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[3-Dialkylamino-substituted 2H-1,4-benzoxazines].
Il Farmaco; Edizione Scientifica
|December 1, 1986
Summary
Researchers synthesized novel benzoxazine and pyrido-oxazine derivatives using phosphorus oxychloride. Some synthesized compounds exhibited weak depressant activity in pharmacological screenings.
Area of Science:
- Organic synthesis
- Medicinal chemistry
- Heterocyclic chemistry
Context:
- The synthesis of novel heterocyclic compounds is crucial for drug discovery.
- Benzoxazine and pyrido-oxazine scaffolds are present in various biologically active molecules.
Purpose:
- To synthesize novel N,N-dialkyl-2H-1,4-benzoxazine-2-carboxamides and related pyrido-oxazine derivatives.
- To investigate the chemical reactivity of substituted aminophenoxy malonamides and acetamides.
Summary:
- N,N,N',N'-Tetrasubstituted 2-(2-aminophenoxy)malonamides reacted with phosphorus oxychloride to yield N,N-dialkyl-3-(dialkylamino)-2H-1,4-benzoxazine-2-carboxamides.
- Similarly, 2-(2-amino-3-pyridyloxy)-N,N,N',N'-tetraethylmalonamide produced a pyrido[3,2-b][1,4]oxazine derivative.
- N,N-dialkyl-2-(2-aminophenoxy)acetamides also afforded 3-(dialkylamino)-2H-1,4-benzoxazines upon treatment with phosphorus oxychloride.
Impact:
- The synthesized compounds represent new chemical entities with potential applications in medicinal chemistry.
- Preliminary pharmacological screening indicated weak depressant activity in the Irwin test, suggesting avenues for further investigation.