Electric Literature of 2002-24-6, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 2002-24-6 as follows.
EXAMPLE 2 N-(3-{4-[3-Chloro-4-(3-fluoro-benzyloxy)-phenylamino]-quinazolin-6-yl}-prop-2-ynyl)-N’-cyano-N”-3-(2-hydroxy-ethyl)guanidine. A mixture of crude 1-(3-{4-[3-chloro-4-(3-fluoro-benzyloxy)-phenylamino]-quinazolin-6-yl}-prop-2-ynyl)-2-phenyl-N-cyano-isourea (70 mg, 0.12 mmol) (from Step H, Example 1), 2-hydroxyethylamine hydrochloride (39 mg, 0.4 mmol) and triethylamine (0.07 mL, 0.5 mmol) in isopropanol (2 mL) was heated to 85 C. in a sealed tube. The reaction was cooled to room temperature after 3 hours. Solvent was removed via rotovap. The residue was then purified by FCC to give the final productproduct (25 mg, 38%) as a light yellow solid. MS ESI (+) m/z 544 (M+1) detected; 1H NMR (400 MHz, deuterated DMSO) 9.95 (s, 1H), 8.7 (s, 1H), 8.6 (s, 1H), 8.05 (s,1H), 8.0 (s, 1H), 7.8 (m, 1H), 7.78 (m, 2H), 7.6 (br, 1H), 7.5 (m, 1H), 7.22-7.4 (m, 2H), 7.2 (m, 1H), 7.1 (m, 1H), 5.25 (s, 2H), 4.25 (m, 2H), 3.5 (m, 2H), 3.25 (m, 2H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,2002-24-6, its application will become more common.
Reference:
Patent; Wallace, Eli; Topolov, George; Zhao, Qian; Lyssikatos, Joseph P.; US2005/101617; (2005); A1;,
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