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Design, synthesis, biological evaluation and docking study of …

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WebDec 1, 2024 · Deprotection with conc. HCl afforded amine 11, which was coupled with 4-methylbenzoic acid in the presence of EDCi, HOBt and TEA to obtain the reversed amide linker compound 12. Additionally, the ester intermediate 3 was coupled with 3,5-dimethoxyaniline or 4-chloroaniline to give compounds 13 and 14, respectively. WebTo a solution of the acid intermediate and the TFA salt of dioxaoctanediamine derivative of biotin8 (207.0 mg, 0.42 mmol) in 4 mL of DMF was added EDCI (98.0 mg, 0.51 mmol), HOBT (13.5 mmol, 0.1 mmol), and TEA (1 mL). The reaction mixture was stirred at rt for 10 h. The solvent was removed in vacuo. WebNov 11, 2024 · TEA (97 μL, 0.70 mmol), HOBt (51.3 mg, 0.38 mmol), EDCI (72.8 mg, 0.38 mmol) and carboxylic acid (0.32 mmol) were added in order. The reaction was stirred at room temperature overnight. The volatile was removed under vacuo, then diluted with EtOAc and washed with water (3x). da vinci skills