阿加曲班的合成
发布时间：2018-09-13 07:14
【摘要】：(2R,4R)-4-甲基哌啶-2-甲酸通过酯化后,与(S)-2-[(叔丁氧羰基)氨基]-5-(3-硝基胍基)戊酸缩合,去Boc保护基,与3-甲基-8-喹啉磺酰氯缩合,再经酯水解、Pd/C氢化还原喹啉环及脱硝基保护、精制得抗血栓药物阿加曲班,总收率约12%,纯度99.5%。该合成方法操作简单,工艺稳定,适合工业化生产。
[Abstract]:(2R 4R) -4-methylpiperidine -2-formic acid was condensed with (S) -2- [(tert-butyloxycarbonyl) amino] -5- (3-nitroguanidinyl) valeric acid after esterification, Boc protection group was removed, condensed with 3-methyl-8-quinolinyl chloride, and then hydrolyzed by ester, the quinoline ring was hydrogenated to reduce quinoline ring and denitro protection. The antithrombotic drug Agatriban was purified with a total yield of about 12 and a purity of 99.5. The synthetic method is simple in operation, stable in process and suitable for industrial production.
【作者单位】： 北京阳光诺和药物研究有限公司;河北中医学院药学院;
【基金】：河北省重点基础研究项目(12966417D)
【分类号】：R914.5
[Abstract]:(2R 4R) -4-methylpiperidine -2-formic acid was condensed with (S) -2- [(tert-butyloxycarbonyl) amino] -5- (3-nitroguanidinyl) valeric acid after esterification, Boc protection group was removed, condensed with 3-methyl-8-quinolinyl chloride, and then hydrolyzed by ester, the quinoline ring was hydrogenated to reduce quinoline ring and denitro protection. The antithrombotic drug Agatriban was purified with a total yield of about 12 and a purity of 99.5. The synthetic method is simple in operation, stable in process and suitable for industrial production.
【作者单位】： 北京阳光诺和药物研究有限公司;河北中医学院药学院;
【基金】：河北省重点基础研究项目(12966417D)
【分类号】：R914.5
【参考文献】
相关期刊论文 前3条
1 施猛;刘恩桂;夏春森;张俊s，
本文编号：2240446
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