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发明公开
CN103360352A 4-甲氧基-2,6-二羟基-2-苄基-3(2H)-苯并呋喃酮的全合成方法 失效 - 权利终止

4-甲氧基-2,6-二羟基-2-苄基-3(2H)-苯并呋喃酮的全合成方法
摘要：
本发明公开了一种化合物4-甲氧基-2，6-二羟基-2-苄基-3(2H)-苯并呋喃酮的全合成方法。该合成方法包括：以间苯三酚为起始原料，经过傅克酰基化反应及关环反应得到3(2H)-苯并呋喃酮母核；接着将两个酚羟基用苄基保护起来然后催化氢化，选择性脱掉4位苄基，再甲基化，得到关键中间体6-苄氧基-4-甲氧基-3(2H)-苯并呋喃酮；最后经羟醛缩合、催化氢化、烯醇化、环氧化开环以及脱苄基反应，全合成得到目的物4-甲氧基-2，6-二羟基-2-苄基-3(2H)-苯并呋喃酮。本发明具有原料易得、操作简便、成本低廉等优点。目的物可用作对照品控制蜂胶的质量。
摘要（英）：

The invention discloses a total synthesis method for the compound 4-methoxy-2,6-dihydroxy-2-benzyl-3(2H)-benzofuranone. The total synthesis method comprises the following steps: with m-trihydroxybenzene as a starting raw material, carrying out Friedel-Crafts acylation and cyclization so as to obtain a 3(2H)-benzofuranone mother nucleus; protecting two phenolic hydroxyl groups by using benzyl groups, then carrying out catalytic hydrogenation to selectively remove the benzyl group at position 4 and then carrying out methylation so as to obtain a key intermediate 6-benzyloxy-4-methoxy-3(2H)-benzofuranone; and finally carrying out aldol condensation, catalytic hydrogenation, enolization, epoxidation, a ring-opening reaction and debenzylation so as to totally synthesize the target compound 4-methoxy-2,6-dihydroxy-2-benzyl-3(2H)-benzofuranone. The total synthesis method provided by the invention has the advantages of easily available raw materials, simple operation, low cost, etc. The target compound can be used as a reference substance for controlling of the quality of propolis.

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