Prof. Pierre De Clercq was a Professor at Ghent University from 1989 to 2013. Since his retirement, he is now active as a part time research Professor (5%), following up some ongoing collaborative projects. He was born in Ghent in 1948, and obtained a MSc degree in chemistry at Ghent University in 1969, where he also earned his doctoral degree in organic synthesis in 1973, working under the advisorship of Prof. Maurits Vandewalle. He held postdoctoral appointments at the University of California (Santa Cruz) working with Prof. John E. McMurry (1974-75), and at the University Chemical Laboratories in Cambridge working with Prof. Ralph Raphael (1977). For 20 years (1969-1989), he has conducted his scientific career as a research fellow of the Research Foundation-Flanders (NFWO, later FWO). During that period, he authored more than 75 research papers, and has been a visiting Professor at the Free University of Brussels (1984−86) and at the Catholic University of Leuven (1987−88). In 1989, he joined the faculty at Ghent University as Professor, and was promoted to Full Professor in 1994. He was Head of the organic chemistry department from 2002 until 2012. Up until now, he has published over 150 publications in peer-reviewed journals. He has been a promotor of 39 PhD students and also advised many Master students and postdocs.

His earlier work focused on natural product total synthesis and conformational analyses of ring systems, mostly in the terpene series, and is characterized by highly step economical approaches to several important classes of natural products, such as (pseudo)guaianolides, 11-oxo-steroids and gibberellic acids. Some of these routes have stood the test of time and remain the shortest entries to these terpenoid natural products available to this day. In later work, he became more closely involved with biology and focused on the synthesis of analogues of vitamin D3 (calcitriol) and enediyne antibiotic-inspired scaffolds for applications in cancer therapies. He also investigated analogues of himbacine for applications in the treatment of neurodegenerative diseases. In collaboration with the group of Prof. Maurits Vandewalle, his group produced over 400 conformationally constrained analogs of calcitriol through both partial and total synthesis approaches, several of which are still part of ongoing research, including phase II clinical trials. He also had an active interest in enzyme catalysed processes, especially the cationic polyene cyclisation reactions involved in terpene biosynthesis.

Representative total syntheses

(±)-desmethyl-dehydrohimgravine

1995 (with Govert De Baecke)
Studies directed towards the total synthesis of (±)-himbacine

(±)-periplanone B

1994 (with Tom De Geyter and Serge Cauwberghs)
Total Synthesis of Periplanone-B Via Intramolecular Diels-Alder Reaction with Furan-Diene and Allene-Dienophile

(+)-biotin

1993 (with Frederik Deroose)
A novel enantioselective synthesis of (+)-biotin

(±)-gibberellin A5

1986 (with Werner Grootaert)
A novel expeditious entry into gibberellins. The total synthesis of (±)-GA5

(±)-andrenosterone

1985 (with Luc Van Royen and Roelant Mijngheer)
Intramolecular diels-alder reaction with furan-diene: Total synthesis of (±)-11-ketotestosterone and (±)-adrenosterone

(±)-prostaglandin F1α

1974 (with Maurits Vandewalle, PhD work)
Cyclopentanones. X A novel synthesis of (dl)-prostaglandin F1α

Representative medicinally oriented synthetic work

Analogs of 1α,25-dihydroxyvitamin D

The development of CD-ring modified analogs of 1α,25-dihydroxyvitamin D

Himbacine-related analogues

Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists

Estramycins

Estramycins: A New Diyl Precursor Family Derived from Estradiol

Representative synthetic work on enzyme model studies

Application of Combinatorial Procedures in the Search for Serine-Protease-Like Activity with Focus on the Acyl Transfer Step

A Model for the Nonenzymatic BCD Cyclization of Squalene

Polyene Cyclizations Related to Oxidosqualene Cyclization. A Model for the Anti-Markovnikov Closure of Ring C

Graduated PhD students

  1. Duchan Laplace (2014) “Total synthesis of biologically active polycyclid terpenoids: frondosanes, liphaganes, guaianolides, zizaanes and calcitriols”
  2. Frederik De Buysser (2008) "Development of spirocyclic vitamin D3 analogs with potential dissociation of biological activities"
  3. Garrett Minne (2008) "Development of decalin analogues of calcitriol"
  4. Freek Vrielynck (2008) "Development of analogues of calcitriol with an enforced side-chain orientation"
  5. Johan Winne (2007) "Synthesis and polycyclisation of analogues of oxidosqualene with a preformed C-ring"
  6. Jo D'Herde (2005) "Development of a solid-phase Julia olefination method for applications in the parallel synthesis of vitamin D3 analogues"
  7. Samuel Demin (2004) "Development of CE-ring type analogues of 1α,25-dihydroxyvitamin D3"
  8. Wim Schepens (2004) "Development of CD-ring modified vitamin D3 analogues with an enforced side-chain orientation: spirocyclic CF-ring analogues"
  9. Pol Lombaert (2003) "Novel approaches for the total synthesis of (-)- Periplanone B: intramolecular Diels-Alder reaction and ring closing metathesis"
  10. Nadia Farcy (2002) "Efforts towards the synthesis of a tripodal library for the discovery of serine-protease mimics"
  11. Vanessa Daelman (2002) "Stepwise development of a non-enzymatic hydrolase based on carbohydrate derivatives"
  12. Ibrahim Murad (2002) "The development of CD-ring modified analogues of 1α,25-dihydroxyvitamin D3 prossessing a trans-decalin structure"
  13. Sandra Claeys (2001) "Total synthesis of 11-oxosteroids via an intramolecular Diels-Alder reaction with a furan diene as a key step"
  14. Jean-Baptiste Joos (2001) "Contribution to the total synthesis of (+)-biotin"
  15. Gunther Van Cauwenberghe (2001) "Synthesis of analogues of (+)-himbacine as a muscarin receptor antagonist"
  16. Hilde De Muynck (2000): "The development of model compounds with serine protease-like activity via combinatoriol techniques"
  17. Hilde Van Dingenen (2000) "Development of trans-fused CE-ring type analogues of vitamin D3"
  18. Christel Meert (2000): "The development of novel cycloaromatisation precursors based on the oestradiol scaffold"
  19. Sven Hofman (2000): "Synthesis of H-himbacine, a muscarin receptor antagonist"
  20. Stefan Gabriëls (2000): "Development of analogues of vitamin D3 with an enforced side-chain orientation"
  21. Mario Sey (2000): "Study of the cyclisation of conformationally anchored analogues of squalene"
  22. Annemieke Madder (1997): "Stepwise development of non-enzymatic hydrolases"
  23. Xiaoming Zhou (1997): "A symmetric synthesis of 1α,25-dihydroxyvitamin D analogs modified in the C-ring"
  24. Karla Berckmoes (1997): "Synthesis and cyclisation of model compounds of 2,3-epoxysqualeen"
  25. Govert De Baecke (1995): "Contribution to the total synthesis of himbacine"
  26. Johny De Schrijver (1994): "Study for the total synthesis of 1(S),25-dihydroxyvitamine D3 derivatives with an A-ring assembly via a Diels-Alder reaction of a furan diene and an allene dienophile"
  27. Frederik Deroose (1994): "Study for the total synthesis of (+)-biotin"
  28. Jing Wang (1994): "The synthesis of novel cycloaromatization precursors incorporating estradiol"
  29. Frank Nuyttens (1994): "Biomimetic approach towards the total synthesis of gibberellins via intramolecular Diels-Alder reaction with furan diene"
  30. Tom De Geyter (1994): "Study for the total synthesis of (-)-periplanone B"
  31. Ivan Steels (1993): "Study of the use of anchoring groups in the design of model compounds for serine protease activity and chiral inductors for the stereoselective reduction of prochiral ketones"
  32. Gui-Dong Zhu (1993): "Synthesis of fluorine substituted and of D-ring modified analogues of vitamin D for modulation of the biological activity"
  33. Filip De Corte (1992): "Study of the use of anchoring groups in the design of chiral inductors and for the control of intramolecular Diels-Alder reactions"
  34. Jan Hoflack (1991): "Part I. Computer methods for the conformational analysis of polycyclic compounds starting from a two dimensional structure diagram. Part II. Initial study towards a biomimetic total synthesis of gibberellin plant growth hormones via an intramolecular Diels-Alder reaction with a furan diene"
  35. Serge Cauwberghs (1989): "The intramolecular Diels-Alder reaction with furan diene and allene dienophile; a novel approach to the synthesis of (±)-periplanone B"
  36. Patrick Missiaen (1988): "Study for the total synthesis of steroids via: 1. intramolecular Diels-Alder reaction with furan diene and allene dienophile; 2. Cation olefin cyclisation"
  37. Werner Grootaert (1986): "The intramolecular Diels-Alder reaction with furan diene: a novel approach to (±)-gibberellins"
  38. Luc Van Royen (1984): "The intramolecular Diels-Alder reaction with furan diene. A novel approach to (±)-11-ketosteroids"
  39. Berthold Simmons (1983): "Contribution to the total synthesis of diterpenes of the aphidicolin and stemodine series"