Solid-phase synthesis of 1,5-benzodiazepin-2-ones
1998; Elsevier BV; Volume: 39; Issue: 46 Linguagem: Inglês
10.1016/s0040-4039(98)01956-x
ISSN1873-3581
AutoresMatthias Schwarz, David Tumelty, Mark A. Gallop,
Tópico(s)Synthetic Organic Chemistry Methods
ResumoA solid-phase synthesis of polysubstituted 1,5-benzodiazepin-2-ones is described. Resin-bound 4-fluoro-3-nitrobenzoic acid was reacted with different β-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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