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Figure 2 | Malaria Journal

Figure 2

From: Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum

Figure 2

Synthetic route for compound 3. Reagents and Conditions: (i) trichloroacetyl isocyanate (1 eq), THF, 0°C to r.t, 2 h, 91%; (ii) bromine (3.8 eq), acetic acid, 0°C to 80°C, 14 h, 65%; (iii) ammonia, CH3OH, 0°C to r.t., 30 min, 76%; (iv) t-BuOK, DMF, RT, 14 h, 99%; (v) POCl3,N,N- dimethyl aniline (0.5 eq), 130°C, 14 h 88%; (vi) 3-dimethylaminopropylamine (1 eq), Na2CO3 (2 eq), EtOH, r.t., 14 h, 72%; (vii) 2 M methyl amine in THF (10 eq), dioxane, sealed tube, 100°C, 14 h, 83%; (viii) phenylboronic acid (1.1 eq), Pd(PPh3)2Cl2 (0.05 eq), aq. 1 M K2CO3 (1.05 eq), DMF, 90°C, 14 h, 63%.

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