alkylation of Indoles

scientific article published on 03 July 2012

Synthesis of benzo[1,2-d;3,4-d']diimidazole and 1H-pyrazolo[4,3-b]pyridine as putative A2A receptor antagonists.

scientific article published in August 2007

The collisional behavior of ESI-generated protonated molecules of some carbamate FAAH inhibitors isosteres and its relationships with biological activity

scientific article published on 01 April 2009

Total Synthesis of (-)-Clavicipitic Acid via γ,γ-Dimethylallyltryptophan (DMAT) and Chemoselective C-H Hydroxylation

scientific article published on 05 June 2019

Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.

scientific article

List of works by Giovanni Piersanti

A novel one-pot approach of hexahydropyrrolo[2,3-b]indole nucleus by a cascade addition/cyclization strategy: synthesis of (+/-)-esermethole.

A simple, modular synthesis of C4-substituted tryptophan derivatives

An improved synthesis of cis-4-phenyl-2-propionamidotetralin (4-P-PDOT): a selective MT(2) melatonin receptor antagonist

Concise and Convergent Enantioselective Total Syntheses of (+)- and (-)-Fumimycin

Conformation by NMR of two tetralin-based receptor ligands

Correlation between energetics of collisionally activated decompositions, interaction energy and biological potency of carbamate FAAH inhibitors

Cyclohexylcarbamic acid 3'- or 4'-substituted biphenyl-3-yl esters as fatty acid amide hydrolase inhibitors: synthesis, quantitative structure-activity relationships, and molecular modeling studies

Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors.

Diastereo- and enantioselective hydrogenation of a challenging enamide derived from 4-phenyl-2-tetralone: an appealing shortcut towards enantiopure cis-2-aminotetraline derivatives

Direct B-alkyl Suzuki-Miyaura cross-coupling of 2-halopurines. Practical synthesis of ST1535, a potent adenosine A2A receptor antagonist.

Direct preparation of unsymmetrical difunctionalized cyclen derivatives by an Ugi multicomponent reaction

Direct, One-Pot Reductive Alkylation of Anilines with Functionalized Acetals Mediated by Triethylsilane and TFA. Straightforward Route for Unsymmetrically Substituted Ethylenediamine

Direct, regioselective, and chemoselective preparation of novel boronated tryptophans by Friedel-Crafts alkylation

Divergent synthesis of novel 9-deazaxanthine derivatives via late-stage cross-coupling reactions.

Enantioselective total synthesis of (-)-acylfulvene and (-)-irofulven

Enantioselective total synthesis of (-)-acylfulvene and (-)-irofulven.

Facile synthesis of @-tide beta-strand peptidomimetics: improved assembly in solution and on solid phase

Iridium-catalyzed direct synthesis of tryptamine derivatives from indoles: exploiting n-protected β-amino alcohols as alkylating agents.

Iron-Catalyzed Direct C3-Benzylation of Indoles with Benzyl Alcohols through Borrowing Hydrogen

New branched macrocyclic ligand and its side-arm, two urea-based receptors for anions: synthesis, binding studies and crystal structure

New family of polyamine macrocycles containing 2,5-diphenyl[1,3,4]oxadiazole as a signaling unit. Synthesis, acid-base and spectrophotometric properties

Observations in the Synthesis of the Core of the Antitumor Illudins via an Enyne Ring Closing Metathesis Cascade

Organocatalytic Aza-Friedel-Crafts/Lactonization Domino Reaction of Naphthols and Phenols with 2-Acetamidoacrylate to Naphtho- and Benzofuranones Bearing a Quaternary Center at the C3 Position

Palladium(II)-Catalyzed Cross-Dehydrogenative Coupling (CDC) of N-Phthaloyl Dehydroalanine Esters with Simple Arenes: Stereoselective Synthesis of Z-Dehydrophenylalanine Derivatives

Palladium(II)-Catalyzed Intramolecular Oxidative C-H/C-H Cross-Coupling Reaction of C3,N-Linked Biheterocycles: Rapid Access to Polycyclic Nitrogen Heterocycles

Potent, Metabolically Stable 2-Alkyl-8-(2H-1,2,3-triazol-2-yl)-9H-adenines as Adenosine A2A Receptor Ligands

Switchable reactivity of acylated alpha, beta-dehydroamino ester in the Friedel-Crafts alkylation of indoles by changing the Lewis acid

Synthesis and Structure-Activity Relationships of FAAH Inhibitors: Cyclohexylcarbamic Acid Biphenyl Esters with Chemical Modulation at the Proximal Phenyl Ring

Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.

Synthesis and configuration determination of all enantiopure stereoisomers of the melatonin receptor ligand 4-phenyl-2-propionamidotetralin using an expedient optical resolution of 4-phenyl-2-tetralone.

Synthesis and quantitative structure-activity relationship of fatty acid amide hydrolase inhibitors: modulation at the N-portion of biphenyl-3-yl alkylcarbamates.

Synthesis of (-)-epi-indolactam V by an intramolecular Buchwald-Hartwig C-N coupling cyclization reaction.

Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.

Synthesis of (±)-cis-clavicipitic acid by a Rh(I)-catalyzed intramolecular imine reaction

Synthesis of 2-substituted tryptophans via a C3- to C2-alkyl migration.

Synthesis of Tryptamine Derivatives via a Direct, One-Pot Reductive Alkylation of Indoles

Synthesis of benzo[1,2-d;3,4-d']diimidazole and 1H-pyrazolo[4,3-b]pyridine as putative A2A receptor antagonists.

The collisional behavior of ESI-generated protonated molecules of some carbamate FAAH inhibitors isosteres and its relationships with biological activity

Total Synthesis of (-)-Clavicipitic Acid via γ,γ-Dimethylallyltryptophan (DMAT) and Chemoselective C-H Hydroxylation

Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity.