With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1953-54-4,5-Hydroxyindole,as a common compound, the synthetic route is as follows.
0.5 g (3.8 mmol) 5-hydroxyindole (1 ) were dissolved in 5 ml acetone and mixed with 535 muIota (4.5 mmol) benzylbromide (BnBr), 2.45 g (7.5 mmol) Cs2C03 and 1.2 g (4.5 mmol) 18-crown-6 at room temperature (rt). After stirring for 2.5 to 17 h, preferably for 6 h, the mixture was diluted with water, smoothly acidified with 1 M HCI and extracted three times with CH2CI2. The combined organic layers were dried with Na2S04, filtered and evaporated. The crude product was purified by flash chromatography (Si02, cyclohexane – ethyl acetate 4:1 ) and yielded 762 mg (3.4 mmol, 91 %) of a pale yellow solid. 1H-NMR (500 MHz, CDCl3): 8.11 (br, 1 H), 7.52 (d, J=7.5 Hz, 2 H), 7.41 (t, J=7.8 Hz, 2 H), 7.37-7.30 (m, 2 H), 7.22 (d, J=2.3 Hz, 1 H), 7.21 (t, J=2.8 Hz, 1 H), 6.98 (dd, J=8.8 Hz, J=2.4 Hz, 1 H), 6.51 (br, 1 H), 5.15 (s, 2 H).
1953-54-4, The synthetic route of 1953-54-4 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; TECHNISCHE UNIVERSITAeT MUeNCHEN; SKERRA, Arne; MUeLLER, Michael; SCHEMANN, Michael; BERGER, Thomas; WO2014/125084; (2014); A1;,
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