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A Dömling

Publications and source records attributed to A Dömling.

6 recordsLinked to original sources
PubMed2001

A novel three-component butenolide synthesis.

[reaction: see text]. 5-Acylamino butenolides can be assembled by a multicomponent reaction (MCR) of isocyanides, glyoxals, and acetophosphonic acid diethylesters, followed by a intramolecular Wittig-type reaction. The reaction can be performed either in one pot or with the isolation of the intermediate Passerini product. This versatile reaction offers three independent inputs displayed in the final product. Applications in combinatorial chemistry and natural product synthesis can be envisioned.

4-Butyrolactone↗
PubMed2000

Multicomponent Reactions with Isocyanides.

Multicomponent reactions (MCRs) are fundamentally different from two-component reactions in several aspects. Among the MCRs, those with isocyanides have developed into popular organic-chemical reactions in the pharmaceutical industry for the preparation of compound libraries of low-molecular druglike compounds. With a small set of starting materials, very large libraries can be built up within a short time, which can then be used for research on medicinal substances. Due to the intensive research of the last few years, many new backbone types have become accessible. MCRs are also increasingly being employed in the total synthesis of natural products. MCRs and especially MCRs with isocyanides offer many opportunities to attain new reactions and basic structures. However, this requires that the chemist learns the "language" of MCRs, something that this review wishes to stimulate.

Journal Article↗
PubMed2000

One-pot synthesis and biological evaluation of aspergillamides and analogues.

A one-pot total synthesis of aspergillamide and analogues by a solution phase Ugi multi component reaction (MCR) is described. The reaction is easily performed in 96-well plates and offers a facile access to diverse aspergillamide analogue compound libraries. The antibiotic and cytotoxic activity of these compounds is measured. Several of them are more potent than the natural product.

Anti-Bacterial Agents↗
PubMed2000

The discovery of new isocyanide-based multi-component reactions.

Multi-component reactions are finding increasing use in the discovery process of new drugs and agrochemicals. Some years ago they were considered as highly exotic types of organic reactions. Recently, many groups have realized that the field of multi-component reactions is full of new opportunities. These comprise fast and efficient production of small-molecular-weight compound libraries, highly atom-economic chemistry, very large chemical libraries, improvements in total synthesis, and applications in bioconjugate chemistry, as well as in related fields (e.g. chemical biology).

Combinatorial Chemistry Techniques↗
PubMed1998

Isocyanide based multi component reactions in combinatorial chemistry.

Although usually regarded as a recent development, the combinatorial approach to the synthesis of libraries of new drug candidates was first described as early as 1961 using the isocyanide-based one-pot multicomponent Ugi reaction. Isocyanide-based multi component reactions (MCR's) markedly differ from their usual two component counterparts. In the context of combinatorial chemistry, they offer more structural variations, more accessible compounds and more diversity than any other previously known reaction. This review examines the history of isocyanide based MCR's and their applicability in combinatorial chemistry.

Chemistry, Pharmaceutical↗