The subtle co-catalytic intervention of benzophenone in radical cation mediated cyclization - an improved synthesis of 2-(3 ',4 '-Dimethoxyphenyl) indoline

Document Type

Article

Publication Date

1-22-2008

Abstract

The addition of benzophenone to a FeCl(3)/CH(2)Cl(2) mixture in the presence of 3',4'-dimethoxy-2-acetamidostilbene 17 unexpectedly leads to a dramatic improvement in yield of the indoline 20 from 38% (previously reported by us) to 75.4%, after careful examination of a variety of reaction conditions. A catalytic cycle has been proposed that involves not only stilbene radical cations but also Fe(2+) promoted benzophenone ketyl radical formation which enhances cyclisation, suppresses dimerization and accounts for the virtually quantitative recovery of the benzophenone.

Keywords

radical cation, benzophenone, ketyl radical, maleic anhydride, oxidative cyclization, fecl3-promoted synthesis, alkaloids, derivatives, construction, dimerization, duocarmycins, cc-1065

Divisions

CHEMISTRY

Publication Title

Heterocycles

Volume

75

Issue

5

Additional Information

Department of Chemistry, Faculty of Science Building, University of Malaya, 50603 Kuala Lumpur, MALAYSIA

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