Antibacterial drug for targeted therapy of staphylococcal infection by synergizing with antibiotic as well as synthesis method and application of antibacterial drug
A technology of reactions and compounds, applied in the field of medicinal chemistry, which can solve problems such as ineffectiveness
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Embodiment 1
[0040] The structural formula of ASC-NB of the present invention is as follows:
[0041]
[0042] The above-mentioned ASC-NB is prepared according to the following steps:
[0043] 1. The preparation steps of intermediate product C4 are as follows,
[0044]
[0045] (1) Mix C1 and hydrazine hydrate at a molar ratio of 1:1, heat up to 80 °C and reflux for 8-12 h. After the reaction is completed, it is slowly cooled to room temperature, and a large amount of white solid C2 is generated during the cooling process;
[0046] 1 H NMR (400 MHz, DMSO- d 6 ): δ 12.52 (s, 1H), 10.07 (s, 1H), 7.79 (d, 1H), 7.37(t, 1H), 6.87(dd, 2H), 4.65 (s, 2H).
[0047] (2) Dissolve C2 in a sufficient amount of ethanol, stir at room temperature until clear, add ammonium thiocyanate in an equimolar ratio, then add concentrated hydrochloric acid and heat up to 80-100 °C for 12-16 h under reflux. After the reaction was completed, it was cooled to room temperature, the insoluble matter was removed...
Embodiment 2
[0061] The structural formula of ASC-NA of the present invention is as follows:
[0062]
[0063] 1. the preparation step of intermediate product D3,
[0064]
[0065] (1) Mix D1 and thiosemicarbazide in acetonitrile at a molar ratio of 1:1 and reflux for 2 h. After cooling, the obtained solid is washed repeatedly with ethanol to obtain the intermediate product D2.
[0066] (2) Dissolve D2 in sodium hydroxide solution, reflux overnight and adjust the pH to acidic with dilute hydrochloric acid to obtain D3;
[0067] 1 H NMR (400 MHz, CDCl 3 ): δ 3.26 (s, 1H), 2.53 (t, J = 5.9 Hz, 2H), 2.31(t, J = 5.5 Hz, 2H), 1.89 (p, J = 5.7 Hz, 2H).
[0068] 2. the preparation step of intermediate product D4,
[0069]
[0070] (1) Dissolve A1 and 2,6-lutidine in acetonitrile, add 1.5 equivalents of acid chloride dropwise at 0 °C for 2 h, then add an equivalent amount of triethylamine, stir overnight and then rise to room temperature. TLC tracking, after the reaction was co...
Embodiment 3
[0079] ASC-SB structural formula of the present invention is as follows:
[0080]
[0081] 1. the preparation step of intermediate product E4,
[0082]
[0083] (1) Mix E1 and hydrazine hydrate at a molar ratio of 1:1, heat up to 80-100 °C and reflux for 8-10 h. After the reaction was completed, it was cooled to room temperature, and a large amount of white solid E2 was obtained after cooling.
[0084] (2) Dissolve E2 in a sufficient amount of ethanol, stir at room temperature until clarified, then add an equivalent amount of ammonium thiocyanate, then add concentrated hydrochloric acid and raise the temperature to 80-100 °C for 12-16 h under reflux. After the reaction was completed, it was cooled to room temperature, the insoluble matter was removed by filtration, the filtrate was spin-dried under reduced pressure, and dried in vacuum to obtain E3.
[0085] (3) Dissolve E3 in a small amount of concentrated hydrochloric acid, stir and reflux. After the reaction was co...
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