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Integrase strand transfer inhibitors adopted in the present study. Panel A: Synthesis of CHI1010 (7) and CHI1019 (8). Reagents and conditions: i) AcCl, Et2AlCl, CH2Cl2, 0°C, 2 h. ii) benzyl or 4-fluorobenzyl bromide, NaH, DMF, 0°C, 30 min; iii) diethyl oxalate, dry C2H5ONa, THF, two separated steps in the same conditions: 50°C, 2 min, 250 W, 300 psi; iv) 2N NaOH, MeOH, rt, 1.5 h. Panel B: structure of Merck's compound L-870,810 (9).
