Synthesis and Biological Evaluation of Allenic Quinazolines Using Palladium‐Catalyzed Hydride‐Transfer Reaction.

Abstract

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Synthesis and Reactivity of Propargylamines in Organic Chemistry

“…On the basis of the same principle of anion equivalency, the same authors attempted to introduce allenic groups into the backbone of pharmacologically active molecules in order to produce new pharmacological properties. 581 Allenic quinazolines 1029 were synthesized from the coupling of corresponding iodides 1027 and dicyclohexyl-propargylamine via Sonogashira/hydrogen-transfer reactions (Scheme 201).…”

Hexachlorocyclotriphosphazene (HCCP)-Mediated Direct Formation of Thioethers and Ethers from Quinazolin-4(3H)-ones

“…They have attracted interest in the past because of their varied biological activities, such as anticonvulsant, antihypertensive, vasodilator, antiinflammatory, antibiosis, fibrinogen receptor antagonistic and nanomolar Hedgehog-antagonistic properties [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 ]. Among the family of quinazolines, quinazoline (thio)ethers, including 4-arylthioquinazolines and 4-aryloxyquinazolines, have received considerable interest because of their potential pharmacological activity [ 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 ].…”

“…Generally, 4-arylthioquinazolines and 4-aryloxyquinazolines are obtained through S N Ar substitution of electron-deficient 4-chloroquinazolines with the appropriate thiophenols or phenols in the presence of a base [ 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 ]. The common method for preparation of 4-chloroquinazolines is the chlorination of corresponding quinazolin-4(3 H )-ones.…”