【摘要】：(2R,4R)-4-甲基哌啶-2-甲酸通過酯化后,與(S)-2-[(叔丁氧羰基)氨基]-5-(3-硝基胍基)戊酸縮合,去Boc保護(hù)基,與3-甲基-8-喹啉磺酰氯縮合,再經(jīng)酯水解、Pd/C氫化還原喹啉環(huán)及脫硝基保護(hù)、精制得抗血栓藥物阿加曲班,總收率約12%,純度99.5%。該合成方法操作簡單,工藝穩(wěn)定,適合工業(yè)化生產(chǎn)。
[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.
【作者單位】： 北京陽光諾和藥物研究有限公司;河北中醫(yī)學(xué)院藥學(xué)院;
【基金】：河北省重點(diǎn)基礎(chǔ)研究項(xiàng)目(12966417D)
【分類號(hào)】：R914.5

【參考文獻(xiàn)】

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1 施猛;劉恩桂;夏春森;張俊s，

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