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High-throughput combinatorial synthesis of substituted benzimidazolones

✍ Scribed by Pi-Chi Pan; Chung-Ming Sun

Book ID
104262059
Publisher
Elsevier Science
Year
1999
Tongue
French
Weight
245 KB
Volume
40
Category
Article
ISSN
0040-4039

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✦ Synopsis

An efficient liquid-phase synthesis of substituted benzimidazolones 7 is des~bed. Resin bound ofluoronitrobenzene 1 is reacted with various primary amines to afford o-nitroaniline derivatives 2. Subsequent reduction of the aromatic nitro group followed by cyclization gives a PEG bound benzimidazole-2-one 4. N-Alkylation of this resin bound scaffold 4 with several electrophiles gives the resulting library in excellent yield and purity after cleavage.

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✍ Viktor KrchňÑk πŸ“‚ Article πŸ“… 1999 πŸ› John Wiley and Sons 🌐 English βš– 93 KB πŸ‘ 2 views

A semi-automated technique for massive parallel solid-phase organic synthesis based on a "split only" strategy is described. Two different types of purpose-oriented reaction vessels are used. The initial steps are performed in domino blocks, and the resin-bound intermediates then split into wells of