52. A Multi-component Route to Functionalized Amides and Oxazolidinones

McPherson Amide OL GA

51. Practical Synthesis of Pharmaceutically Relevant Molecules Enriched in sp3 Character

Campbell sp3 Chem Comm GA

50. Chemoselective One-pot Synthesis of Functionalized Amino-azaheterocycles Enabled by COware

Clohessy COware GA

49. Cyrene as a Bio-based Solvent for the Suzuki-Miyaura Cross-coupling

Wilson Cyrene Suzuki GA

48. Connecting the Dots: Method Development Using Sustainable Solvents

Wilson Chem

 

47. A One-pot Tandem Chemoselective Allylation/Cross-coupling via Temperature Control of a Multi-nucleophile/electrophile System

allylation-SM GA

46. Recent Developments in Organoboron Chemistry: Old Dogs, New Tricks

Chem Review GA

45. Modular, Step-efficient Palladium-catalyzed Cross-coupling Strategy to Access C6-Heteroaryl 2-Aminopurine Ribonucleosides

, , , and Org. Lett. 2017, 19, 3759-3762. [pdf] [Supporting Information]

 

Ribonucleoside Org Lett GA

44. A Strategy for Conditional Orthogonal CuAAC Reactions Using a Protected Aromatic Ynamine

, , , and J. Org. Chem. 2017, 82, 5461–5468. [pdf] [Supporting Information]
 
Hatit JOC Deprotection-Click GA

43. Amidation of Unactivated Ester Derivatives Mediated by Trifluoroethanol

C. G. McPherson, N. Caldwell, C. Jamieson, I. Simpson, and A. J. B. Watson Org. Biomol. Chem. 2017, 15, 3507–3518. [pdf] [Supporting Information]

McPherson OBC GA

42. Spectroscopic Studies of the Chan-Lam Amination: A Mechanism-inspired Solution to Boronic Ester Reactivity

J. C. Vantourout, H. N. Miras, A. Isidro-Llobet, S. Sproules, and A. J. B. Watson J. Am. Chem. Soc. 2017, 139, 4769–4779. [pdf] [Supporting Information]

Highlighted by Derek Lowe [link]

Highlighted in OPRD

A most read paper in JACS

Cham-Lam Amination GA

41. Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators

W.-J. Keune, F. Potjewyd, T. Hediebrecht, F. Salgado-Polo, S. J. F. Macdonald, L. Chelvarajan, A. A. Latif, S. Soman, A. J. Morris, A. J. B. Watson, C. Jamieson, and A. Perrakis J. Med. Chem. 2017, 60, 2006–2017. [pdf] [Supporting Information]

 ATX-Hybrids GA

40. Determining the Origin of Rate-independent Chemoselectivity in CuAAC Reaction: An Alkyne-specific Shift in Rate-determining Step

C. P. Seath, G. A. Burley, and A. J. B. Watson Angew. Chem. Int. Ed. 2017, 56, 3314–3318. [pdf] [Supporting Information]

Click kinetics GA

39. The Emergence of Small Molecule Non-RGD-mimetic Inhibitors for RGD Integrins

L. M. Miller, J. Pritchard, S. J. F. Macdonald, C. Jamieson, and A. J. B. Watson J. Med. Chem. 2017, 60, 3241–3251.[pdf]

non-RGD J Med Chem GA

 

38. Structure-activity Relationships of Small Molecule Autotaxin Inhibitors with a Discrete Binding Mode

L. M. Miller, W.-J. Keune, D. Castagna, L. Young, E. Duffy, F. Potjewyd, F. Salgado-Polo, P. Engel García, D. Semaan, J. Pritchard, A. Perrakis, S. J. F. Macdonald, C. Jamieson, and A. J. B. Watson J. Med. Chem. 2017, 60, 722–748. [pdf] [Supporting Information]

Amira ATX GA

37. Chemoselective Suzuki-Miyaura Cross-coupling via Kinetic Transmetallation

J. W. B. Fyfe, N. J. Fazakerley, and A. J. B. Watson Angew. Chem. Int. Ed. 2017, 56, 1249–1253. [pdf] [Supporting Information]

A most read article in ACIE during December 2016

Chemoselective TM ACIE GA

 

36. Chemoselective Brown Oxidation of Aryl Organoboron Systems Enabled by Boronic Acid-selective Phase Transfer

J. J. Molloy, T. A. Clohessy, C. Irving, N. A. Anderson, G. C. Lloyd-Jones, and A. J. B. Watson Chem. Sci. 2017, 8, 1551–1559. [pdf] [Supporting Information]

Highlighted in OPRD

Brown Oxidation GA

35. Scope and Limitations of a DMF Bio-alternative within Sonogashira Cross-coupling and Cacchi-type Annulation

K. L. Wilson, A. R. Kennedy, J. Murray, B. Greatrex, C. Jamieson, and A. J. B. Watson Beilstein J. Org. Chem. 2016, 12, 2005-2011. [pdf] [Supporting Information]

Cyrene Sonogashira GA

34. Synthesis of Oxindoles and Benzofuranones via Oxidation of 2-Heterocyclic BMIDAs

C. P. Seath, J. W. B. Fyfe, J. J. Molloy, and A. J. B. Watson Synthesis 2017, 49, 891–898. [pdf] [Supporting Information]

Oxindole GA

33. Highlights from the 51st EUCHEM Conference on Stereochemistry, Bürgenstock, Switzerland, May 2016

A. J. B. Watson and J. R. Frost Chem. Commun. 2016, 52, 9173–9177. [pdf]

 

32. Synthesis of 2-BMIDA 6,5-Bicyclic Heterocycles by Cu(I)/Pd(0)/Cu(II) Cascade Catalysis of 2-Iodoanilines/phenols

C. P. Seath, K. L. Wilson, A. Campbell, J. M. Mowat, and A. J. B. Watson, Chem. Commun. 2016, 52, 8703–8706. [pdf] [Supporting Information]

BMIDA Indole GA

31. Synthetic Approaches to Coronafacic Acid, Coronamic Acid, and Coronatine

M. M. Littleson, C. J. Russell, E. C. Frye, K. B. Ling, C. Jamieson, and A. J. B. Watson, Synthesis, 2016, 48, 3429–3448. [pdf]

COR-CFA-CMA Synthesis GA

30. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

P. Bamborough, H. A. Barnett, I. Becher, M. J. Bird, C. Chung, P. D. Craggs, E. H. Demont, H. Diallo, D. J. Fallon, L. J. Gordon, P. Grandi, C. I. Hobbs, E. Hooper-Greenhill, E. J. Jones, R. P. Law, A. Le Gall, D. Lugo, A.-M. Michon, D. J. Mitchell, R. K. Prinjha, R. J. Sheppard, A. J. B. Watson, and R. J. Watson, ACS Med. Chem. Lett. 2016, 7, 552–557. [pdf] [Supporting Information]

Selected as an ACS Editor's Choice Article

A Most Read Paper in ACS Med. Chem. Lett. in 2016

BRPF1 Graphical Abstract

 

29. Chan-Evans-Lam Amination of Boronic Acid Pinacol (BPin) Esters: Overcoming the Aryl Amine Problem

J. C. Vantourout, R. P. Law, A. Isidro-Llobet, S. J. Atkinson, and A. J. B. Watson, J. Org. Chem. 2016, 81, 3942–3950. [pdf] [Supporting Information]

Top 5 Most Read Article (April-May 2016)

Highlighted in OPRD

A Most Read Paper in J. Org. Chem. in 2016

Highlighted in Organic Chemistry Portal [link]

CEL BPin Abstract

28. Chemoselective Sequential Click Ligations Directed by Enhanced Reactivity of an Aromatic Ynamine

M. Z. C. Hatit, J. C. Sadler, L. A. McLean, B. C. Whitehurst, C. P. Seath, L. D. Humphreys, R. J. Young, A. J. B. Watson, and G. A. Burley, Org. Lett. 2016, 18, 1694–1697. [pdf] [Supporting Information]

Ynamine click abstract

 

27. The Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature

D. Castagna, D. C. Budd, S. J. F. Macdonald, C. Jamieson, and A. J. B. Watson, J. Med. Chem. 2016, 59, 5604–5621. [pdf]

LPA-ATX review

26. When Two Reactions Become One

J. W. B. Fyfe and A. J. B. Watson, Science 2016, 351, 26–27. [pdf] See the original article by Prof Jim Morken here.

Highlighted in C&EN.

Two become one GA

 

25. One-Pot Homologation of Boronic Acids: A Platform for Diversity-Oriented Synthesis

C. W. Muir, J. C. Vantourout, A. Isidro-Llobet, S. J. F. Macdonald and A. J. B. Watson, Org. Lett. 2015, 17, 6030–6033. [pdf] [Supporting Information]

BOH2 homologation

24. Tandem Chemoselective Suzuki-Miyaura Cross-coupling Enabled by Nucleophile Speciation Control

C. P. Seath, J. W. B. Fyfe, J. J. Molloy, and A. J. B. Watson, Angew. Chem. Int. Ed. 2015, 54, 9976–9979. [pdf] [Supporting Information]

Highlighted in Science [link]

Highlighted in SynFACTS [link]

Double Suzuki-Miyaura

23. Development of Solvent Selection Guides

H. E. Eastman, C. Jamieson, and A. J. B. Watson, Aldrichimica Acta, 2015, 48, 51-55.

Aldrichimica Acta

22. Catalytic Amidation of Unactivated Ester Derivatives Mediated by Trifluoroethanol

N. Caldwell, C. Jamieson, I. Simpson, and A. J. B. Watson, Chem. Commun., 2015, 51, 9495–9498. [pdf] [Supporting Information]

NC Chem Comm

21. Identification of a Novel Class of Autotaxin Inhibitors Through Cross-screening

D. Castagna, E. L. Duffy, D. Semann, L. C. Young, J. M. Pritchard, S. J. F. MacDonald, D. C. Budd, C. Jamieson, and A. J. B. Watson, Med. Chem. Commun., 2015, 6, 1149-1155. [pdf] [Supporting Information]

ATX-LPA Graphical Abstract

 

20. Speciation Control During Suzuki-Miyaura Cross-coupling of Haloaryl and Haloalkenyl MIDA Boronic Ester

J. W. B. Fyfe, E. Valverde, C. P. Seath, A. R. Kennedy, J. M. Redmond, N. A. Anderson, and A. J. B. Watson, Chem.-Eur. J., 2015, 24, 8951–8964. [pdf] [Supporting Information]

Speciation Full Paper Abstract

 

19. Strategies Towards Chemoselective Suzuki-Miyaura Cross-Coupling

J. W. B. Fyfe  and A. J. B. Watson, Synlett (SynPACT), 2015, 26, 1139–1144. [pdf]

SynPACT Abstract

 

18. A Modular Synthesis of Functionalised Phenols Enabled by Controlled Boron Speciation

J. J. Molloy, R. P. Law, J. W. B. Fyfe, C. P. Seath, D. J. Hirst, and A. J. B. Watson, Org. Biomol. Chem.2015, 13, 3093-3102. [pdf] [Supporting Information]

Modular synthesis of phenol abstract

17. Chemoselective Boronic Ester Synthesis by Controlled Speciation

J. W. B. Fyfe, C. P. Seath, and A. J. B. Watson, Angew. Chem. Int. Ed.2014, 53, 12077-12080. [pdf] [Supporting Information]

Boron Speciation

 

16. Amidation of Esters with Amino Alcohols Using Organobase Catalysis

N. Caldwell, P. S. Campbell, C. Jamieson, F. Potjewyd,  I. Simpson, and A. J. B. Watson, J. Org. Chem., 2014, 79, 9347-9354. [pdf] [Supporting Information]

Amidation with Organobase

 

15. Development of chiral heteroleptic magnesium amides; asymmetric deprotonations mediated by six-membered metallocyclic amidomagnesium naphtholates

E. L. Carswell, William J. Kerr, Duncan McArthur, Marek Pazicky, A. J. B. Watson, Tetrahedron, 2014, 70, 7344-7349. [pdf]

Amidomagnesium phenolate abstract

 

14. Molar Efficiency: A Useful Metric to Gauge Relative Reaction Efficiency in Discovery Medicinal Chemistry

F. I. McGonagle, H. F. Sneddon, C. Jamieson, and A. J. B. Watson, ACS Sustainable Chem. Eng., 2014, 2, 523-532. [pdf] [Supporting Information]

MolEFigure

 

13. Synthesis of Functionalised 4H-Quinolizinones via Tandem Horner-Wadsworth-Emmons Olefination/Cyclisation

C. W. Muir, A. R. Kennedy, J. M. Redmond, and A. J. B. Watson, Org. Biomol. Chem., 2013, 11, 3337-3340. [pdf] [Supporting Information]

Quinolizinone Abstract
12. Development of a Solvent Selection Guide for Aldehyde-based Direct Reductive Amination Processes

F. I. McGonagle, D. S. MacMillan, J. Murray, H. F. Sneddon, C. Jamieson, and A. J. B. Watson, Green Chem., 2013, 15, 1159-1165. [pdf] [Supporting Information]

ReductiveAminationAbstract

 

11. Development of a Catalytic Ester Amidation Process

N. Caldwell, C. Jamieson, I. Simpson, and A. J. B. Watson, ACS Sustainable Chem. Eng., 2013, 1, 1339-1344. [pdf] [Supporting Information]

CatalyticAmidationAbstract

 

10. Evaluation of Alternative Solvents in Common Amide Coupling Reactions:Replacement of Dichloromethane and N,N-Dimethylformamide

D. S. MacMillan, J. Murray, H. F. Sneddon, C. Jamieson, and A. J. B. Watson, Green Chem., 2013, 15, 596-600. [pdf] [Supporting Information]

AmidationCommAbstract


9. Soft Scorpionates as Platforms for Novel Heterocycles

R. Rajasekharan Nair, A. Marckwordt, S. Lutta, M. Schwalbe, A. Biernat, D. R. Armstrong, A. J. B. Watson, A. R. Kennedy, J. Reglinski, and M. D. Spicer, Chem.-Eur. J., 2013, 19, 13561–13568. [pdf] [Supporting Information]

 

 

8. Replacement of Dichloromethane Within Chromatographic Purification: A Guide to Alternative Solvents

D. S. MacMillan, J. Murray, H. F. Sneddon, C. Jamieson, and A. J. B. Watson, Green Chem., 2012, 14, 3016-3019. [pdf] [Supporting Information]

 ChromatographyCommAbstract

 

7. Asymmetric Rhodium-Catalysed Addition of Arylboronic Acids to Acyclic Unsaturated Esters Containing a Basic delta-Amino Group.

N. A. Anderson, B. J. Fallon, E. Valverde, S. J. F. MacDonald, J. M. Pritchard, C. J. Suckling, and A. J. B. Watson, Synlett, 2012, 2817-2821. [pdf]

NAA Synlett abstract

 

6. Towards Energetically Viable Asymmetric Deprotonations: Selectivity at More Elevated Temperatures with C2-Symmetric Magnesium Bisamides

L. S. Bennie, W. J. Kerr, M. Middleditch, and A. J. B. Watson, Chem. Commun., 2011, 47, 2264-2266. [pdf] [Supporting Information]

C2ChemCommAbstract


5. New Potentially Chelating Chiral Magnesium Amide Bases for Use in Enantioselective Deprotontion Reactions

W. J. Kerr, M. Middleditch, and A. J. B. Watson, Synlett, 2011, 177-180. [pdf]

ChelationSynlettAbstract

 

4. Tuned methods for conjugate addition to a vinyl oxadiazole: synthesis of pharmaceutically important motifs

A. R. Burns, J. H. Kerr, W. J. Kerr, J. Passmore, L. C. Paterson, and A. J. B. Watson, Org. Biomol. Chem., 2010, 8, 2777-2783. [pdf] [Supporting Information]

OxadiazoleAbstract

 

3. Di-tert-Butylmagnesium as an Atom-efficient, Carbon-centred Base Reagent for the Preparation of Silyl Enol Ethers from Ketones

W. J. Kerr, A. J. B. Watson, and D. Hayes, Synlett, 2008, 1386-1390. [pdf]

tBu2MgAbstract

 


2. In situ Generation of Mes2Mg as a Non-nucleophilic Carbon-centred Base Reagent for the Efficient One-pot Conversion of Ketones to Silyl Enol Ethers

W. J. Kerr, A. J. B. Watson, and D. Hayes, Org. Biomol. Chem., 2008, 6, 1238-1243. [pdf]

Mes2MgAbstract


1. Bismesitylmagnesium: A Thermally Stable and Non-nucleophilic Carbon-centred Base Reagent for the Efficient Preparation of Silyl Enol Ethers

W. J. Kerr, A. J. B. Watson, and D. Hayes, Chem. Commun., 2007, 5049-5051. [pdf] [Supporting Information]

Mes2MgChemCommAbstract



Book Chapters

5. J. J. Molloy and A. J. B. Watson, "B-Protected Boronic Acids" in Boron Reagents in Synthesis (ACS Symposium Series): A. Coca, Ed., ACS, Chapter 12, pp 379-413 (DOI: 10.1021/bk-2016-1236.ch012).

4. C. Jamieson and A. J. B. Watson, "Application of Organocatalysis in Sustainable Synthesis" In Catalysis for Sustainability: Goals, Challenges, and Impacts: T. A. Umile, Ed., Taylor and Francis, Chapter 3, p 47-82.

3. A. J. B. Watson and D. W. C. MacMillan, “Iminium Catalysis” In Science of Synthesis Reference Library: Asymmetric Organocatalysis: B. List, Ed., Chapter 1.1.7, p 309-401.

2. A. J. B. Watson and D. W. C. MacMillan, “alpha-Functionalisation of Carbonyl Compounds (Not Enolate)” In Science of Synthesis: Stereoselective Synthesis 3: Stereoselective Pericyclic Reactions, Cross Coupling, and C-H and C-X Activation: P. A. Evans, Ed., Chapter 3.16, p 675-745.

1. A. J. B. Watson and D. W. C. MacMillan, "Iminium and Enamine Catalysis” In Catalytic Asymmetric Synthesis, 3rd ed.; I. Ojima, Ed., Chapter 2, p 39-57.