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Molecules 2005, 10(2), 444-456; doi:10.3390/10020444
Article

Solution-phase Synthesis of a Combinatorial Library of 3-[4-(Coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid Amides

* , ,  and
National Pharmaceutical University, Kharkiv, Ukraine
* Author to whom correspondence should be addressed.
Received: 27 August 2004 / Revised: 23 December 2004 / Accepted: 24 December 2004 / Published: 28 February 2005
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Abstract

The parallel solution-phase synthesis of a new combinatorial library of 3-[4-(R1-coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid amides 9 has been developed. The synthesis involves two steps: 1) the synthesis of core building blocks – 3- [4-(coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acids, 6 – by the reaction of 3-(ω-bromacetyl)coumarins 1 with 3-amino(thioxo)methylcarbamoylpropanoic acid (5); 2) the synthesis of the corresponding 3-[4-(coumarin-3-yl)-1,3-thiazol-2-yl- carbamoyl]propanoic acids amides 9 using 1,1’-carbonyldimidazole as a coupling reagent. The advantages of the method compared to existing ones are discussed.
Keywords: Coumarin derivatives; 2-aminothiazole derivatives; dicarboxylic acids; combinatorial synthesis. Coumarin derivatives; 2-aminothiazole derivatives; dicarboxylic acids; combinatorial synthesis.
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Zhuravel, I.; Kovalenko, S.; Vlasov, S.; Chernykh, V. Solution-phase Synthesis of a Combinatorial Library of 3-[4-(Coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid Amides. Molecules 2005, 10, 444-456.

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