113697-60-2Relevant academic research and scientific papers
Synthesis of some bicyclic thiazolo- and oxothiazolo-pyrimidines
Mobinikhaledi,Foroughifar,Ahmadi
, p. 339 - 345 (2005)
Oxothiazolopyrimidine compounds 2(a-e) were synthesized under reflux condition by a simple one-pot condensation reaction of the pyrimidine derivative 1 and chloroacetylchloride in the presence of silver acetate as a catalyst. In a similar way the thiazolo
Oxidation of thiazolo[3,2-a]pyrimidin-3(2H)-ones with DMSO and Lawesson's reagent
Lashmanova, Eugenia A.,Kirdyashkina, Anastasiya I.,Slepukhin, Pavel A.,Shiryaev, Andrey K.
supporting information, p. 1099 - 1103 (2018/02/19)
2,2′-Dimers with a central double bond were prepared by the oxidation of 5,6-disubstituted 7-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-3(2H)-ones with DMSO and Lawesson's reagent at room temperature. The role of DMSO as an oxidizing reagent was confirmed by NMR spectroscopy. The E-configuration of the central C[dbnd]C bond for the two diastereomers of compound 8m was proven by single crystal X-ray data. The dimeric thiazolopyrimidines were orange or red colored and absorption bands at 283–330 and 459–476 nm were observed in the UV spectra.
Biological evaluation of halogenated thiazolo[3,2-a]pyrimidin-3-one carboxylic acid derivatives targeting the YycG histidine kinase
Zhao, Dan,Chen, Chen,Liu, Huayong,Zheng, Likang,Tong, Yao,Qu, Di,Han, Shiqing
, p. 500 - 507 (2015/01/09)
With an intention to potent inhibitors of YycG histidine kinase, a series of halogenated thiazolo[3,2-a]pyrimidin-3-one carboxylic acid derivatives were synthesized and evaluated for their antibacterial, antibiofilm and hemolytic activities. The majority of the compounds showed good activity against Staphylococcus epidermidis and Staphylococcus aureus, with MIC values of 1.56-6.25 μM, simultaneously presented promising antiobifilm activity against S. epidermidis ATCC35984 at 50 μM. The test of inhibitory activity on YycG kinase suggested the antibacterial activities of these derivatives are based on inhibiting the enzyme activity of the YycG HK domain. The hemolytic activity test suggested these compounds exhibited in vitro antibacterial activity at non-hemolytic concentrations.
A facile, rapid, one-pot regio/stereoselective synthesis of 2-iminothiazolidin-4-ones under solvent/scavenger-free conditions
Sathishkumar, Murugan,Nagarajan, Sangaraiah,Shanmugavelan, Poovan,Dinesh, Murugan,Ponnuswamy, Alagusundaram
supporting information, p. 689 - 697 (2013/06/05)
A rapid and efficient one pot solvent/scavenger-free protocol for the synthesis of 2-iminothiazolidin-4-ones has been developed. Interestingly, the regio/stereoselective synthesis affords the regioisomeric (Z)-3-alkyl/aryl-2-(2- phenylcyclohex-2-enylimino
A convenient synthesis of thiazolopyrimidines, thiazolodipyrimidines and heterocyclothiazolopyrimidines
Sherif,Youssef,Mobarak,Abdel-Fattah
, p. 9561 - 9572 (2007/10/02)
Ethyl 4-aryl-6-substituted-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxyla tes 1 reacted with bromomalononitrile (2) to give ethyl 3-amino-5-aryl-2-cyano-7-substituted-5H-thiazolo[3,2-a]pyrimidine-6-ca rboxylates 3. The latter compounds reacted with formic acid, hydroxylamine hydrochloride and with formamide to give 9H-3,4-dihydrothiazolo[3,2-a:4,5-b]dipyrimidine-8-carboxylates 5, 1H,8H-pyrazolo[3,4-d]thiazolo[3,2-a]pyrimidine-7-carboxylates 8 and 2,7-diaminothiazolo[4,5-d]pyrimidine (7), respectively. Compounds 1b,e reacted with chloroacetyl chloride to yield ethyl 5-aryl-3-oxo-7-substituted-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6- carboxylates 9a,b which coupled with arenediazonium chlorides to give the corresponding 2-arylhydrazone derivatives 10a,b. Compound 9a adds α-cyanocinnamonitriles 12a-c to yield ethyl 2-amino-4-aryl-3-cyano-9-(4-methoxyphenyl)-7-methyl-4H,9H-pyrano[2,3-d ]thiazolo[3,2-a]pyrimidine-8-carboxylates 13a-c. Refluxing 1b-d with phenacyl bromide produced ethyl 5-aryl-7-methyl-3-phenyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylates 14a-c.
Syntheses of 2,3-Dihydro-5H-thiazolopyrimidines and Tetrasubstituted Dihydropyrimidine Derivatives as Possible Anthelmintic Agents
Akhtar, M. Shamim,Seth, M.,Bhaduri, A. P.
, p. 556 - 561 (2007/10/02)
The hitherto unreported ring closure reaction of 5-ethoxycarbonyl-6-methyl-4-substitutedphenyl-3,4-dihydropyrimidine-2-thione with monochloroacetic acid in the presence of BF3-etherate is described.The reaction appears to have a general applicability and
