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4-(5-amino-6-benzylpyrazin-2-yl)phenol synthesis
- Product Name:4-(5-amino-6-benzylpyrazin-2-yl)phenol
- CAS Number:37156-84-6
- Molecular formula:C17H15N3O
- Molecular Weight:277.32
Yield:37156-84-6 95%
Reaction Conditions:
with bis-triphenylphosphine-palladium(II) chloride;potassium carbonate in ethanol;water;toluene at 80;Inert atmosphere;
Steps:
3 Preparation of 2-amino-3-benzyl-5-(4-hydroxyphenyl)-pyrazine:
2-Amino-3-benzyl-5-bromo-pyrazine (2g, 7.57mmol), 4-hydroxyphenylboronic acid (1.57g, 11.36mmol), bistriphenylphosphine palladium dichloride (200mg, 0.28mmol) , Anhydrous potassium carbonate (2.09g, 15.14mmol) is dissolved in the solution of toluene:ethanol:water=2:4:1, under nitrogen protection, under the condition of 80 , monitor the reaction, until the reaction of the raw materials is complete, stop the reaction , filter through celite, add 50mL saturated ammonium chloride solution and 2×50mL ethyl acetate to the filtrate, extract, collect the organic layer solution, dry over anhydrous sodium sulfate, filter, collect the filtrate, spin dry, add 100- 200-mesh silica gel sample was mixed, packed with 200-300-mesh silica gel, and ethyl acetate and petroleum ether were used as eluents for gradient elution to obtain intermediate 147-20, Rf=0.3, and the developing solvent was petroleum ether:acetic acid Ethyl ester=1:1, pale yellow needle-like compound 2g, namely C2 compound, yield 95%,
References:
CN113683617,2021,A Location in patent:Paragraph 0029; 0086; 0089-0090
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