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Scheme 1 | Clinical Epigenetics

Scheme 1

From: Dissecting the role of novel EZH2 inhibitors in primary glioblastoma cell cultures: effects on proliferation, epithelial-mesenchymal transition, migration, and on the pro-inflammatory phenotype

Scheme 1

Reagents and conditions: (a) glacial acetic acid, sealed tube, 100 °C, 1.5 h (35-80%); (b) Pd(OAc)2, PH(tBu)3BF3, potassium tert-butoxide, dry toluene, sealed tube, N2, 80 °C, 4 h (76-80%); (c) trichloroacetyl chloride, dry 1,2-dichloroethane, sealed tube, 0 °C to 70 °C, 1 h; (d) I. 2 N KOH (aq), EtOH, r.t. to 60 °C; II. 2 N HCl (aq) (54-73 %); (e) triethylamine, TBTU, dry DMF, N2, r. t., 4 h (52-75%)

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