An Improved and Impurity-Free Large-Scale Synthesis of Venlafaxine Hydrochloride

Mohanarangam Saravanan; Bollikonda Satyanarayana; Padi Pratap Reddy

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An Improved and Impurity-Free Large-Scale Synthesis of Venlafaxine Hydrochloride

机译：改进的无杂质盐酸文拉法辛的大规模合成

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An improved and impurity-free synthetic method for large-scale synthesis of venlafaxine hydrochloride was developed using inexpensive reagents. The overall yield obtained from this newly developed process is 55% in a highly pure state with >99.9% purity by HPLC. Venlafaxine, (RS)-1-[2-(Dimethylamino)-1-(4-methoxy-phenyl)ethyl]cyclohexanol hydrochloride (1), is a member of the cycloalkanol ethylamine scaffold and was the first dual-acting serotonin and norepinephrine reuptake inhibitor (SNRI), used for the treatment of depression and anxiety disorders. It was developed by Wyeth laboratories and is currently being marketed under the trade name Effexor.

机译：使用廉价的试剂，开发了一种用于大规模合成盐酸文拉法辛的无杂质合成方法。通过该新开发的方法获得的总产率在高纯状态下为55％，通过HPLC纯度> 99.9％。盐酸文拉法辛（RS）-1- [2-（二甲基氨基）-1-（4-甲氧基-苯基）乙基]环己醇盐酸盐（1）是环烷醇乙胺支架的成员，并且是第一个双重作用的5-羟色胺和去甲肾上腺素再摄取抑制剂（SNRI），用于治疗抑郁症和焦虑症。它由惠氏实验室开发，目前以商品名Effexor销售。

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《Organic process research & development》 |2011年第6期|共4页
作者
Mohanarangam Saravanan; Bollikonda Satyanarayana; Padi Pratap Reddy;
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机译：改进的无杂质盐酸文拉法辛的大规模合成
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An Improved and Impurity-Free Large-Scale Synthesis of Venlafaxine Hydrochloride

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