Indole compounds and preparation method and application thereof as drug-resistant bacteria resistant drugs
A compound and indole technology, applied in the field of chemical and compound medicine, can solve problems such as slow progress and inability to treat drug-resistant bacteria
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Embodiment 1
[0168] Embodiment 1 general formula III, the preparation of I compound
[0169]
[0170] Preparation of intermediate 1-(3- or 4-substituted benzyl)-3-formyl-5(or 6)-methoxycarbonylindole 3 in general formula V
[0171]
[0172] Preparation of 3-formyl-5(or 6)-methoxycarbonylindole (2)
[0173] 5 (or 6)-methoxycarbonylindole (1) and phosphorus oxychloride (POCl 3 ) Vilsmeier-Hack reaction occurs under the condition of dry N,N-dimethylsulfoxide to generate 3-formyl-5 (or 6)-methoxycarbonylindole (2)
[0174] Preparation of 3-formyl-5 (or 6)-methoxycarbonylindole (2) manipulation example
[0175] Preparation of 3-formyl-5-methoxycarbonylindole
[0176]Under nitrogen protection, 5.00 g (28.57 mmol) of methyl indole-5-carboxylate was added to 20 mL of ultra-dry DMF, cooled to 0°C, and then 3.62 mL (38.86 mol) of phosphorus oxychloride was slowly added dropwise. After reacting at 0°C for 10 min, react at room temperature for 3 h. After cooling the reaction liquid to 0°C, ...
Embodiment 2
[0236] Embodiment two general formula IV, the preparation of II compound
[0237] Preparation of target compound Ⅳ
[0238] Intermediate (3) or (4) or (8) respectively reacts with 4,5-dihydroimidazole-2-hydrazine hydrogen bromide VI in dry methanol to reflux the target compound IV;
[0239] Preparation of 1-p-chlorobenzyl-5-methoxycarbonyl-3-indolecarbaldehyde, (4,5-dihydro-1H-imidazol-2-yl)hydrazonone hydrogen bromide salt (compound 61 in Table 8) manipulation instance
[0240] 0.05 g (0.15 mmol) of 1-p-chlorobenzyl-3-formyl-6-methoxycarbonylindole was added to 2 mL of anhydrous methanol, and then 4,5-dihydroimidazole-2-hydrazine was brominated 0.03 g (0.15 mmol) of hydrogen was added to the reaction solution, and heated to 75°C for reaction. After the reaction, the reaction solution was cooled to room temperature, and diethyl ether was added to stand still to precipitate a solid, which was filtered under reduced pressure, and the filter cake was washed with diethyl ether ...
Embodiment 3
[0250] Embodiment 3 The preparation of compound sterile powder injection of the present invention
[0251] 1. Prescription:
[0252] Prescription 1:
[0253] Any one of compound III or IV 250g (calculated as compound)
[0254] A total of 1000 sticks were prepared
[0255] Prescription 2:
[0256] Any one of compound III or IV 500g (calculated as compound)
[0257] A total of 1000 sticks were prepared
[0258] Prescription 3:
[0259] Any one of compound III or IV 1000g (calculated as compound)
[0260] A total of 1000 sticks were prepared
[0261] Prescription 4:
[0262] Any one of compound III or IV 2000g (calculated as compound)
[0263] A total of 1000 sticks were prepared
[0264] 2. Preparation process:
[0265] (1) Aseptically process the antibiotic glass bottles, rubber stoppers, etc. used for the preparation;
[0266] (2) Weigh the raw materials according to the prescription (feeding after conversion), put the sterile powder in the filling machine for subp...
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