Pd-catalyzed amination of 6-halo-2-cyclopropyl-3-(pyridyl-3-ylmethyl) quinazolin-4(3H)-one |
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| Authors: | Ramesh Garlapati Narender Pottabathini Venkateshwarlu GurramAvinash B Chaudhary Venkata Rao Chunduri Balaram Patro |
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| Institution: | a Medicinal Chemistry Division, GVK Biosciences Pvt. Ltd., 28A, IDA Nacharam, Hyderabad 500076, AP, India
b Organic Chemistry Division, Department of Chemistry, Sri Venkateshwara University, Tirupathi 517 502, AP, India |
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| Abstract: | 6-Halo-2-cyclopropyl-3-(pyridyl-3-ylmethyl) quinazolin-4(3H)-one derivatives have been synthesized and utilized for amination reactions with aryl, heteroaryl and alkyl amines. Optimization of reaction conditions with different catalysts, ligands, bases, and solvents was conducted. The combination of Pd2(dba)3 with DavePhos (L3) proved to be best for these conversions in the presence of NaOtBu in 1,4-dioxane at 100 °C. The relative reactivities of 6-bromo and 6-chloro-2,3-disubstitued quinazolinones with p-toluidine were conducted and as anticipated the 6-bromo analogue was totally consumed and 6-chloro derivative was completely unreactive. |
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| Keywords: | UPFCZJXNJPKWAU-UHFFFAOYSA-N |
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