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Bifunctional compound, and preparation method and application thereof
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A bifunctional compound and solvate technology, which is applied in the field of bifunctional compounds and their preparation, can solve the problems of drug resistance in patients
Active Publication Date: 2021-09-14
SUZHOU KINTOR PHARMA
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Problems solved by technology
Despite the development of effective targeted therapies, most patients develop drug resistance and the disease continues to progress
Method used
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Embodiment A1
[0520]
[0521] 1-1 (2g, 10mmol), TMSCN (3g, 30mmol), ZnCl 2 (136mg, 1mmol) was added to 50ml of acetone in turn, reacted at room temperature for 1h, after the reaction, washed with 100ml of water, extracted with 100ml of EA, washed with 50ml of saturated brine, dried over anhydroussodiumsulfate, and spin-dried to obtain 2.3g of product 1-2, yield 88%, the product was used directly in the next step without purification.
[0522]
[0523] Add 1-2 (2.3 g, 8.8 mmol), 1-3 (4.3 g, 17.6 mmol) to 10 ml of DMF in turn, and react at room temperature overnight. After the reaction, add 20 ml of methanol, 20 ml of 6NHCl, and react at 90°C for 1 h. Washed with 50ml of water, extracted with 50ml of EA, washed with 20ml of saturated brine, dried over anhydroussodiumsulfate, spin-dried on the upper chromatography column PE:EA=5:1-2:1 to obtain 400 mg of product 1-4 with a yield of 9.2%.
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technical field [0001] The invention belongs to the field of medicine, and in particular relates to a bifunctional compound and a preparation method and use thereof, wherein the bifunctional compound comprises a binding part bound to E3 ubiquitin ligase; a target protein binding part bound to androgen receptor; and E3 ubiquitin ligase binding part; A linking moiety that connects the ubiquitin ligase-binding moiety and the target protein-binding moiety. The bifunctional compounds of the present application locate androgen receptors adjacent to ubiquitin ligases to achieve degradation or inhibition of androgen receptors. Background technique [0002] The androgen receptor (AR) belongs to the nuclear hormone receptor family that is activated by androgen. In the absence of androgens, AR is bound by heat shockprotein 90 (Hsp90) in the cytosol. When androgen binds AR, its conformation changes to release AR from Hsp90 and expose the nuclear localization signal (NLS). The latter...
Claims
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