3-羟甲基四氢呋喃的合成研究

3-羟甲基四氢呋喃是合成第3代烟碱类杀虫剂呋虫胺和核苷类抗病毒药物喷昔洛韦的关键中间体,但长期以来由于使用大量金属硼氢化物造成生产成本高、安全风险高、废物多等缺点。以γ-丁内酯为原料,经Aldol缩合、硼氢化钠还原两步反应得到3-羟甲基四氢呋喃,总收率为51.9%,该法中间体α-羟甲基-γ-丁内酯只有一个内酯羰基需还原,原料γ-丁内酯和甲醛价廉易得,整个工艺路线适于工业化。

Study on synthesis of 3-(hydroxymethyl) tetrahydrofuran

3-(hydroxymethyl)tetrahydrofuran is the key intermediate for preparing the third generation of synthetic insecticides dinotefuran and penciclovir,Lowe's,but for a long time the large usage amount of metal borohydride brings high cost,high security risk,waste and other shortcomings.In this paper,withγ-butyrolactone as raw material,through Aldol condensation and sodium borohydride reduction 3-(hydroxymethyl)tetrahydrofuran was prepared with a total yield of 51.9%.The intermediateα-hydroxymethyl-γ-butyrolactone has only one lactone carbonyl that needs to restore.The process uses lower cost materials and it is easily scaled up.