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Two-step solution-phase synthesis of novel benzimidazoles utilizing a UDC (Ugi/de-Boc/cyclize) strategy

✍ Scribed by Paul Tempest; Vu Ma; Samuel Thomas; Zheng Hua; Michael G Kelly; Christopher Hulme

Book ID: 104230981
Publisher: Elsevier Science
Year: 2001
Tongue: French
Weight: 84 KB
Volume: 42
Category: Article
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(01)00919-4

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✦ Synopsis

The novel solution-phase synthesis of an array of biologically relevant benzimidazoles in a simple two-step procedure is revealed. Transformations are carried out in excellent yield by condensation of mono-Boc protected ortho-phenylene diamine and supporting Ugi reagents. Subsequent acid treatment and evaporation affords benzimidazoles in good to excellent yield. The described protocol represents a highly attractive solution-phase procedure for the rapid generation of benzimidazole libraries.

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