摘要
目的合成盐酸帕洛诺司琼。方法以(S)-1,2,3,4-四氢-1-萘甲酸和(S)-3-氨基奎宁环胺为原料经酰化、还原、关环3步反应合成目标物。结果合成了盐酸帕洛诺司琼,总收率76%。结论本实验合成盐酸帕洛诺司琼,操作简便,提高了收率,缩短了反应时间。
Abstract
OBJECTIVE To synthesize palonosetron hydrochloride.METHODS Palonosetron hydrochloride was prepared from(S)-3-amino-quinuclidine and(S)-1,2,3.4-tetrahydro-l-naphalenecarboxylic acid as a starting material via three steps including acylation,reduction,and cyclization.RESULTS The total yield of palonosetron hydrochloride was 76%. CONCLUSION The easily manipulated and reliable procedure to synthesize palonosetron hydrochloride is applicable.
关键词
盐酸帕洛诺司琼 /
(S)-3-氨基奎宁环胺 /
(S)-1 /
2 /
3 /
4-四氢-1-萘甲酸 /
药物合成
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Key words
palonosetron hydrochloride /
(S)-3-amino-quinuclidine /
(S)-1 /
2 /
3 /
4-tetrahydro-1-naphalenecarboxylicacid /
drug synthesis
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唐田;吴永福.
盐酸帕洛诺司琼的合成[J]. 中国药学杂志, 2009, 44(10): 794-795
TNG Tin;WU Yong-fu.
Synthesis of Palonosetron Hydrochloride [J]. Chinese Pharmaceutical Journal, 2009, 44(10): 794-795
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参考文献
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[3] JAMES R，JOHN C，BRUCE A，et al. Process for preparing 2-(1-azabicyclo[2,2,2] oct-3-yl)-2,3,3A,4,5,6-hexahydro-1H-benz[de] isoquinolin-1-one：US，5510486 [P]. 1996-04-23.
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[5] CLARK R D，MILLER A B，BERGR J，et al. 2-(Quinuclidin-3-yl) pyrido[4,3-b]indol-1 -ones and isoquinolin-1-ones. Potent conformationally restricted 5-HT3 receptor Antagonists [J]. J Med Chem，1993，36 (18)：2645-2657.
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脚注
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