1687855-43-1Relevant articles and documents
4 - amino quinoline - 8 - carboxylic acid methyl ester
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Paragraph 0008; 0015; 0024-0025, (2017/08/25)
The invention provides a synthesis method of 4-aminoisoquinoline-8-methyl formate. According to the synthesis method, 8-bromoisoquinoline reacts with carbon monoxide in methanol in the presence of palladium acetate to generate 8-isoquinoline methyl formate; 8-isoquinoline methyl formate reacts with N-bromosuccinimide in acetic acid to generate 4-bromoisoqunoline-8-methyl formate; the compound reacts with tert-butyl carbamate in the presence of the palladium acetate and cesium carbonate to generate amino protected 4-t-butoxycarbonylaminoisoquinoline-8-methyl formate, and finally, the protecting group of 4-t-butoxycarbonylaminoisoquinoline-8-methyl formate is removed in a mixed solvent of hydrochloric acid and methanol to obtain 4-aminoisoquinoline-8-methyl formate. The synthesis method of 4-aminoisoquinoline-8-methyl formate is good in selectivity, high in total yield (71%), convenient to operate, simple in after-treatment and suitable for large-scale production.