An efficient conversion of 5-nitroisatin into 5-nitroindole derivative |
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| Authors: | Torisawa Y Nishi T Minamikawa J |
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| Affiliation: | Process Research Laboratory, Second Tokushima Factory, Otsuka Pharmaceutical Co. Ltd., Japan. torisawa@fact.otsuka.co.jp |
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| 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. |
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