University of Groningen
Exploring multicomponent reactions
Kroon, Edwin
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2017
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Kroon, E. (2017). Exploring multicomponent reactions: From chemistry to drug design. Rijksuniversiteit
Groningen.
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Behorende bij het proefschrift
Exploring Multicomponent Reactions
From Chemistry to Drug Design van Edwin Kroon
1. The ATP binding site of kinases is highly conserved throughout the kinome and developing selective modulators remains challenging after thirty years of research.
2. Asking to synthesize an enantiopure compound before publication of a manuscript would, in case of multicomponent reactions, be a PhD project on its own. Moreover, it is common practice to use chiral separating techniques for racemates in the pharmaceutical industry (Chapter 2).
3. β-Cyanoethyl isocyanide outperforms current known tetrazole protecting groups in terms of reaction conditions and reaction time (Chapter 3).
4. Multicomponent reaction chemistry is a powerful tool in the synthesis of complex scaffolds, however, synthesis of the scaffold can be as complex as the scaffold itself.
5. Application of α-CH-acidic imines (enolizable imines) would greatly improve the scope and usefulness of the Castagnoli reaction (Chapter 2).
6. Column chromatography (silica/methanol) is insufficient to properly elute a sulfocarboxylic acid. See: Jariwala, F. B., Wood, R. E., Nishshanka, U. & Attygalle, A. B. Formation of the bisulfite anion (HSO3–, m/z 81) upon collision-induced dissociation of anions derived from organic sulfonic acids. J.
Mass Spectrom. 47, 529–538 (2012) and Chapter 4.
7. Writing the full IUPAC name as part of an article title is unnecessary and does not add to the purpose of a title.
For example: Venkatraman, S. et al. Discovery of (1R,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-diox-opropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dime-thyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection. J. Med. Chem. 49, 6074–6086 (2006).
8. Labnesia is a benign form of amnesia that spontaneously develops in healthy lab members when some-thing happens in the lab (e.g., some expensive glassware is broken), but no one did it. After the event has taken place and ‘forgotten,’ all those affected are cured.
9. “It is good to have an end to journey toward; but it is the journey that matters, in the end.” – Ernest Hemingway.
