替诺福韦艾拉酚胺半D-(-)-酒石酸盐的制备及其稳定性研究

陈鸿翔; 毛建丰; 盛荣<sup>*</sup>

引用本文:	陈鸿翔,毛建丰,盛荣.替诺福韦艾拉酚胺半D-(-)-酒石酸盐的制备及其稳定性研究[J].中国现代应用药学,2017,34(7):978-981.
	CHEN Hongxiang,MAO Jianfeng,SHENG Rong.Preparation and Stability Research of Tenofoviral Afenamide D-(-)-Tartaric Acid Salt (2:1)[J].Chin J Mod Appl Pharm(中国现代应用药学),2017,34(7):978-981.

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替诺福韦艾拉酚胺半D-(-)-酒石酸盐的制备及其稳定性研究
陈鸿翔^1,2, 毛建丰², 盛荣¹
1.浙江大学药学院, 杭州 310058;2.杭州和泽医药科技有限公司, 杭州 310018

摘要:

目的制备替诺福韦艾拉酚胺半D-（-）-酒石酸盐，并开展稳定性研究。方法以替诺福韦（PMPA）为原料，经亚磷酸三苯酯缩合、二氯亚砜氯代、L-丙氨酸异丙酯缩合制得替诺福韦艾拉酚胺，再与D-（-）-酒石酸成盐。结果制得的替诺福韦艾拉酚胺半D-（-）-酒石酸盐，经1H-NMR、31P-NMR、MS确证结构，并与半富马酸盐进行稳定性比较。结论替诺福韦艾拉酚胺半D-（-）-酒石酸盐比半富马酸盐具有更好的稳定性，值得进一步开发。

关键词: 替诺福韦艾拉酚胺替诺福韦 D-(-)-酒石酸稳定性

DOI：10.13748/j.cnki.issn1007-7693.2017.07.010

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基金项目:

Preparation and Stability Research of Tenofoviral Afenamide D-(-)-Tartaric Acid Salt (2:1)

CHEN Hongxiang^1,2, MAO Jianfeng², SHENG Rong¹

1.College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China;2.Hangzhou Heze Pharmaceutical Technology Co., Ltd., Hangzhou 310018, China

Abstract:

OBJECTIVE To prepare tenofoviralafenamide D-(-)-tartaric acid salt (2:1) and to study its stability.METHODS Tenofovir (PMPA) was utiliazed as the starting material,condensed with triphenylphosphite,chlorinated by thionyl chloride,and then condensed with L-alanine isopropyl to obtain tenofoviralafenamide.Tenofoviralafenamide was reacted with D-(-)-tartaric acid to form the salt.RESULTS The chemical structure of tenofoviralafenamide D-(-)-tartaric acid salt (2:1) was confirmed by 1H-NMR,31P-NMR,MS.The stability of the compound was also studied and compared with tenofoviralafenamide hemifumarate.CONCLUSION The results showed that D-(-)-tartaric acid salt has a better effect on stability than hemifumarate salt.It is worthy to be futher developed.

Key words: tenofoviralafenamide D-(-)-tartaric acid stability