Paul Giles - Academia.edu (original) (raw)

Papers by Paul Giles

Research paper thumbnail of Indoline derivatives as 5-HT 2C receptor agonists

Bioorganic & Medicinal Chemistry Letters, 2004

A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT 2C receptor agon... more A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT 2C receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for all of the compounds at 5-HT 2 receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration.

Research paper thumbnail of An Improved Process for the <i>N</i>-Alkylation of Indoles Using Chiral <i>N</i>-Protected 2-Methylaziridines

Organic Process Research & Development, Nov 14, 2002

An improved process for the N-alkylation of indoles using N-protected homochiral aziridines has b... more An improved process for the N-alkylation of indoles using N-protected homochiral aziridines has been developed. This procedure allows reduced quantities of homochiral starting material to be used and leads to improved overall yields and operability.

Research paper thumbnail of Ring Formation by Aromatization and Heteroaromatization

Research paper thumbnail of Structures of 3-formylthiachromen-4-one and 3-(chloromethyl)chromen-4-one

Acta Crystallographica Section C Crystal Structure Communications, 1991

C9oH2004 anthrenecarboxylate whose structure was analyzed by MuUica, Milligan, Belew, Grossie & S... more C9oH2004 anthrenecarboxylate whose structure was analyzed by MuUica, Milligan, Belew, Grossie & Sappenfield (1984). Interest in stable ozonides employed in the synthesis of steroid intermediates led to the first two complete single-crystal structure analyses of such compounds (

Research paper thumbnail of Synthesis of Functional Groups using Vilsmeier Reagents

Synthesis Using Vilsmeier Reagents, 2018

Research paper thumbnail of Formation, Structure, and General Reactions of Vilsmeier Reagents

Synthesis Using Vilsmeier Reagents, 2018

Research paper thumbnail of 4-quinolinemethanol derivatives as purine receptor antagonists (II)

Research paper thumbnail of Preparation of aldehydes or ketones from alcohols

Research paper thumbnail of Thieno-and furopyrimidine derivatives as A2A-receptor antagonists

Research paper thumbnail of ChemInform Abstract: Aerobic, Metal-Catalyzed Oxidation of Alcohols

Research paper thumbnail of Evaluation of analogues of (-)-mefloquine as adenosine A (2A) receptor antagonists

Research paper thumbnail of Stereocontrolled syntheses of novel cyclic sulfinates using N-sulfinyl-p-toiuenesulfonamide

Journal of the Chemical Society, Chemical Communications, 1993

Chiral cyclic and bicyclic sulfinates (sultines) are formed with high stereoselection by the reac... more Chiral cyclic and bicyclic sulfinates (sultines) are formed with high stereoselection by the reacti a I co h o I s with N-su If i n y I-p-to I u e n esu Ifo n a m i de (Ts N SO).

Research paper thumbnail of An Improved Process for the N-Alkylation of Indoles Using Chiral N-Protected 2-Methylaziridines

Organic Process Research & Development, 2003

An improved process for the N-alkylation of indoles using N-protected homochiral aziridines has b... more An improved process for the N-alkylation of indoles using N-protected homochiral aziridines has been developed. This procedure allows reduced quantities of homochiral starting material to be used and leads to improved overall yields and operability.

Research paper thumbnail of Dimethylchloromethyleneammonium Chloride

Encyclopedia of Reagents for Organic Synthesis, 2001

Research paper thumbnail of Dimethylbromomethyleneammonium Bromide

Encyclopedia of Reagents for Organic Synthesis, 2001

Research paper thumbnail of Syn-Stereocontrolled dihydroxylation of Baylis-Hillman adducts

Recueil des Travaux Chimiques des Pays-Bas, 2010

... R. Giles #, Zdenek Janousek #, Nigel J. Hindley #*b, Jean-Paul Declercq #, Bernard Tinant #, ... more ... R. Giles #, Zdenek Janousek #, Nigel J. Hindley #*b, Jean-Paul Declercq #, Bernard Tinant #, Janine Feneau-Dupont # and John S. Svendsen ... Acetylation (AcCl/py/CH,CI,) pro-ceeded efficiently and without rearrangement, while sily-lation (tBuMezSiC1/Im/CHzC12) gave the ...

Research paper thumbnail of Aerobic, Metal-Catalyzed Oxidation of Alcohols

ChemInform, 2005

Page 1. 2.13.1 Introduction The oxidation of alcohols (1) into aldehydes and ketones (2) is a ubi... more Page 1. 2.13.1 Introduction The oxidation of alcohols (1) into aldehydes and ketones (2) is a ubiquitous trans-formation in Organic Chemistry (Fig. 1). The plethora of reagents available to ac-complish this key reaction is a testimony ...

Research paper thumbnail of Towards the total synthesis of clerocidin. Efficient assembly of the decalin subunit

Tetrahedron Letters, 1999

Decalin 14, the fully-functionalised southern subunit of Clerocidin 1, a unique fungal metabolite... more Decalin 14, the fully-functionalised southern subunit of Clerocidin 1, a unique fungal metabolite, can be readily and stereoselectively assembled from diketone 7.

Research paper thumbnail of Oxidative formylation and chloromethylation in Vilsmeier reactions of O- and S-heterocyclic ketones

Tetrahedron, 1991

The action of DMF-POC13 at 20°C on tetrahydro-4H-pyran-4-one. tetrahydro-4H-thiopyran-4-one, chro... more The action of DMF-POC13 at 20°C on tetrahydro-4H-pyran-4-one. tetrahydro-4H-thiopyran-4-one, chroman-4-one. and thiochroman-4-one affords the corresponding g-chlorovinylaldehydes, whereas with excess DMF-POC13 at 1OO'C chroman-4-one affords 3-(chloromethyl)chromone. and thiochromanone gives 3formylthiochromone.

Research paper thumbnail of Use of a Modified Leimgruber–Batcho Reaction to Prepare 6‐Chloro‐5‐fluoroindole

Synthetic Communications, 2004

... DOI: 10.1081/SCC-120038513 Jon M. Bentley a , James E. Davidson a , Matthew AJ Duncton a b * ... more ... DOI: 10.1081/SCC-120038513 Jon M. Bentley a , James E. Davidson a , Matthew AJ Duncton a b * , Paul R. Giles a &amp;amp; Robert M. Pratt a pages 2295-2301. Available online: 17 Aug 2006. ...

Research paper thumbnail of Indoline derivatives as 5-HT 2C receptor agonists

Bioorganic & Medicinal Chemistry Letters, 2004

A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT 2C receptor agon... more A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT 2C receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for all of the compounds at 5-HT 2 receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration.

Research paper thumbnail of An Improved Process for the <i>N</i>-Alkylation of Indoles Using Chiral <i>N</i>-Protected 2-Methylaziridines

Organic Process Research & Development, Nov 14, 2002

An improved process for the N-alkylation of indoles using N-protected homochiral aziridines has b... more An improved process for the N-alkylation of indoles using N-protected homochiral aziridines has been developed. This procedure allows reduced quantities of homochiral starting material to be used and leads to improved overall yields and operability.

Research paper thumbnail of Ring Formation by Aromatization and Heteroaromatization

Research paper thumbnail of Structures of 3-formylthiachromen-4-one and 3-(chloromethyl)chromen-4-one

Acta Crystallographica Section C Crystal Structure Communications, 1991

C9oH2004 anthrenecarboxylate whose structure was analyzed by MuUica, Milligan, Belew, Grossie & S... more C9oH2004 anthrenecarboxylate whose structure was analyzed by MuUica, Milligan, Belew, Grossie & Sappenfield (1984). Interest in stable ozonides employed in the synthesis of steroid intermediates led to the first two complete single-crystal structure analyses of such compounds (

Research paper thumbnail of Synthesis of Functional Groups using Vilsmeier Reagents

Synthesis Using Vilsmeier Reagents, 2018

Research paper thumbnail of Formation, Structure, and General Reactions of Vilsmeier Reagents

Synthesis Using Vilsmeier Reagents, 2018

Research paper thumbnail of 4-quinolinemethanol derivatives as purine receptor antagonists (II)

Research paper thumbnail of Preparation of aldehydes or ketones from alcohols

Research paper thumbnail of Thieno-and furopyrimidine derivatives as A2A-receptor antagonists

Research paper thumbnail of ChemInform Abstract: Aerobic, Metal-Catalyzed Oxidation of Alcohols

Research paper thumbnail of Evaluation of analogues of (-)-mefloquine as adenosine A (2A) receptor antagonists

Research paper thumbnail of Stereocontrolled syntheses of novel cyclic sulfinates using N-sulfinyl-p-toiuenesulfonamide

Journal of the Chemical Society, Chemical Communications, 1993

Chiral cyclic and bicyclic sulfinates (sultines) are formed with high stereoselection by the reac... more Chiral cyclic and bicyclic sulfinates (sultines) are formed with high stereoselection by the reacti a I co h o I s with N-su If i n y I-p-to I u e n esu Ifo n a m i de (Ts N SO).

Research paper thumbnail of An Improved Process for the N-Alkylation of Indoles Using Chiral N-Protected 2-Methylaziridines

Organic Process Research & Development, 2003

An improved process for the N-alkylation of indoles using N-protected homochiral aziridines has b... more An improved process for the N-alkylation of indoles using N-protected homochiral aziridines has been developed. This procedure allows reduced quantities of homochiral starting material to be used and leads to improved overall yields and operability.

Research paper thumbnail of Dimethylchloromethyleneammonium Chloride

Encyclopedia of Reagents for Organic Synthesis, 2001

Research paper thumbnail of Dimethylbromomethyleneammonium Bromide

Encyclopedia of Reagents for Organic Synthesis, 2001

Research paper thumbnail of Syn-Stereocontrolled dihydroxylation of Baylis-Hillman adducts

Recueil des Travaux Chimiques des Pays-Bas, 2010

... R. Giles #, Zdenek Janousek #, Nigel J. Hindley #*b, Jean-Paul Declercq #, Bernard Tinant #, ... more ... R. Giles #, Zdenek Janousek #, Nigel J. Hindley #*b, Jean-Paul Declercq #, Bernard Tinant #, Janine Feneau-Dupont # and John S. Svendsen ... Acetylation (AcCl/py/CH,CI,) pro-ceeded efficiently and without rearrangement, while sily-lation (tBuMezSiC1/Im/CHzC12) gave the ...

Research paper thumbnail of Aerobic, Metal-Catalyzed Oxidation of Alcohols

ChemInform, 2005

Page 1. 2.13.1 Introduction The oxidation of alcohols (1) into aldehydes and ketones (2) is a ubi... more Page 1. 2.13.1 Introduction The oxidation of alcohols (1) into aldehydes and ketones (2) is a ubiquitous trans-formation in Organic Chemistry (Fig. 1). The plethora of reagents available to ac-complish this key reaction is a testimony ...

Research paper thumbnail of Towards the total synthesis of clerocidin. Efficient assembly of the decalin subunit

Tetrahedron Letters, 1999

Decalin 14, the fully-functionalised southern subunit of Clerocidin 1, a unique fungal metabolite... more Decalin 14, the fully-functionalised southern subunit of Clerocidin 1, a unique fungal metabolite, can be readily and stereoselectively assembled from diketone 7.

Research paper thumbnail of Oxidative formylation and chloromethylation in Vilsmeier reactions of O- and S-heterocyclic ketones

Tetrahedron, 1991

The action of DMF-POC13 at 20°C on tetrahydro-4H-pyran-4-one. tetrahydro-4H-thiopyran-4-one, chro... more The action of DMF-POC13 at 20°C on tetrahydro-4H-pyran-4-one. tetrahydro-4H-thiopyran-4-one, chroman-4-one. and thiochroman-4-one affords the corresponding g-chlorovinylaldehydes, whereas with excess DMF-POC13 at 1OO'C chroman-4-one affords 3-(chloromethyl)chromone. and thiochromanone gives 3formylthiochromone.

Research paper thumbnail of Use of a Modified Leimgruber–Batcho Reaction to Prepare 6‐Chloro‐5‐fluoroindole

Synthetic Communications, 2004

... DOI: 10.1081/SCC-120038513 Jon M. Bentley a , James E. Davidson a , Matthew AJ Duncton a b * ... more ... DOI: 10.1081/SCC-120038513 Jon M. Bentley a , James E. Davidson a , Matthew AJ Duncton a b * , Paul R. Giles a &amp;amp; Robert M. Pratt a pages 2295-2301. Available online: 17 Aug 2006. ...