solution-phase synthesis of a combinatorial library of 3-[4-(coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid amides组合库的液相合成3 -[4 -(coumarin-3-yl)1,3-thiazol-2-ylcarbamoyl]丙酸酰胺.pdfVIP

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solution-phase synthesis of a combinatorial library of 3-[4-(coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid amides组合库的液相合成3 -[4 -(coumarin-3-yl)1,3-thiazol-2-ylcarbamoyl]丙酸酰胺.pdf

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solution-phase synthesis of a combinatorial library of 3-[4-(coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid amides组合库的液相合成3 -[4 -(coumarin-3-yl)1,3-thiazol-2-ylcarbamoyl]丙酸酰胺

Molecules 2005, 10, 444–456 molecules ISSN 1420-3049 Solution-phase Synthesis of a Combinatorial Library of 3-[4- (Coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid Amides Irina O. Zhuravel *, Sergiy M. Kovalenko, Sergiy V. Vlasov and Valentin P. Chernykh National Pharmaceutical University, Kharkiv, Ukraine * Author to whom correspondence should be addressed; E-mail: kosn@ic.kharkov.ua Received: 27 August 2004; in revised form: 23 December 2004 / Accepted: 24 December 2004 / Published: 28 February 2005 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. Introduction 2-Aminothiazole derivatives are widely used as pharmaceuticals. For example, Talipexol [1] and Pramipexole [2] with a 2-aminothiazole moiety are used as antiparkinsonian drugs and dopami