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Solid-phase synthesis of 1,5-benzodiazepin-2-ones

✍ Scribed by Matthias K. Schwarz; David Tumelty; Mark A. Gallop

Publisher
Elsevier Science
Year
1998
Tongue
French
Weight
269 KB
Volume
39
Category
Article
ISSN
0040-4039

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✦ Synopsis

A solid-phase synthesis ofpolysubstituted 1,5-benzodiazepin-2-ones is described. Resinbound 4-fluoro-3-nitrobanzoic acid was reacted with different ~amino acids, followed by nitro group reduction and formation of the seven-membered ring. Subsequent alkylations at N(5) and N(1) afforded the title compounds in high purities and yields.

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