Synthesis of Highly Substituted Imidazole Uracil Containing Molecules via Ugi-4CR and Passerini-3CR | Zendy

Rudrakshula Madhavachary | Zendy; Tryfon ZarganesTzitzikas | Zendy; Pravin Patil | Zendy; Katarzyna Kurpiewska | Zendy; Justyna KalinowskaTłuścik | Zendy; Alexander Dömlingꝉ | Zendy

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Synthesis of Highly Substituted Imidazole Uracil Containing Molecules via Ugi-4CR and Passerini-3CR

Author(s) -

Rudrakshula Madhavachary,

Tryfon ZarganesTzitzikas,

Pravin Patil,

Katarzyna Kurpiewska,

Justyna KalinowskaTłuścik,

Alexander Dömlingꝉ

Publication year - 2018

Publication title -

acs combinatorial science

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.928

H-Index - 81

eISSN - 2156-8952

pISSN - 2156-8944

DOI - 10.1021/acscombsci.7b00145

Subject(s) - chemistry , imidazole , uracil , combinatorial chemistry , molecule , thymine , sequence (biology) , stereochemistry , organic chemistry , biochemistry , dna

The synthesis of uracil/thymine containing tetra/trisubstituted imidazole derivatives was demonstrated using Ugi/Passerini-reaction followed by a postcyclization reaction sequence. The approach enables the one-pot facile construction of diverse compounds in moderate to excellent yields (47-82%). The 5-fluorouracil and 5-methyluracil moieties afford potentially bioactive molecules with drug-like properties. These scaffolds are currently being utilized in the screening deck of the European Lead Factory.

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