Pyrazole boric acid compound, pharmaceutical composition containing pyrazole boric acid compound, and application of pyrazole boric acid compound and pharmaceutical composition
A compound and pharmaceutical technology, applied in the field of medicine, can solve the problems of poor in vitro and in vivo stability, large toxic and side effects, and poor biological selectivity.
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[0093] Next, the present application will be described in detail through examples, but the present application is not limited to these examples. Unless otherwise stated, all reagents, materials, and equipment used in the following examples are commercially available; and all reagents are commercially available chemically or analytically pure.
[0094] Route 1: Synthesis of Compound 1-Compound 26
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preparation example 1
[0096] Preparation Example 1: Synthesis of Compound 1
[0097] Step 1: Synthesis of Intermediate 1-2
[0098] To a solution of KOH (16.8 g, 300 mmol) in 95% EtOH (125 mL) was added 1-(2-hydroxyphenyl)ethan-1-one (13.6 g, 100 mmol) and benzaldehyde (10.6 g, 100 mmol) ). The solution was stirred at room temperature for 12 hours until complete as monitored by TLC, poured into ice water (1000 mL) and acidified to pH 2-3 with 4N HCl. After standing, the precipitate was filtered and washed with water until the pH value reached 6-7, and dried in vacuum to obtain a crude yellow solid (23.1 g, yield 95.1%).
[0099] Step 2: Synthesis of Intermediates 1-3
[0100] The crude product from step 1 (8.69 g, 40 mmol) and ethyl hydrazinoacetate hydrochloride (7.74 g, 48 mmol) were suspended in EtOH (150 mL). The solution was heated to reflux for 12 h, then concentrated under reduced pressure. The residue was dissolved in ethyl acetate (100 mL) and water (100 mL), then acidified to pH 5-6 ...
preparation example 2- preparation example 26
[0111] Preparation Example 2-Preparation Example 26: According to route 1, using the same steps as the synthesis of compound 1, compound 2-compound 26 was obtained as a white solid, and the compounds are shown in the following table:
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[0118] Route 2: Synthesis of compound 27
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