Quetiapine hemifumarate synthesis technology

The invention discloses a quetiapine hemifumarate synthesis technology. The technology comprises the following steps: mixing a compound of formula (II) and C1-C4 alkyl acid, heating the compound of formula (II) and the C1-C4 alkyl acid to 80-100 DEG C, adding zinc powder or iron powder, and carrying...

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Bibliographische Detailangaben
Hauptverfasser: ZHANG WENWEN, WANG TINGSHENG, TAN CHAO, ZHOU XUDONG, ZOU XIN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a quetiapine hemifumarate synthesis technology. The technology comprises the following steps: mixing a compound of formula (II) and C1-C4 alkyl acid, heating the compound of formula (II) and the C1-C4 alkyl acid to 80-100 DEG C, adding zinc powder or iron powder, and carrying out a heat insulation reaction for 4-6 h to obtain quetiapine; and carrying out salt formation on the obtained quetiapine and fumaric acid to obtain quetiapine hemifumarate, wherein a feeding molar ratio of quetiapine to fumaric acid is 1:0.5. The technology has the advantages of simplicity in operation, high yield, high purity of the above obtained product, and easy realization of industrialization. 本发明公开了种半富马酸喹硫平的合成工艺,包括如下步骤:将式(II)化合物、C1-C4烷酸混合,并升温至80-100℃,加入锌粉或铁粉,保温反应4-6h,得喹硫平;将所得的喹硫平与富马酸成盐,得半富马酸喹硫平,其中,喹硫平与富马酸投料的摩尔比为1:0.5。本发明的工艺具有操作简便、收率高,所得产品纯度高等优势,且易于实现工业化。