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

Molecules

Irina O. Zhuravel¹  Sergiy M. Kovalenko²  Sergiy V. Vlasov² 

[1] id="af1-molecules-10-00444">National Pharmaceutical University, Kharkiv, Ukrai

关键词: Coumarin derivatives;    2-aminothiazole derivatives;    dicarboxylic acids;    combinatorial synthesis.;   

DOI  :  10.3390/10020444

来源: mdpi

【 摘 要 】

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.

【 授权许可】

Unknown   
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