Preparation and application of tyrosine phosphorylation inhibitor A9_Industrial additives

Background and overview[1-2]

Tyrosine phosphorylation inhibitor A9 (Tyrphostin9) can act as an effective uncoupler of oxidative phosphorylation and can inhibit the differentiation of preadipocytes into mature adipocytes, thereby preventing adipocytes from form. Tyrphostin9 is a cytoprotective agent with extremely low toxicity (in vitro and in vivo) that inhibits the TNF-induced respiratory burst of human neutrophils without inhibiting their bactericidal activity and is antifogging and may be used in the treatment of intimal hyperplasia diseases. treat. In addition, because the tyrosine phosphorylation inhibitor A9 is structurally very similar to casein 9 and can strongly activate cytoprotective genes by inducing the nuclear translocation of the transcription factor Nrf2, tyrphostin9 is likely to exert its cytoprotective effects through this pathway.


Anhydrous DMF solution (3 mL) of 3,5-di-tert-butyl-4-hydroxybenzaldehyde (244 mg, 1.0 mmol) and malononitrile (80 mg, 1.2 mmol) was refluxed for 10 h. The solvent was distilled off under reduced pressure, and the residue was purified by column chromatography on silica gel (hexane/Et2O, 1:1) to obtain tyrosine phosphorylation inhibitor A9 (233 mg , 83%) as a yellow solid: mp 131–134°C. 1H NMR (CDCl3, MHz): d 7.81 (s, 2H), 7.65 (s, 1H), 6.06 (s, 1H), 1.47(s, 18H).EI–MS: m/z 282 (M+).Anal.calcd forC18H22N2O(Mr 282.4): C, 76.56; H, 7.85; N, 9.92. Found: C, 76.34; H, 7.66; N, 9.63. logP: 5.02 (calcd), 2.32 (obsd). dGW: 62.4 KJ. pKa: 6.87 (ref36, 6.80)UV–vis max: 464 nm (10,031), 364 nm (11,101).


CN201080038071.0 discloses a compound for treating malaria and preventing the spread of malaria, including mepenthioheptadone, clotidine dichloride, doxepin, protyptiline, vijingin, MLS000708402-02 , NCGC00163169‑03, MLS000556883‑02, tyrosine phosphorylation inhibitor A9, ellipticine, mitoxantrone, cyclosporine A, demethoxycin, (S)‑(+)‑camptothecin Base, niclosamide, propiopropionate hydrochloride, catithromycin, (S)-(-)-propiopropionate hydrochloride, 2′-(4-aminophenyl)-[2,5′ -Di-1H-benzimidazole]-5-amine (Ro90-7501), 1,5-bis(4-allyldimethylammoniumphenyl)pentan-3-one dibromide (BW284c51), WB64 , U‑83836 dihydrochloride, aminopterin, methotrexate, clofluphenanthrol, pyrimethamine, triamterin, trimethoprim, 1,5‑di(4‑allyldi At least one of methylammonophenyl)pentane-3-one dibromide, mefloquine, artemisinin, and dihydroergotamine sulfonatemethane.

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