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盐酸埃罗替尼中间体3,4-二(2-甲氧基乙氧基)苯腈 合成新工艺研究

Songze LI,Zeqing HUANG

Chemistry & Bioengineering（2019）

Cited 0|Views3
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Abstract
盐酸埃罗替尼是第一个应用于临床的口服表皮生长因子受体(EGFR)抑制剂,其中3,4-二(2-甲氧基乙氧基)苯腈是盐酸埃罗替尼合成的关键中间体.以儿茶酚为原料,经醚化、Vilsmeier反应、氰基化3步反应合成了3,4-二(2-甲氧基乙氧基)苯腈,总收率达61.2％,产品结构经NMR和MS确证.该工艺原料价廉易得、操作简便、成本较低、收率较高,适合工业化生产.
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