2289-75-0Relevant articles and documents
Synthesis of 6-membered-ring fused thiazine-dicarboxylates and thiazole-pyrimidines via one-pot three-component reactions
Mohlala, Reagan L.,Coyanis, Elena Mabel,Fish, Muhammad Q.,Fernandes, Manuel A.,Bode, Moira L.
, (2021/09/18)
A facile and efficient one-pot three-component reaction method for the synthesis of thiazine-dicarboxylates is reported. Reaction of an isocyanide and dialkyl acetylenedicarboxylate with 2-amino-4H-1,3-thiazin-4-one derivatives containing both an acidic proton and an internal nucleophile gave the products in good yields of 76–85%. The reactivity of dialkyl acetylenedicarboxylates was further tested in the synthesis of thiazole-pyrimidines where a two-component reaction of 2-aminothiazole with dialkyl acetylenedicarboxylates was successfully converted to a more efficient three-component reaction of a thiourea, α-haloketone and dialkyl acetylenedicarboxylate (DMAD/DEtAD) to give thiazole-pyrimidines in good yields of 70–91%.
A kind of 3,4-dichloro-thiazole derivatives and process for their preparation and use
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Paragraph 0040-0043; 0093-0094, (2016/10/08)
The invention provides 3,4-dichloro isothiazole derivatives, their preparation method and application. The invention relates to a heterocyclic compound containing 3,4-dichloro isothiazol, and the compound is represented by the following chemical structural general formula. The invention discloses the structural general formula of the compound, a synthetic method of the compound and applications of the compound as pesticide, bactericide, anti-plant virus agent, and plant activator, and a technology of mixing the compound with agriculturally acceptable auxiliary agents or synergists for preparing pesticide, bactericide, anti-plant virus agent, and plant activator. The invention further discloses the combined application of the compound and the commercial pesticide, bactericide, anti-plant virus agent, and plant activator in controlling diseases, insect pests, and virus diseases in agriculture, forestry and gardening, and a preparation method of the compound and the commercial pesticide, bactericide, anti-plant virus agent, and plant activator.
Synthesis of 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one derivatives
Veretennikov,Pavlov
, p. 575 - 579 (2013/06/27)
The reaction of 2-aminothiazoles with ethyl acetoacetate in acetic or polyphosphoric acid gave a series of 5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one derivatives which were nitrated with a mixture of nitric and sulfuric acid to 6-nitro-5H-[1,3]thiazolo[3,2-a]
Convenient and simple synthesis of 2-aminothiazoles by the reaction of α-halo ketone carbonyls with ammonium thiocyanate in the presence of N-methylimidazole
Meshram,Thakur, Pramod B.,Madhu Babu,Bangade, Vikas M.
, p. 5265 - 5269 (2012/10/30)
Substituted 2-aminothiazole derivatives were obtained as a result of N-methylimidazole catalyzed cyclization of α-halo ketone carbonyls with ammonium thiocyanate in water-alcoholic media. The generality of the method has been demonstrated by screening a series of aromatic/heteroaromatic/aliphatic α-halo ketones, α-halo β-diketones, and α-halo β-ketoesters. The developed method is simple, mild, and general route for the preparation of diversely functionalized 2-aminothiazoles in good to moderate yields from readily available starting materials.
One pot synthesis using supported reagents system KSCN/SiO 2-RNH3OAc/Al2O3: Synthesis of 2-aminothiazoles and N-allylthioureas
Aoyama, Tadashi,Murata, Sumiko,Arai, Izumi,Araki, Natsumi,Takido, Toshio,Suzuki, Yoshitada,Kodomari, Mitsuo
, p. 3201 - 3213 (2007/10/03)
A simple and efficient method has been developed for the synthesis of 2-aminothiazoles and N-allylthioureas from commercially available materials in one pot by using a supported reagents system, KSCN/SiO2-RNH 3OAc/Al2O3, in which α-halo ketone reacts first KSCN/SiO2 and the product, α-thiocyanatoketone, reacts with RNH3OAc/Al2O3 to give the final product, 2-aminothiazoles, in good yield and allyl bromide reacts with KSCN/SiO 2 and the product, allyl isothiocyanate, reacts with RNH 3OAc/Al2O3 to give N-allylthiourea.
SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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, (2008/06/13)
The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
One-pot synthesis of 2-aminothiazoles using supported reagents
Kodomari, Mitsuo,Aoyama, Tadashi,Suzuki, Yoshitada
, p. 1717 - 1720 (2007/10/03)
A simple and efficient method has been developed for the synthesis of 2-aminothiazoles from α-bromo ketones in one-pot using a supported reagents system, KSCN/SiO2-RNH3OAc/Al2O3, in which α-bromo ketone reacts first with KSCN/SiO2 and the product, α-thiocyano ketone, reacts with RNH3OAc/Al2O3 to give the final product, 2-aminothiazole, in high yield.
N-(4-Substituted-thiazolyl)oxamic Acid Derivatives, a New Series of Potent, Orally Actve Antiallergy Agents
Hargrave, Karl D.,Hess, Friedrich K.,Oliver, James T.
, p. 1158 - 1163 (2007/10/02)
A series of N-(4-substituted-thiazolyl)oxamic acid derivatives were synthesized and tested for antiallergy activity in the rat PCA model.These compounds were conveniently prepared by treatment of the appropriate acetophenone with thiourea and iodine or by reaction of the chloroacetylbenzene with thiourea to give the corresponding aminothiazoles; subsequent condensation with ethyloxalyl chloride gave the thiazolyloxamates.Many of the analogues showed a 50percent inhibition at oxamic acid ethanolamine salt (61, PRH-836-EA), has been selected for further pharmacological evaluation.