107288-96-0

Upstream product

• 631861-00-2 N-(2-benzoylphenyl)butyramide 
• 141-75-3 butyryl chloride 
• 1885-29-6 anthranilic acid nitrile 
• 2835-77-0 (2-aminophenyl)(phenyl)methanone 
• 13047-06-8 o-bromobenzophenone 
• 3020-81-3 butylamidine hydrochloride 
• 4765-54-2 2-propyl-3H-quinazolin-4-one 
• 1448311-40-7 C₁₈H₁₈N₂O₃S 
• 98-80-6 phenylboronic acid 
• 3958-47-2 triphenylindium 
• 4250-81-1 1-phenyl-1-pentyne 
• 5439-98-5 2-phenyl-2,3-dihydro-phthalazine-1,4-dione 

Relevant academic research and scientific papers

Design, synthesis and molecular properties prediction of novel quinazoline derivatives as potent antibacterial agents

A novel series of compounds were synthesized by C-C bond formation of substituted quinazolinones (1) with substituted boronic acids (2) to get 2,4-disubstituted quinazoline (3a-3n) in good to excellent yields. The structures of the new compounds were confirmed by IR, 1H NMR, 13C NMR and mass spectral data. An antibacterial and antifungal activity screening results showed that compounds 3b, 3e, 3i and 3l possess excellent activity against Gram (+), Gram (-) bacteria (S. aureus, Klebsiella species, P. aeruginosa) compared to standard drugs. 3l, 3g and 3n showed better antifungal activity against A. nigeri and C. albicans organisms. In this investigation, the target compounds 3a-3n were subjected to in silico molecular properties prediction and drug likeness by employing Molinspiration (Molinspiration, 2014) and MolSoft (MolSoft, 2007) property explorer tool kits for predicting their high oral bioavailability.

Ru(II)-Catalyzed C-H Activation and Annulation Reaction via Carbon-Carbon Triple Bond Cleavage

An unprecedented Ru(II)-catalyzed C-H activation and annulation reaction, which proceeds via C-C triple bond cleavage, is reported. This reaction of 2-phenyldihydrophthalazinediones with alkynes, which works most efficiently in the presence of bidented ligand 1,3-bis(diphenylphosphino)propane, affords good yields of substituted quinazolines.

Palladium-Catalyzed Cross-Coupling of 4-Tosyloxyquinazolines with Organoindium Reagents: An Efficient Route to 4-Substituted Quinazolines

An efficient route to 4-substituted quinazolines by arylation or alkylation of quinazolinones under mild conditions is described. 4-Tosyloxyquinazolines were obtained through the reaction of quinazolinones and p-methylbenzenesulfonyl chloride in the presence of K2CO3. The cross-coupling reaction of 4-tosyloxyquinazolines with organoindium reagents, carried out in tetrahydrofuran, catalyzed by Pd2(dba)3/ (2-furyl)3P led to the formation of 4-functionalized quinazolines in good to excellent yields. Higher yields were obtained by the one-pot reaction of quinazolinone, p-methylbenzenesulfonyl chloride, Pd2(dba)3-/(2-furyl)3P, and organoindium reagent. These methods using organoindium compounds as coupling partners provided an efficient route to 4-(hetero)aryl/alkylquinazolines, especially 4-substituted quinazolines bearing a halogen scaffold.

Synthesis of 4-arylquinazolines by arylation of quinazolin-4-ones under mild conditions

An efficient route to 4-arylquinazolines via arylation of quinazolin-4-ones under mild condition is described. The reaction is carried out by the palladium-catalyzed coupling of quinazolin-4-ones with arylboronic acids in the presence of TsCl leading to 4-arylquinazolines in good to excellent yields. Georg Thieme Verlag Stuttgart New York.

Highly efficient copper-catalyzed cascade synthesis of quinazoline and quinazolinone derivatives

We have developed a general and highly efficient copper-catalyzed method for synthesis of quinazoline and quinazolinone derivatives, the target products were obtained in good to excellent yields via cascade reactions of amidine hydrochlorides with substituted 2-halobenzaldehydes, 2-halophenylketones, or methyl 2-halobenzoates, and the method is of simple, economical and practical advantages. The Royal Society of Chemistry 2008.

SYNTHESIS OF QUINAZOLINES

Grignard reagents reacted with 2-aminobenzonitrile to give the intermediate (10), which readily could be cyclized to quinazolines by reaction with carbonyl compounds (e.g. acid chlorides, anhydrides, formates and oxalates).The intermediate (10) and aldehy