Quinazolinones are interesting molecules with a wide range of biological activities. We prepared a number of quinazolinone derivatives by the condensation of 5-bromo- or 5-nitro-substituted anthranilic acids with chloro-acyl chlorides. Anthranilic acid derivatives were treated with either 3-chloro-propionyl chloride or 4-chloro-butyryl chloride to yield the corresponding N-acyl-anthranilic acid...

HIE-124 is the new member of ultra-short acting hypnotics drug family. In this research, thiadiazole can act as the bio-isosteric replacement of thiazole in synthesized compounds as HIE-124 derivatives. HIE-124 drug, in which the heterocyclic thiazole ring replaced to thiadiazole, will be presented. Thiadiazolodiazepines were synthesized by a two-step reaction starting from the amino thiadiazol...

Reaction of thionyl chloride with 7-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid 1 gave acid chloride 2. Compound 2 was reacted with glycine and D-glutamic acid to afford 2-(7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4- dihydroquinoline-3-carbonyl) aminopantandioicacid 3a and 2-(7-chloro-1-cyclopropyl-6- fluoro -4- oxo-1,4-dihydroquinoline-3-carbonyl)aminoacetica...

The reaction of 4,5-dichloro-1,2,3-dithiazolium chloride with 2-(phenylsulfonyl)acetonitrile (1 equiv) in the presence pyridine (2 gave S-(3-chloro-5-cyanoisothiazol-4-yl)benzenesulfonothioate and (Z)-2-(4-chloro-5H-1,2,3-dithiazol-5-ylidene)-2-(phenylsulfonyl)acetonitrile 19% 23% yield, respectively. compounds were fully characterized mechanistic rationale is proposed for formation benzensulfo...

Mixed crystals of 1-(4-chlorophenylsulfonyl)-2,5-dimethyl-1 H -benzimidazole and 1-(4-chlorophenylsulfonyl)-2,6-dimethyl-1 (ratio 0.707:0.293; two molecules in the asymmetric unit), 0.707C 15 13 ClN 2 O S·0.293C S, ( I ), 2- n -butyl-1-(4- tert -butylphenylsulfonyl)-5-chloro-1 -butylphenylsulfonyl)-6-chloro-1 [ratio 0.731 (2):0.269 (2); one molecule unit], 0.731C 21 25 S·0.269C II were obtained...

Conjugate addition reaction of various nucleophiles across the vinyl group of 2-chloro-4-vinylpyrimidine, 2-chloro-4-(1-phenylvinyl)pyrimidine and 2-chloro-4-vinylquinazoline provides the corresponding 2-chloro-4-(2-substituted ethyl)pyrimidines and 2-chloro-4-(2-substituted ethyl)quinazolines. Treatment of these products, without isolation, with N-methylpiperazine results in nucleophilic displ...

Chloromuconate cycloisomerases of bacteria utilizing chloroaromatic compounds are known to convert 3-chloro-cis,cis-muconate to cis-dienelactone (cis-4-carboxymethylenebut-2-en-4-olide), while usual muconate cycloisomerases transform the same substrate to the bacteriotoxic protoanemonin. Formation of protoanemonin requires that the cycloisomerization of 3-chloro-cis,cis-muconate to 4-chloromuco...

Various 7-chloro-6-fluoro-2-arylidenylaminobenzo(1,3)thiazole (2a-h) have been synthesized by the condensation of 7-chloro-6-fluoro-2-aminobenzo(1,3)thiazole (1) with different aromatic aldehydes. The Schiff's bases on reaction with acetyl chloride, chloroacetyl chloride and phenyl acetyl chloride yielded 1-(7-chloro-6-fluorobenzothiazol-2-yl)-3,4-substituted-aryl-azetidin-2-ones (3a-x). Simila...

The synthesis of the title compounds is described. Reaction of 1-substituted 2-pyrazolin-5-ones with 5-chloro-1-phenyl-1H-pyrazole-4-carbonyl chloride or 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbonyl chloride, respectively, using calcium hydroxide in refluxing 1,4-dioxane gave the corresponding 4-heteroaroylpyrazol-5-ols, which were cyclized into 1H-pyrano[2,3-c:6,5-c]dipyrazol-4(7H)-ones b...