4-AMINO-N-(2-PHENYLETHYL)BENZENESULFONAMIDE

C-7280948 is a PRMT1 inhibitor.IC50 value:Target: PRMT1in vitro: Especially arginine methyltransferases also target non-histone protein substrates and are therefore often called protein methyltransferases (PRMTs). The subtype PRMT1 has been linked to the activation of estrogen and androgen receptors and therefore may represent a new treatment option for hormone-dependent cancer. C-7280948 is a inhibitor, which is available for PRMT1.

General procedure: Concentrated HCl (10-15 ml) was added slowly to a mixture of 4-nitrobenzenesulfonamide or 4-nitrobenzamide analog (13a-q, 1.4 mmol, 1 eq) and Sn granules (2-2.5 eq) in ethanol (10 mL). The reaction mixture was refluxed for 3.5-6 h. When the TLC plates howed that there is no more starting material left, the reaction mixture was cooled down to rt. NaOH (30percent or 5M, aq) was added to the mixture until it became basic. The mixture was extracted with EA or DCM and the organic layer was dried with Na2SO4. The solvent was evaporated. The product was purified with column chromatography when required. 4.6.4.27 General procedure: The aromatic nitro compounds are dissolved in ethyl acetate and SnClUnder nitrogen protection, A mixture of 4-aminobenzenesulfonamide (172 mg, 1 mmol)[Cp * IrCl2] 2 (8 mg, 0.01 mmol, 1 molpercent), Potassium hydroxide (56 mg, 1 mmol), Phenethyl alcohol (610mg, 5equiv) were added sequentially to the reaction flask 25mLSchlenk.The mixture was allowed to react at 120 ° C for 12 hours, Cooled to room temperature, The solvent was removed under vacuum.And then subjected to column chromatography (developing solvent:Ethyl acetate / n-hexane) to give the pure title compound, Yield: 80percent.

Molecular Weight:276.36
XLogP3:2.2
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:4
Rotatable Bond Count:5
Exact Mass:276.09324893
Monoisotopic Mass:276.09324893
Topological Polar Surface Area:80.6
Heavy Atom Count:19
Complexity:350
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes