Improved Methodology for the Preparation of Chiral Amines

Table of Contents
Abstract.
Acknowledgment.
List of Abbreviations.
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1. Introduction to Chirality
1.1. Chiral Drugs 1
1.2. Isomers and Isomerism 2
1.3. Nature is Chiral 3
1.4. Chirality and Drug-Receptor Interaction 8
1.5. Sources of Enantiopure Substances 8
1.5.1. Synthesis of Enantiomerically Pure Compounds 9
1.5.2. Resolution 9
1.5.2.1. Preferential Crystallization 9
1.5.2.1. Diastereomer Crystallization 10
1.5.2.2. Kinetic Resolution 11
1.5.3. Chiral Pool Approach 12
1.5.4. Stereoselective Conversion of Prochiral Substrates to Enantiopure
Compounds (Asymmetric Synthesis) 15
1.5.5. Asymmetric Synthesis vs Kinetic Resolution vs Chiral Pool 18
1.6. α-Chiral Amines Defining Terms 19
1.7. α-Chiral Amines Importance 20
1.8. α-Chiral Amine Synthesis Different Methodologies 22
1.8.1. Imine and Enamide Synthesis 23
1.8.2. Enantioselective Reduction of Enamides 23
1.9. Conclusion 28
1.10. References 28
2. Imine Reduction
2.1. Historical View 34
2.2. Asymmetric Reduction of N-Phosphinoyl Imines 35
2.2.1. Synthesis of N-Phosphinoyl Imines 35
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