Course

Each module should include case studies or research articles related to the Total Synthesis and Purification Process

Unit 1

Unit1: Introduction to Total Synthesis (5 credits)

• Overview of Total Synthesis
• Historical Perspectives
• Importance in Drug Discovery
• Key Concepts and Terminology

Unit 2

Unit 2: Synthetic Strategies and Methodologies (15 credits)

• Inert reactions
• Protecting Groups: Protection for alcohols, carbonyl groups, carboxylic groups, and amino groups.
• Multi-Step Synthesis
• Total Synthesis (Analysis of Classic Total Syntheses, Discussion of Recent Advances, Application to Pharmaceutical Development)
• Applications of synthetic strategies in the total synthesis of selected organic molecules:
  1. Cholesterol
  2. Estrone
  3. Progesterone
  4. Reserpine
  5. Penicillin
  6. Prostaglandin

Unit 3

Unit 3: Purification process including Chromatographic Techniques (10 credits)

• Reaction work-up
• Recrystallisation
• TLC
• Column Chromatography
• Flash Chromatography
• HPLC (High-Performance Liquid Chromatography)

This course provides an in-depth exploration of total synthesis and purification processes in pharmaceutical chemistry. It covers fundamental principles, advanced techniques, and modern applications, preparing students for careers in research and development in the pharmaceutical industry. The Total Synthesis and Purification Process course is designed to give students a comprehensive understanding of the synthetic strategies and purification techniques used in the development of pharmaceutical compounds. Through a combination of theoretical lectures, and case studies of classical and recent total syntheses, students will gain a deep appreciation for the complexity and creativity involved in this field.

By the end of this course, students shall be able to

KNOWLEDGE

K1. Define essential terminology related to Total Synthesis.

K2. Apply retrosynthetic analysis techniques to plan synthetic routes for complex molecules.

K3. Comprehend the planning and execution of multi-step synthetic routes, optimizing for yield and selectivity.

K4. Analyse the synthetic challenges and solutions in the Total Synthesis

K5. Evaluate classical and recent case studies of total synthesis to understand practical applications and challenges

K6 Develop synthetic strategies in advanced organic synthesis techniques.

SKILL

S1. Execute multi-step synthetic routes with precision and efficiency. S2. Practice planning synthetic routes using retrosynthetic analysis.

S3. Perform various purification methods to achieve high-purity compounds. S4. Interpret data from synthesis and purification experiments accurately.

S5. Solve complex synthetic challenges using creative and innovative approaches.

S6. Develop hands-on skills in laboratory techniques essential for synthesis and purification

ATTITUDE

A1. Exhibit a strong sense of ethical responsibility

A2. Demonstrate meticulous attention to detail in laboratory work and data analysis. A3. Foster curiosity and innovation in approaching synthetic challenges.

A4. Embrace collaboration and teamwork in laboratory and research settings. A5. Adhere to all safety protocols in the laboratory.

A6. Uphold professional integrity and honesty in all scientific endeavors.

REFERENCE BOOKS

1. Francis Carey and Richard J. Sundberg, Advanced Organic Chemistry: Part B: Reaction and Synthesis, 5^th edition, Springer, 2008
2. O.C. Norman and J.M. Coxon, Principles of Organic Synthesis, 3rd Edition, CRC Press, 2017
3. L.F.Armarego and Christina Chai, Purification of Laboratory Chemicals, 6^th edition, Butterworth-Heinemann, 2009
4. Clayden, , Greeves, N., & Warren, S, Organic Chemistry, 2^nd edition, Oxford University Press, 2012

JOURNALS

Journal of the American Chemical Society (ACS Publications) https://pubs.acs.org/journal/jacsat

Journal of Organic Chemistry (ACS Publications) https://pubs.acs.org/journal/joceah

Organic & Biomolecular Chemistry (RSC) https://pubs.rsc.org/en/journals/journalissues/ob#!recentarticles&adv

ASSIGNMENTS:

1. Preparation of synthetic scheme for the total synthesis of selected compounds
2. Selection of solvent system for Flash Chromatography for synthesised compounds
3. SOP for finding out the solubility of the synthesised compounds
4. SOP for checking the purity of synthesised compounds by HPLC