With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.35320-67-3,2-Methyl-1H-indol-4-ol,as a common compound, the synthetic route is as follows.
To a stirred solution of 2-chloro-N-[(3- fluorophenyl)methyl] -7,8-dihydro-5H-pyrano [4,3-d]pyrimidin-4-amine (350 mg, 1.19 mmol) in Dioxane (20 ml) were added 2-methyl-1H-indol-4-ol (193 mg, 1.31 mmol), Pd2dba3 (218 mg, 0.24 mmol), X-Phos (113 mg, 0.24 mmol) and Cs2CO3 (782 mg, 2.38 mmol). The black suspension was stirred at 100 oC for 3 h under N2. TLC showed the reaction was completed. The reaction was filtered through a pad of celite and the filtrate was diluted with EtOAc (50 mL) and H2O (20 mL). The aqueous layer was extracted with EtOAc (20 mL x 3), dried over Na2SO4 and concentrated in vacuo. The red oil was purified via silica gel column chromatography (hexane and ethyl acetate) to afford the desired product 1-(4-((3-fluorobenzyl)amino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin- 2-yl)-2-methyl-1H-indol-4-ol (300 mg, 54%) as a yellow solid.
As the paragraph descriping shows that 35320-67-3 is playing an increasingly important role.
Reference£º
Patent; CLEAVE BIOSCIENCES, INC.; ZHOU, Han-Jie; WUSTROW, David; (498 pag.)WO2016/200840; (2016); A1;,
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