| 第 45 卷第 5 期 |  | Vol. 45 No. 5 | | 2015 年 10 月 | Oct 2015 |
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所屬欄目：醫藥及中間體
西他沙星及其有關(guān)物質(zhì)D-2的合成 |
| 陳言德，楊 勇，周士闊，呂曉霞
（江蘇吳中醫藥集團有限公司，江蘇 蘇州 215168） |
| 摘 要：合成了西他沙星及其有關(guān)物質(zhì)D-2，總收率78.7%。并對其進(jìn)行了MS、HNMR和TG等表征；研究了氫化脫芐的反應條件、縮合反應的后處理優(yōu)化和脫Boc的鹽酸用量，優(yōu)化的條件為：脫芐反應10%鈀炭，回流反應0.5 h，縮合反應后處理溶劑比例v（乙腈）∶v（水）=1∶2，脫Boc的鹽酸用量為15 mol倍量。 |
| 關(guān)鍵詞：西他沙星；D-2；氫化；脫芐 |
| 中圖分類(lèi)號：R978.5 文獻標識碼：A 文章編號：1009-9212（2015）05-0030-04 |
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| Synthesis of Sitafloxacin and Its Related Substance D-2 |
| CHEN Yan-de, YANG Yong, ZHOU Shi-kuo, L?譈 Xiao-xia
(Jiangsu wuzhong pharmaceutical group, Suzhou 215168, China) |
| Abstract：Sitafloxacin and its related substance D-2 were obtained with a total product yield of 78.7%. The structures of Sitafloxacin and intermediates from the step reactions were confirmed using MS, HNMR and TG. The optimal conditions for each step reaction were as following: in the debenzylation reaction,10% of Pd/C with a reflux time of 0.5 h was adopted; in the post-treatment of condensation reaction, a mixed solvent of water and acetonitrile with a volume ratio of 2∶1 was used; in the deprotection of N-boc reaction, the amount of hydrochloric acid was 15 times of the substrate in mole. |
| Key words：sitafloxacin; D-2; hydrogenation; debenzylation |
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基金項目：蘇州市科技發(fā)展計劃項目（ZXY2012004）。
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作者簡(jiǎn)介：陳言德（1984-），男，江蘇泗洪人，工程師，碩士，主要從事化學(xué)藥物開(kāi)發(fā)工作（E-mail：chenyande86@163.com）。
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收稿日期： 2015-08-2
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