Reference of 90434-01-8, 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 90434-01-8 as follows.
Example 8 N-[(R)-1-Hydroxymethyl-2-(1H-indol-3-yl)-ethyl]-2-isopropoxy-5-(3-ethylcarbamoylphenylethynyl)-benzamide 3-lodo-N-methyl-benzamide (58 mg), 5-Ethynyl-N-[(R)-1-hydroxymethyl-2-(1H-indol-3-yl)-ethyl]-2-isopropoxy-benzamide (100 mg), palladium dichlorobis(triphenylphosphine) (4.7 mg) and TBAF x 3 H2O (170 mg in THF (5 ml) were stirred at 80C for 5 hours. The reaction mixture was concentrated and extracted with ethylacetate / water. The combined organic layers were dried over sodium sulphate and the solvent was evaporated. The title compound was obtained in 79 % yield (89 mg) after flash chromatography. 1H-NMR (CDCl3): 8.48 (J = 7.3 Hz, 1H); 8.39 d (J = 2.0 Hz, 1H); 8.20 s (1H); 7.87 s (1H); 7.77 d (J = 6.6 Hz, 1H); 7.72 d (J = 7.6 Hz, 1H); 7.61 d (J = 6.6 Hz, 1H); 7.52 dd (J = 2.3 Hz / 8.6 Hz, 1H); 7.4 m (2 H); 7.19 m (1H); 7.09 m (2H); 6.90 d (J = 8.6 Hz, 1H); 4.66 m (1H); 4.57 m (1H); 3.81 m (2H); 3.14 m (2H); 3.03 d (J = 4.3 Hz, 3H); 1.27 m (3H); 1.21 m (3H).
According to the analysis of related databases, 90434-01-8, the application of this compound in the production field has become more and more popular.
Reference:
Patent; Bayer Schering Pharma Aktiengesellschaft; EP1932831; (2008); A1;,
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