49667-91-6

Upstream product

• 118-48-9 isatoic anhydride 
• 2038-57-5 3-Phenylpropan-1-amine 
• 118-92-3 anthranilic acid 

Downstream Products

• 141306-04-9 3-(3-phenylpropyl)quinazolin-4(3H)-one 

Relevant academic research and scientific papers

Palladium-catalyzed atroposelective coupling-cyclization of 2-isocyanobenzamides to construct axially chiral 2-aryl- And 2,3-diarylquinazolinones

A palladium-catalyzed imidoylative cycloamidation of N-alkyl-2-isocyanobenzamides with 2,6-disubstituted aryl iodides, affording unprecedented axially chiral 2-arylquinazolinones, has been developed with good yields and atroposelectivities. In this coupling-cyclization process, the biaryl linkage and the heteroaromatic ring are formed sequentially in one step. When N-(2,4dimethoxyphenyl)-2-isocyanobenzamide is applied as a substrate, 2,3-diarylquinazolinones containing two stereogenic axes are produced with moderate diastereoselectivity and good enantioselectivities.

Design, synthesis, and evaluation of novel small molecule inhibitors of the influenza virus protein NS1

Influenza is a continuing world-wide public health problem that causes significant morbidity and mortality during seasonal epidemics and sporadic pandemics. The existing vaccination program is variably effective from year to year, and drug resistance to available antivirals is a growing problem, making the development of additional antivirals an important challenge. Influenza virus non-structural protein 1 (NS1) is the centerpiece of the viral response to the host interferon (IFN) system. NS1 was demonstrated previously to be a potential therapeutic target for antiviral therapy by the identification of specific small-molecule inhibitors. One inhibitory compound, NSC125044, was subjected to chemical evaluation. Initial synthetic work comprised simplifying the core structure by removing unwanted functionality and determination of key features important for activity. Several subclasses of molecules were designed and synthesized to further probe activity and develop the basis for a structure-activity relationship. Apparent potency, as judged by activity in virus replication assays, increased dramatically for some analogs, without cytotoxicity. Results suggest that the target binding site tolerates hydrophobic bulk as well as having a preference for weakly basic substituents.

2-ACYLAMINOBENZAMIDE DERIVATIVES AND PREVENTIVE AND REMEDY FOR DISEASES CAUSED BY THE SUPERMULTIPLICATION OF VASCULAR INTIMAL CELLS

The present invention relates to 2-acylaminobenzamide derivatives represented by the general formula: wherein R1, R2, R3, R4and R5represent each a hydrogen atom etc.; X represents a vinylene group etc.; B represents a group represented by the general formula: -N(R6)(R7)wherein R6and R7represent each a hydrogen atom etc., a group represented by the general formula: -NH-(CH2)n-A-R8wherein A represents a single bond etc.; R8represents a hydroxy group etc. or a hydroxyamino group which are useful as agents for the prevention and treatment of diseases caused by excessive proliferation of vascular intimal cells.

Synthesis and in vitro study of platelet antiaggregant activity of some 4-quinazolinone derivatives

Some new 4-quinazolinones were prepared. Their antiplatelet activity was evaluated in vitro with respect to aggregation induced by ADP, collagen, arachidonic acid and the platelet serotonin release reaction. Most molecules showed an inhibiting power similar to that of acetylsalicylic acid under the same conditions, and even greater when aggregation was induced by ADP. Reduction of the 4-quinazolinone derivatives to their 1,2,3,4-tetrahydroquinazoline homologues produced an increase in platelet inhibitory action except when ADP is the inductor.