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海若qi

铁杆木虫 (著名写手)

[交流] 【求助】一下哌拉西林的合成方法

求助一下哌拉西林的合成方法,越多越好。谢谢!

[ Last edited by jw227 on 2009-9-27 at 09:11 ]
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hexinhua0920

木虫 (正式写手)

★ ★ ★ ★ ★ ★ ★
海若qi(金币+5,VIP+0):谢谢 9-27 20:05
472514568(金币+2,VIP+0):奖励积极回帖 9-28 14:47
【药物名称】Piperacillin
化学结构式(Chemical Structure):


参考文献No. 800605
标题: Piperacillin
作者: Loren, J.G.; Casta馿r, J.
来源: Drugs Fut 1978,3(11),829

合成路线图解说明:
The cyclization of diethyl oxalate (I) with N-ethylethylenediamine (II) in ethanol gives ethyl-2,3-dioxopiperazine (III), which by reaction first with trimethylsilyl chloride and triethytamine and then with phosgene in THF is converted into 4-ethyl-2,3-dioxopiperazine-1-carboxylic acid chloride (IV). Finally, this compound is condensed with 6-D-(-)-alpha-aminophenylacetamidopenicillanic acid (V) by means of triethylamine in THF - water.

参考文献No. 800606
标题: Penicillins and cephalosporins and process for producing the same
作者: Saikawa, I.; et al.
来源: DE 2519400; FR 2269937; FR 2320295; GB 1508062

合成路线图解说明:
The cyclization of diethyl oxalate (I) with N-ethylethylenediamine (II) in ethanol gives ethyl-2,3-dioxopiperazine (III), which by reaction first with trimethylsilyl chloride and triethytamine and then with phosgene in THF is converted into 4-ethyl-2,3-dioxopiperazine-1-carboxylic acid chloride (IV). Finally, this compound is condensed with 6-D-(-)-alpha-aminophenylacetamidopenicillanic acid (V) by means of triethylamine in THF - water.
2楼2009-09-27 09:49:07
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hexinhua0920

木虫 (正式写手)

不好意思,反应式没复制过来
3楼2009-09-27 09:49:58
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hexinhua0920

木虫 (正式写手)

4楼2009-09-27 10:20:19
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海若qi

铁杆木虫 (著名写手)

引用回帖:
Originally posted by hexinhua0920 at 2009-9-27 09:49:
【药物名称】Piperacillin
化学结构式(Chemical Structure):


参考文献No. 800605
标题: Piperacillin
作者: Loren, J.G.; Casta馿r, J.
来源: Drugs Fut 1978,3(11),829

合成路线图解说明:
...

能提供一下这两篇文献吗?
安心做人,认真做事!
5楼2009-09-27 20:06:06
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sywsf

铁杆木虫 (初入文坛)


小木虫(金币+0.5):给个红包,谢谢回帖交流
哌拉西林钠的合成工艺改进
6楼2009-09-28 14:28:52
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