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盐酸奥扎莫德的合成研究进展

Progress in the Synthesis of Ozanimod Hydrochloride
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摘要 盐酸奥扎莫德是一种新型口服1-磷酸鞘氨醇(S1P)受体调节剂,临床上用于治疗复发性多发性硬化。文章根据不同的合成思路对盐酸奥扎莫德及其重要中间体的合成方法进行总结和概括,并对各路线进行了简要评价。盐酸奥扎莫德骨架结构是(S)-1-氨基-4-(1,2,4- 二唑-3-基)-2,3-二氢-1H-茚。以4-氰基-2,3-二氢-1H-1-茚酮(2)为原料,应用手性辅助剂或不对称氢化催化剂,在2,3-二氢-1H-1-茚的1-位构建手性氨基;或者先将1-位羰基转换为手性羟基,再合成手性氨基。在2,3-二氢-1H-1-茚的4-位,原位合成噁二唑环。 Ozanimod hydrochloride, a new type of oral sphingosine 1-phosphate(S1P) receptor modulator,is clinically used for the treatment of relapsing multiple sclerosis. In this review, the synthetic methods of ozanimod hydrochloride and its key intermediates are summarized and evaluated based on different schemes described in the literature. The scaffold structure of ozanimod hydrochloride is(S)-1-amino-4-(1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-indene. Starting from 4-cyano-2,3-dihydro-1H-inden-1-one(2), chiral auxiliary agents or catalysts for asymmetric hydrogenation are used to construct the chiral amino group at the 1-position of 2,3-dihydro-1H-indene. Alternatively, the 1-carbonyl group is converted to the chiral hydroxyl before constructing the chiral amino group. The oxadiazole ring at the 4-position of 2,3-dihydro-1H-indene is synthesized in situ from 4-cyano group.
作者 王军政 王冬梅 杨天明 WANG Junzheng;WANG Dongmei;YANG Tianming(College of Pharmacy,Inner Mongolia Medical University,Hohhot O10110;Tianjin Key Lab.of Molecular Design and Drug Discovery,Tianjin Institute of Pharmaceutical Research,Tianjin 300301)
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2023年第8期1145-1156,共12页 Chinese Journal of Pharmaceuticals
关键词 盐酸奥扎莫德 1-磷酸鞘氨醇受体调节剂 合成 多发性硬化 ozanimod hydrochloride sphingosine 1-phosphate receptor modulator synthesis multiple sclerosis
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