Trans-2-amino-cyclopropyl formic acid derivative and synthetic method thereof

The invention discloses a trans-2-amino-cyclopropyl formic acid derivative and a synthetic method thereof. The synthetic method includes the following steps that a compound II is used as a raw material and reacts with di-tert-butyl dicarbonate under the alkaline condition to prepare a compound III;...

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Hauptverfasser: LI HUI, JIE YUANPING, JING HAOYU, PAN GUOJUN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a trans-2-amino-cyclopropyl formic acid derivative and a synthetic method thereof. The synthetic method includes the following steps that a compound II is used as a raw material and reacts with di-tert-butyl dicarbonate under the alkaline condition to prepare a compound III; the compound III and alkaline are subjected to hydrolysis reaction to obtain a compound IV; the compound IV and trifluoroacetic acid react for deprotection to prepare a compound I. The synthetic method of trans-2-amino-cyclopropyl formic acid derivative includes three-step reaction, is short in route, low in cost, high in yield, easy to prepare on a large scale and capable of keeping stability of a three-membered ring, and the total yield can reach 90.92%. 本发明公开了种反式2-氨基-环丙基甲酸衍生物及其合成方法,包括以下步骤:以化合物II为原料,在碱性条件下与二碳酸二叔丁酯反应制备得到化合物III;化合物III与碱发生水解反应制备得到化合物IV;化合物IV再与三氟乙酸反应脱保护制备得到化合物I。本发明的种反式2-氨基-环丙基甲酸衍生物的合成方法共3步反应,路线短、成本低廉、收率高、易于放大制备,且可以保持三元环的稳定性,总收率可达90.92%。