An efficient conversion of 5-nitroisatin into 5-nitroindole derivative.
作者信息
Torisawa Y, Nishi T, Minamikawa J
机构信息
Process Research Laboratory, Second Tokushima Factory, Otsuka Pharmaceutical Co. Ltd., Japan.
出版信息
Bioorg Med Chem Lett. 2001 Mar 26;11(6):829-32. doi: 10.1016/s0960-894x(01)00071-3.
Abstract
Our process research on OPC-35564 revealed that a mixed borohydride reducing agent (ZrCl4/NaBH4) in DME (Itsuno system) afforded a rapid and direct conversion of N-alkyl-nitroisatin into nitroindole nucleus. Comparison with other reducing agents indicated the superiority of the present system and the key function of ZrCl4. For the manipulation of base-labile isatin, a useful procedure for its N-alkylation using Cu2CO3 is also presented.
摘要
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