Preparation method of key intermediate of elagolix

The invention relates to the field of pharmacy, and concretely relates to a preparation method of a key intermediate of elagolix. The method adopts simple and easily available Boc-D-phenylglycinol asa starting material, and comprises the following steps: amination, acylamidation, arylation coupling,...

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Hauptverfasser: WANG AIMIN, XU CHENKE, JIANG TAO, CHE FENGFENG
Format: Patent
Sprache:chi ; eng
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Beschreibung
Zusammenfassung:The invention relates to the field of pharmacy, and concretely relates to a preparation method of a key intermediate of elagolix. The method adopts simple and easily available Boc-D-phenylglycinol asa starting material, and comprises the following steps: amination, acylamidation, arylation coupling, cyclization, benzylamine substitution and deprotection. The preparation method adopting the abovesynthesis route has the advantages of simple and easily available starting material, mild reaction conditions, simplicity in post-treatment, avoiding of a noble metal catalyst, great reduction of thesynthesis cost, high purity and high yield of the obtained intermediate, and suitableness for large-scale production in the workshop. 本发明涉及制药领域,具体涉及一种噁拉戈利关键中间体的制备方法,以简单易得的Boc-D-苯甘氨醇为起始原料,包含氨基化、酰胺化、芳基化偶联、环合、苄胺取代和脱保护六步反应,该合成路线起始原料简单易得,反应条件较为温和,后处理简单,避免使用了贵金属催化剂,大大降低了工艺合成成本,得到的中间体纯度和收率也很高,非常适合车间规模化生产。