An efficient conversion of 5-nitroisatin into 5-nitroindole derivative.

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.

journal_name

Bioorg Med Chem Lett

authors

Torisawa Y,Nishi T,Minamikawa J

doi

10.1016/s0960-894x(01)00071-3

subject

Has Abstract

pub_date

2001-03-26 00:00:00

pages

829-32

issue

6

eissn

0960-894X

issn

1464-3405

pii

S0960894X01000713

journal_volume

11

pub_type

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