7-(ARILAMINO)-2,3-DIGIDROPIRROLO[2,1-b]XINAZOLIN-9(1H)-ON HOSILALARINING SINTEZI
Keywords:
Pd2(dba)3, DavePhos, aril va getero aminlar, dioksan, natriytetra butoksidAbstract
7-bromo-2,3-digidropirrolo[2,1-b]xinazolin-9(1H)-onga aril, geteroaril aminlar bilan aminlanish reaksiyalari natijasida 7-(fenilamino)-2,3-digidropirrolo[2,1-b]xinazolin-9(1H)-onning hosilalari sintez qilingan. Turli katalizatorlar, ligandlar, asoslar va erituvchilar bilan reaksiya sharoitlarini optimallashtirish amalga oshirildi. Pd2(dba)3 ning DavePhos (L3) bilan kombinatsiyasi 100oC da 1,4-dioksanda t-BuONa ishtirokida 8 soat davomida qaytarish reaksiyalari olib borildi va reaksiyaning unumi eng yaxshi ekanligi aniqlandi.
References
1. Henriksen, S. and U. Soerensen, 2-Chloroquinazoline: Synthesis and Reactivity of a Versatile Heterocyclic Building Block. Cheminform, 2007. 38.
2. Garlapati, R., et al., Pd-catalyzed amination of 6-halo-2-cyclopropyl-3-(pyridyl-3-ylmethyl) quinazolin-4(3H)-one. Tetrahedron Letters, 2012. 53(38): p. 5162-5166.
3. Nowak, M., et al., Substituted benzoquinazolinones. Part 1: Synthesis of 6-aminobenzo[h]quinazolinones via Buchwald–Hartwig amination from 6-bromobenzo[h]quinazolinones. Tetrahedron, 2014. 70(34): p. 5153-5160.
4. Zhang, Z., et al., Design, synthesis, and biological screening of a series of pyrazolo [1,5-a]quina-zoline derivatives as SIRT6 activators. European Journal of Pharmaceutical Sciences, 2023. 185: p. 106424.
5. Moheb, M., et al., Synthesis and bioactivities evaluation of quinazolin-4(3H)-one derivatives as α-glucosidase inhibitors. BMC Chemistry, 2022. 16(1): p. 97.
6. Scheufler, C., et al., Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket. ACS Medicinal Chemistry Letters, 2016. 7(8): p. 730-734.
7. Du, K., et al., Design, synthesis, and cytotoxic activities of isaindigotone derivatives as potential anti-gastric cancer agents. Journal of Enzyme Inhibition and Medicinal Chemistry, 2022. 37(1): p. 1212-1226.
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