Synthesis and antimicrobial evaluation of 3-(4-arylthieno[2,3-d]pyrimidin-2-yl)- 2H-chromen-2-ones

Heterocyclic communications

article

Sergiy V. Vlasov¹  Sergiy M. Kovalenko²  Pavlo E. Shynkarenko³  Konstantin Yu. Krolenko⁴  Vitaliy S. Vlasov⁵ 

[1] Organic Chemistry Department, National University of Pharmacy;Organic Chemistry Department, V. N. Karazin Kharkiv National University;Enamine Ltd.;Medicinal Chemistry Department, National University of Pharmacy;Pharmacoinformatics Department, National University of Pharmacy

关键词: arylation;    coumarin;    coupling;    rearrangement;    thiophene;   

DOI  :  10.1515/hc-2018-0013

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

Syntheses of 3-(4-arylthieno[2,3- d ]pyrimidin-2-yl)-2 H -chromen-2-ones 5 by the reaction of 2-iminocoumarin-3-carboxamides 1 with (2-aminothiophen-3-yl)(aryl)methanones 2 and by the alternative Suzuki coupling of 4-chlorothieno[2,3- d ]pyrimidin-2-yl-2 H -chromen-2-one 7 with arylboronic acids were developed. Compound 5d showed higher antimicrobial activity against Staphylococcus aureus than the reference drug streptomycin.

【 授权许可】

CC BY|CC BY-NC-ND