Thiazole derivatives and their preparation methods and applications
A technology of derivatives and thiazoles, applied in the field of antibacterial drugs or industrial fungicides, thiazole derivatives with new structures and their preparation
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Embodiment 1
[0024] Preparation steps of 2-(2-(3-hydroxybenzylidene)hydrazino)-4-methyl-5-(1-(guanidinoimino)ethyl)-thiazole (IVa):
[0025]
[0026] 5mmol of 3-hydroxybenzaldehyde, 5mmol of thiosemicarbazide, and 30mL of ethanol were added to the 100mL flask, and the reaction was stirred at 65°C for 6 hours. After the reaction was completed, the filter was filtered, and the filter residue was collected and air-dried to obtain the first step product IIa, i.e., 1-( (thioureidoimino)methyl)-3-hydroxybenzene, 90% yield.
[0027] The first step product IIa of 2 mmol, 2.2 mmol of 3-chloroacetylacetone, and 20 mL of ethanol were added to the 100 mL flask, and the reaction was stirred at 65 ° C for 3 hours, the reaction was completed, filtered, and the filter residue was collected and air-dried to obtain the second step product IIIa, that is, 2-(2-(3-Hydroxybenzylidene)hydrazino)-4-methyl-5-carbonyl)-thiazole, yield 60%.
[0028] 1 mmol of the second step product IIIa, 1.2 mmol of aminoguanid...
Embodiment 2
[0030] Preparation steps of 2-(2-(2,3-difluorobenzylidene)hydrazino)-4-methyl-5-(1-(guanidinoimino)ethyl)-thiazole (IVb):
[0031]
[0032] 5 mmol of 2,3-difluorobenzaldehyde, 5 mmol of thiosemicarbazide and 30 mL of ethanol were added to a 100 mL flask, and the reaction was stirred at 65° C. for 6 hours. After the reaction was completed, the filter residue was collected and air-dried to obtain the first step product IIb, namely 1-((thioureidoimino)methyl)-2,3-difluorobenzene, 90% yield.
[0033] The first step product IIb of 2 mmol, 2.2 mmol of 3-chloroacetylacetone, and 20 mL of ethanol were added to a 100 mL flask, and the reaction was stirred at 65 ° C for 3 hours, the reaction was completed, filtered, and the filter residue was collected and air-dried to obtain the second step product IIIb, that is, 2-(2-(2,3-Difluorobenzylidene)hydrazino)-4-methyl-5-carbonyl)-thiazole, 70% yield.
[0034] 1 mmol of the second step product IIIb, 1.2 mmol of aminoguanidine hydrochlorid...
Embodiment 3
[0036] Preparation steps of 2-(2-(2,5-difluorobenzylidene)hydrazino)-4-methyl-5-(1-(guanidinoimino)ethyl)-thiazole (IVc):
[0037]
[0038] 5mmol of 2,5-difluorobenzaldehyde, 5mmol of thiosemicarbazide, and 30mL of ethanol were added to a 100mL flask, and the reaction was stirred at 65°C for 6 hours. After the reaction was completed, the filter residue was collected and air-dried to obtain the first step product IIc, namely 1-((thioureidoimino)methyl)-2,5-difluorobenzene, 90% yield.
[0039] The first step product IIc of 2 mmol, 2.2 mmol of 3-chloroacetylacetone, and 20 mL of ethanol were added to the 100 mL flask, and the reaction was stirred at 65 ° C for 3 hours, the reaction was completed, filtered, and the filter residue was collected and air-dried to obtain the second step product IIIc, namely 2-(2-(2,5-Difluorobenzylidene)hydrazino)-4-methyl-5-carbonyl)-thiazole, 80% yield.
[0040] 1mmol of the second-step product IIIc, 1.2mmol of aminoguanidine hydrochloride, 0.36...
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