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Improved Process for the Preparation of 6-Chloro-5-(2-chloroethyl)oxindole
Organic Process Research & Development ( IF 3.1 ) Pub Date : September 20, 2008 , DOI: 10.1021/op800105j
Durgesh V. Nadkarni 1 , James F. Hallissey 1
Affiliation  

The current process for ziprasidone involves preparation and isolation of the key intermediate 6-chloro-5-(2-chloroethyl)oxindole. An improved process for the synthesis of this intermediate is reported here. The new process involves use of a novel Lewis acid-mediated selective deoxygenation of the precursor ketone with tetramethyldisiloxane. The new method affords the desired compound in a one-pot process obviating the need for isolation of the potentially hazardous precursor ketone. This process was successfully scaled up to multikilo scale.

中文翻译:

制备6-氯-5-(2-氯乙基)恶吲哚的改进方法

齐拉西酮的当前工艺涉及关键中间体6-氯-5-(2-氯乙基)恶吲哚的制备和分离。这里报道了一种改进的合成该中间体的方法。新方法涉及使用新颖的路易斯酸介导的前体酮与四甲基二硅氧烷的选择性脱氧。新方法通过一锅法制得所需化合物,无需分离潜在危险的前体酮。此过程已成功扩展到多公斤规模。
更新日期:2017-01-31
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