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(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。
(2R, 4R) -4-methylpiperidine-2-carboxylic acid was esterified and reacted with (S) -2 - [(tert- butoxycarbonyl) amino] -5- (3-nitroguanidino) pentanoic acid Condensation, to Boc protective group, and 3-methyl-8-quinoline sulfonyl chloride condensation, and then ester hydrolysis, Pd / C hydrogenation of quinoline ring and denitrification protection, anti-thrombotic drug argatroban, Yield of about 12%, purity of 99.5%. The synthesis method is simple, process stable, suitable for industrial production.