| 第 45 卷第 4 期 |  | Vol. 45 No. 4 | | 2015 年 8 月 | Aug 2015 |
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所屬欄目：醫藥及中間體
7-苯乙酰胺基-3-氯甲基頭孢烷酸對甲氧基芐酯C-3位鹵離子交換反應研究 |
| 王宗利，侯仲軻*，呂秋波，張宜仲，田黎黎，劉 沖
（浙江國邦藥業(yè)有限公司，浙江 上虞 312369） |
| 摘 要：通過(guò)調整7-苯乙酰胺基-3-氯甲基頭孢烷酸對甲氧基芐酯（GCLE）的C-3位鹵素交換試劑的種類(lèi)及用量，改變鹵素交換反應水量，控制反應溫度，明確反應時(shí)間，優(yōu)化了GCLE的C-3位鹵素交換的反應條件。結果表明：在n（碘化鈉）∶n（溴化鈉）∶n（GCLE）= 0.1∶0.9∶1.0，v（水）∶w（GCLE）= 1∶1，反應溫度35℃，反應時(shí)間5 h的條件下，GCLE轉化率99.71%，選擇性97.63%。 |
| 關(guān)鍵詞：GCLE；鹵素交換；反應選擇性 |
| 中圖分類(lèi)號：TQ254 文獻標識碼：A 文章編號：1009-9212（2015）04-0042-04 |
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| Study on the Reaction of Halogen Ion Exchange GCLE C-3 bit |
| WHANG Zong-li, HOU Zhong-ke*, L?譈 Qiu-bo, ZHANG Yi-zhong, TIAN Li-li, LIU Chong
(Zhejiang Guobang Pharmaceutical Co., Ltd., Shangyu 312369, China) |
| Abstract：The reaction conditions for GCLE[(6R-trans)-5-Thia-l-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 3-chloromethyl-8-oxo-7-[(phenylacetyl)amino]-diphenylmethyl ester] C-3 bit halogen exchange reaction were evaluated including different kind of type and amount of reagents, loading of water, and different reaction temperatures and time. The results indicated that the average conversion rate of GCLE was 99.71%, the average selectivity of the reaction was 97.63%, under the following reaction conditions: the molar ratio of sodium iodide, sodium bromide, GCLE is 0.1:0.9:1.0; the ratio of water volume and quality of GCLE is 1:1; reaction temperature was 35℃ and reaction time was 5 h. |
| Key words：GCLE; halogen exchange; reaction selectivity |
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作者簡(jiǎn)介：王宗利（1977-），男，江蘇睢寧人，工程師，主要從事藥物中間體的合成與研究工作（E-mail：jianqiu21@sina.com）。
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聯(lián) 系 人： 侯仲軻，研究員，主要從事藥物中間體的合成與研究（E-mail：houzk2008@hotmail.com）。
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收稿日期：2015-04-03
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