Large-particle tenofovir disoproxil fumarate and preparation method thereof

The invention belongs to the field of medicinal chemistry, and concretely relates to a preparation method for large-particle tenofovir disoproxil fumarate. The method comprises the following steps: (1) taking a mixed liquid of a tenofovir disoproxil fumarate and a good solvent, regulating the mixed...

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Hauptverfasser: CUI YANGWEN, LI YINGFU, SU ZHONGHAI, ZHANG PING, HUANG HAOXI, HUANG JUN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the field of medicinal chemistry, and concretely relates to a preparation method for large-particle tenofovir disoproxil fumarate. The method comprises the following steps: (1) taking a mixed liquid of a tenofovir disoproxil fumarate and a good solvent, regulating the mixed liquid to a first temperature, then adding a poor solvent, and performing crystallization; (2) raising the temperature to a second temperature, then performing cooling to the first temperature, and performing crystallization; and operating the step zero time or more; (3) performing cooling to a third temperature, and performing crystallization; (4) performing cooling to a fourth temperature, and performing crystallization; and (5) separating solid and liquid to obtain the large-particle tenofovir disoproxil fumarate. The preparation method for the large-particle tenofovir disoproxil fumarate improves varieties and ratios of solvents adopted for product crystallization, thus process operation is simple, product qual