Microwave assisted synthesis of 2,3-dihydro-4H-benzo[4,5]thiazolo[3,2-a]furo[2,3-d]pyrimidin-4-ones and 6,7-dihydro-5H-furo[2,3-d]thiazolo [3,2-a]pyrimidin-5-ones using Mn(OAc)(3)


Ustalar A., YILMAZ M.

TETRAHEDRON LETTERS, cilt.58, ss.516-519, 2017 (SCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 58 Konu: 6
  • Basım Tarihi: 2017
  • Doi Numarası: 10.1016/j.tetlet.2016.12.067
  • Dergi Adı: TETRAHEDRON LETTERS
  • Sayfa Sayıları: ss.516-519

Özet

2-Hydroxy-4H-benzo[4,5]thiazolo[3,2-a]pyrimidin-4-one 2a and 7-hydroxy-511-thiazolo[3,2-a]pyrimidin-5-one 2h, were obtained in high yields under mild conditions from the cyclization reactions of bis-(2,4,6-trichlorophenyl) malonate and 2-aminobenzothiazole or 2-aminothiazole, respectively. A new class of compounds, 2,3-dihydro-4H-benzo[4,5]thiazolo[3,2-a]furo[2,3-d]pyrimidin-4-ones and 6,7-dihydro-5H-furo[2,3-d]thiazolo[3,2-a]pyrimidin-5-ones, were synthesized via the microwave assisted radical addition of compounds 2a and 2b to various alkenes using manganese(III) acetate. A preliminary acetylcholine esterase (AchE) inhibition test of compound 4e showed excellent (92%) inhibitory potential, comparable with the standard drug Donapezi (R). (C) 2016 Elsevier Ltd. All rights reserved.