N-methylatation of isatins

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Table of contents

1. Introduction
1.1. Cognitive disorder
1.2. Alzheimer’s disease
1.2.1. Etiology and pathogenesis of Alzheimer’s disease
1.3. Current available drugs for treating Cognitive disorder
1.3.1. Cholinergic system
1.3.1.1. Cholinesterase inhibitors
1.3.1.2. Ach receptor modulators
1.3.2. Glutamatergic system
1.3.2.1. NMDA antagonist
1.4. Background to the present study
1.4.1. Angiotensin (IV)
1.4.2. Insulin–regulated aminopeptidase (IRAP)
1.4.3. Peptide inhibitors
1.4.4. Non-peptide inhibitors
1.4.5. HTS
2. Aim of the present study
2.1. Structural modifications
3. Microwave-assisted synthesis
4. N-methylation of isatins
4.1. SN2 reaction
4.2. Reaction mechanism for N-methylation of isatins
4.3. Method and Results
5. Synthesis of the halogenated analogues
5.1. Imine formation
5.2. Reaction mechanism
5.3. Method
5.4 Results and discussion
6. Other modifications
6.1. Method development
6.2. Optimization results and discussion for the synthesis of 6e
6.3. Optimization results and discussion for the synthesis of 8b
6.4. Results for the synthesis of 8b-d using the method developed
6.5. Optimization results and discussion of the synthesis of 6
6.6. Results for the synthesis of 6e using the method developed
6.7. Results for the synthesis of 6e-f using the method developed
7. Biological evaluation
7.1. Initial SAR study results
7.2. Biological assays results
8. Conclusion and outlook
9. Acknowledgements
10. Experimental data
11. References