137225-33-3

Upstream product

• 72544-42-4 2-(2-chloropropionylamino)benzoic acid methyl ester 
• 64-17-5 ethanol 
• 7623-09-8 2-chloropropionyl chloride 
• 118-92-3 anthranilic acid 

Downstream Products

• 137225-34-4 2-(1-chloroethyl)benzopyrimidin-4(3H)-one 
• 137225-44-6 2-Chloro-N-[2-(3,4-dimethyl-benzoyl)-phenyl]-propionamide 
• 137225-45-7 3-Benzyl-2-(1-chloro-ethyl)-3H-quinazolin-4-one 
• 137225-46-8 2-(1-Chloro-ethyl)-3-phenylamino-3H-quinazolin-4-one 
• 137225-47-9 2-(2-chloropropanamido)-N-phenylbenzamide 
• 137225-42-4 N-Benzyl-2-(2-chloro-propionylamino)-benzamide 
• 137225-41-3 4-benzylimino-2-(1-chloroethyl)-3H-quinazoline 
• 137225-39-9 2-(1-Chloro-ethyl)-3-{[1-(4-chloro-phenyl)-meth-(E)-ylidene]-amino}-3H-quinazolin-4-one 
• 602318-76-3 2-(1-chloroethyl)-3-(4-methoxyphenyl)-3H-quinazolin-4-one 

Relevant academic research and scientific papers

FUSED-RING PYRIMIDIN-4(3H)-ONE DERIVATIVES, PROCESSES FOR THE PREPARATION AND USES THEREOF

AbstractNovel compounds of the following formula (I) and pharmacologically acceptable salt and esters thereof can modulate LXR function and as a result show excellent anti-arteriosclerotic and anti-inflammatory activity:wherein:A represents aryl or heteroaryl;R1, R2 and R3 are the same or different and each represents hydrogen, hydroxyl, nitro, cyano, amino, halogen, carboxy, carbamoyl, mercapto, alkyl, haloalkyl, alkylcarbonyloxy, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, dialkylamino, alkylcarbonylamino, N-(alkylcarbonyl)-N-(alkyl)amino, alkoxycarbonylamino, N-(alkoxycarbonyl)-N-(alkyl)amino, alkylsulfonylamino, N-(alkylsulfonyl)-N-(alkyl)amino, haloalkylsulfonylamino, N-(haloalkylsulfonyl)-N-(alkyl)amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl group, or R1 and R2 together are alkylenedioxy;R4 and R5 are the same or different and each represents hydrogen, hydroxyl, amino, halogen, mercapto, alkyl, haloalkyl, alkoxy, alkoxycarbonyl or alkylthio;X represents hydrogen, hydroxyl, halogen, alkoxy or haloalkoxy; andY represents an optionally substituted alkyl, cycloalkyl, heterocyclyl, aryl, cycloalkylalkyl, heterocyclylalkyl or aralkyl group.

QUINAZOLINONE MODULATORS OF NUCLEAR RECEPTORS

Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.

Synthesis and some reactions of 2-(1-chloroethyl)-3,1-benzoxazin-4(H)-one

2-(1-Chloroethyl)-3,1-benzoxazin-4(H)-one (II) reacts with ammonia to give the corresponding quinazolone (III) which on alkylation provides 3-N-alkyl quinazolones (IVa,b).Quinazolone III undergoes Mannich reaction with formaldehyde to give the Mannich base (V).It also reacts with P2S5 to give quinazole-4-thione (VI).The benzoxazinone II also reacts with hydrazines to give 3-aminoquinazolones (VIIa,b) which undergo condensation with p-chlorobenzaldehyde to afford the schiff base (VIII).Amonolysis of II gives the anilides (XIa,b) which undergo ring closure with Ac2O to give the quinazolone IVb.Reaction of II with P2S5 gives the benzothiazinone (XII) which reacts with benzylamine to give IVb.Reaction of II with hydrocarbons under Friedel Crafts conditions furnishes the phenyl aryl ketone derivatives (XIIIa,b).