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M.Pharm Pharmaceutical Chemistry Syllabus

Pharmaceutical Chemistry is the M.Pharm specialisation on drug design, synthesis and analysis of drug molecules. This page gives the complete syllabus of the branch as prescribed by the Pharmacy Council of India, subject by subject and unit by unit.

Source: Pharmacy Council of India (PCI), The Revised Regulations for the Master of Pharmacy Degree Program, Credit Based Semester System, and the M.Pharm syllabus prescribed by the Pharmacy Council of India. The syllabus below is reproduced from the PCI syllabus, unit by unit.

Semester 1

MPC101T Modern Pharmaceutical Analytical Techniques

Subject notes: MPC101T Modern Pharmaceutical Analytical Techniques notes

Unit 1: Spectroscopy I

Unit 2: NMR spectroscopy

Quantum numbers and their role in NMR, principle, instrumentation, solvent requirement in NMR, relaxation process, NMR signals in various compounds, chemical shift, factors influencing chemical shift, spin-spin coupling, coupling constant, nuclear magnetic double resonance, brief outline of principles of FT-NMR and 13C NMR, applications of NMR spectroscopy.

Unit 3: Mass spectroscopy

Principle, theory, instrumentation of mass spectroscopy, different types of ionization like electron impact, chemical, field, FAB and MALDI, APCI, ESI, APPI, analyzers of quadrupole and time of flight, mass fragmentation and its rules, metastable ions, isotopic peaks, applications of mass spectroscopy.

Unit 4: Chromatography

Principle, apparatus, instrumentation, chromatographic parameters, factors affecting resolution, isolation of drug from excipients, data interpretation and applications of: thin layer chromatography, high performance thin layer chromatography, ion exchange chromatography, column chromatography, gas chromatography, high performance liquid chromatography, ultra high performance liquid chromatography, affinity chromatography, gel chromatography.

Unit 5: Electrophoresis and X-ray crystallography

Electrophoresis: principle, instrumentation, working conditions, factors affecting separation and applications of paper electrophoresis, gel electrophoresis, capillary electrophoresis, zone electrophoresis, moving boundary electrophoresis, isoelectric focusing. X-ray crystallography: production of X rays, different X ray diffraction methods, Bragg law, rotating crystal technique, X ray powder technique, types of crystals, applications of X ray diffraction.

Unit 6: Potentiometry and thermal techniques

Potentiometry: principle, working, ion selective electrodes, applications. Thermal techniques: principle, thermal transitions and instrumentation (heat flux and power compensation designs), modulated DSC, hyper DSC, experimental parameters (sample preparation, experimental conditions, calibration, heating and cooling rates, resolution, source of errors) and their influence, advantages and disadvantages, pharmaceutical applications. Differential thermal analysis (DTA): principle, instrumentation, advantages and disadvantages, pharmaceutical applications, derivative differential thermal analysis (DDTA). TGA: principle, instrumentation, factors affecting results, advantages and disadvantages, pharmaceutical applications.

MPC102T Advanced Organic Chemistry - I

Subject notes: MPC102T Advanced Organic Chemistry - I notes

Unit 1: Basic Aspects of Organic Chemistry

  1. Organic intermediates: carbocations, carbanions, free radicals, carbenes and nitrenes. Their method of formation, stability and synthetic applications.
  2. Types of reaction mechanisms and methods of determining them.
  3. Detailed knowledge regarding the reactions, mechanisms and their relative reactivity and orientations with respect to addition, substitution, elimination and rearrangement reactions.
  4. Chemistry of enolates.

Unit 2: Study of Mechanism and Synthetic Applications of Named Reactions

Ugi reaction, Brook rearrangement, Ullmann coupling reactions, Dieckmann reaction, Doebner-Miller reaction, Sandmeyer reaction, Mitsunobu reaction, Mannich reaction, Vilsmeyer-Haack reaction, Sharpless asymmetric epoxidation, Baeyer-Villiger oxidation, Shapiro and Suzuki reaction, ozonolysis and Michael addition reaction.

Unit 3: Synthetic Reagents and Applications, and Protecting Groups

Synthetic reagents: aluminium isopropoxide, N-bromosuccinimide, diazomethane, dicyclohexylcarbodiimide, Wilkinson reagent, Wittig reagent, osmium tetroxide, titanium chloride, diazopropane, diethyl azodicarboxylate, triphenylphosphine, benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP).Protecting groups: role of protection in organic synthesis. Protection for the hydroxyl group, including 1,2- and 1,3-diols: ethers, esters, carbonates, cyclic acetals and ketals. Protection for the carbonyl group: acetals and ketals. Protection for the carboxyl group: amides and hydrazides, esters. Protection for the amino group and amino acids: carbamates and amides.

Unit 4: Heterocyclic Chemistry

Organic name reactions with their respective mechanism and application involved in synthesis of drugs containing five membered, six membered and fused heterocycles: Debus-Radziszewski imidazole synthesis, Knorr pyrazole synthesis, Pinner pyrimidine synthesis, Combes quinoline synthesis, Bernthsen acridine synthesis, Smiles rearrangement and Traube purine synthesis.Synthesis of representative drugs containing these heterocyclic nuclei: ketoconazole, clotrimazole, metronidazole, miconazole, celecoxib, antipyrine, metamizole sodium, terconazole, alprazolam, triamterene, sulfamerazine, trimethoprim, hydroxychloroquine, quinine, chloroquine, quinacrine, amsacrine, prochlorperazine, promazine, chlorpromazine, theophylline, mercaptopurine and thioguanine.

Unit 5: Synthon Approach and Retrosynthesis Applications

Basic principles, terminologies and advantages of retrosynthesis; guidelines for dissection of molecules. Functional group interconversion and addition (FGI and FGA). C-X disconnections; C-C disconnections: alcohols and carbonyl compounds; 1,2-, 1,3-, 1,4-, 1,5- and 1,6-difunctionalised compounds. Strategies for synthesis of three, four, five and six membered rings and heterocyclic rings. Sequence of events in disconnection.

MPC103T Advanced Medicinal Chemistry

Subject notes: MPC103T Advanced Medicinal Chemistry notes

Unit 1: Drug Discovery

Stages of drug discovery, lead discovery; identification, validation and diversity of drug targets. Biological drug targets: receptors, types, binding and activation, theories of drug receptor interaction, drug receptor interactions, agonists vs antagonists, artificial enzymes.

Unit 2: Prodrug Design and Analog Design

a) Prodrug design: basic concept, carrier linked prodrugs and bioprecursors, prodrugs of functional groups, prodrugs to improve patient acceptability, drug solubility, drug absorption and distribution, site specific drug delivery and sustained drug action. Rationale of prodrug design and practical considerations of prodrug design. b) Combating drug resistance: causes for drug resistance, strategies to combat drug resistance in antibiotics and anticancer therapy, genetic principles of drug resistance. c) Analog design: introduction, classical and non-classical bioisosteric replacement strategies, rigid analogs, alteration of chain branching, changes in ring size, ring position isomers, design of stereoisomers and geometric isomers, fragments of a lead molecule, variation in interatomic distance.

Unit 3: Medicinal Chemistry Aspects of Drug Classes, and Stereochemistry and Drug Action

a) Systematic study, SAR, mechanism of action and synthesis of new generation molecules of the following classes of drugs: anti-hypertensive drugs, psychoactive drugs, anticonvulsant drugs, H1 and H2 receptor antagonists, COX-1 and COX-2 inhibitors, adrenergic and cholinergic agents, antineoplastic agents and antiviral agents. b) Stereochemistry and drug action: realisation that stereoselectivity is a prerequisite for evolution, role of chirality in selective and specific therapeutic agents, case studies, enantioselectivity in drug absorption, metabolism, distribution and elimination.

Unit 4: Rational Design of Enzyme Inhibitors

Enzyme kinetics and principles of enzyme inhibitors, enzyme inhibitors in medicine, enzyme inhibitors in basic research, rational design of non-covalently and covalently binding enzyme inhibitors.

Unit 5: Peptidomimetics

Therapeutic values of peptidomimetics, design of peptidomimetics by manipulation of the amino acids, modification of the peptide backbone, incorporating conformational constraints locally or globally. Chemistry of prostaglandins, leukotrienes and thromboxanes.

MPC104T Chemistry of Natural Products

Subject notes: MPC104T Chemistry of Natural Products notes

Unit 1: Study of natural products as leads for new pharmaceuticals

a) Drugs affecting the central nervous system: morphine alkaloids b) Anticancer drugs: paclitaxel and docetaxel, etoposide and teniposide c) Cardiovascular drugs: lovastatin, teprotide and dicoumarol d) Neuromuscular blocking drugs: curare alkaloids e) Antimalarial drugs and analogues f) Chemistry of macrolide antibiotics (erythromycin, azithromycin, roxithromycin and clarithromycin) and beta-lactam antibiotics (cephalosporins and carbapenems)

Unit 2: Alkaloids, flavonoids and steroids

a) Alkaloids: general introduction, classification, isolation, purification, molecular modification and biological activity; general methods of structural determination; structural elucidation and stereochemistry of ephedrine, morphine, ergot, emetine and reserpine b) Flavonoids: introduction, isolation and purification; general methods of structural determination; structural elucidation of quercetin c) Steroids: general introduction, chemistry of sterols, sapogenins and cardiac glycosides; stereochemistry and nomenclature of steroids; chemistry of contraceptive agents, male and female sex hormones (testosterone, estradiol, progesterone), adrenocorticoids (cortisone), contraceptive agents and steroids (vitamin D)

Unit 3: Terpenoids and vitamins

a) Terpenoids: classification, isolation, isoprene rule and general methods of structural elucidation; structural elucidation of monoterpenoids (citral, menthol, camphor), diterpenoids (retinol, phytol, taxol) and triterpenoids (squalene, ginsenoside); carotenoids (beta carotene) b) Vitamins: chemistry and physiological significance of vitamins A, B1, B2, B12, C, E, folic acid and niacin

Unit 4: Recombinant DNA technology, drug discovery and indigenous crude drugs

a) Recombinant DNA technology and drug discovery: rDNA technology, hybridoma technology, new pharmaceuticals derived from biotechnology, oligonucleotide therapy; gene therapy: introduction, clinical application and recent advances; principles of RNA and DNA estimation b) Active constituents of certain crude drugs used in the indigenous system: diabetic therapy (Gymnema sylvestre, Salacia reticulata, Pterocarpus marsupium, Swertia chirata, Trigonella foenum-graecum); liver dysfunction (Phyllanthus niruri); antitumor (Curcuma longa Linn.)

Unit 5: Structural characterization of natural compounds

Structural characterization of natural compounds using IR, 1H NMR, 13C NMR and MS spectroscopy of specific drugs, for example penicillin, morphine, camphor, vitamin D, quercetin and digitalis glycosides.

Practicals and Seminar

Semester 2

MPC201T Advanced Spectral Analysis

Subject notes: MPC201T Advanced Spectral Analysis notes

Unit 1: UV and IR spectroscopy

Woodward-Fieser rules for 1,3-butadienes, cyclic dienes and alpha,beta-unsaturated carbonyl compounds, and interpretation of enones. ATR-IR. IR interpretation of organic compounds.

Unit 2: NMR spectroscopy

1-D and 2-D NMR. NOESY and COSY, HETCOR, INADEQUATE techniques. Interpretation of organic compounds.

Unit 3: Mass spectroscopy

Mass fragmentation and its rules. Fragmentation of important functional groups like alcohols, amines, carbonyl groups and alkanes. Metastable ions. McLafferty rearrangement. Ring rule. Isotopic peaks. Interpretation of organic compounds.

Unit 4: Chromatography

Principle, instrumentation and applications of the following: a) GC-MS, b) GC-AAS, c) LC-MS, d) LC-FTIR, e) LC-NMR, f) CE-MS, g) High Performance Thin Layer Chromatography, h) Supercritical fluid chromatography, i) Ion chromatography, j) Ion Exclusion Chromatography (I-EC), k) Flash chromatography.

Unit 5: Thermal methods, Raman spectroscopy and radioimmunoassay

a) Thermal methods of analysis: introduction, principle, instrumentation and applications of DSC, DTA and TGA. b) Raman spectroscopy: introduction, principle, instrumentation and applications. c) Radioimmunoassay: biological standardization, bioassay, ELISA, radioimmunoassay of digitalis and insulin.

MPC202T Advanced Organic Chemistry - II

Subject notes: MPC202T Advanced Organic Chemistry - II notes

Unit 1: Green Chemistry

a. Introduction, principles of green chemistry. b. Microwave assisted reactions: merits and demerits of its use, increased reaction rates, mechanism, superheating effects of microwave, effects of solvents in microwave assisted synthesis, microwave technology in process optimization, its applications in various organic reactions and heterocycles synthesis. c. Ultrasound assisted reactions: types of sonochemical reactions, homogeneous, heterogeneous liquid-liquid and liquid-solid reactions, synthetic applications. d. Continuous flow reactors: working principle, advantages and synthetic applications.

Unit 2: Chemistry of Peptides

a. Coupling reactions in peptide synthesis. b. Principles of solid phase peptide synthesis, t-BOC and FMOC protocols, various solid supports and linkers: activation procedures, peptide bond formation, deprotection and cleavage from resin, low and high HF cleavage protocols, formation of free peptides and peptide amides, purification and case studies, site-specific chemical modifications of peptides. c. Segment and sequential strategies for solution phase peptide synthesis with any two case studies. d. Side reactions in peptide synthesis: deletion peptides, side reactions initiated by proton abstraction, protonation, overactivation and side reactions of individual amino acids.

Unit 3: Photochemical Reactions and Pericyclic Reactions

Photochemical reactions: basic principles of photochemical reactions, photo-oxidation, photo-addition and photo-fragmentation. Pericyclic reactions: mechanism, types of pericyclic reactions such as cycloaddition, electrocyclic reaction and sigmatropic rearrangement reactions with examples.

Unit 4: Catalysis

a. Types of catalysis, heterogeneous and homogeneous catalysis, advantages and disadvantages. b. Heterogeneous catalysis: preparation, characterization, kinetics, supported catalysts, catalyst deactivation and regeneration, some examples of heterogeneous catalysis used in synthesis of drugs. c. Homogeneous catalysis: hydrogenation, hydroformylation, hydrocyanation, Wilkinson catalysts, chiral ligands and chiral induction, Ziegler-Natta catalysts, some examples of homogeneous catalysis used in synthesis of drugs. d. Transition-metal and organo-catalysis in organic synthesis: metal-catalyzed reactions. e. Biocatalysis: use of enzymes in organic synthesis, immobilized enzymes/cells in organic reactions. f. Phase transfer catalysis: theory and applications.

Unit 5: Stereochemistry and Asymmetric Synthesis

a. Basic concepts in stereochemistry: optical activity, specific rotation, racemates and resolution of racemates, the Cahn, Ingold, Prelog (CIP) sequence rule, meso compounds, pseudoasymmetric centres, axes of symmetry, Fischer's D and L notation, cis-trans isomerism, E and Z notation. b. Methods of asymmetric synthesis using chiral pool, chiral auxiliaries and catalytic asymmetric synthesis, enantiopure separation and stereoselective synthesis with examples.

MPC203T Computer Aided Drug Design

Subject notes: MPC203T Computer Aided Drug Design notes

Unit 1: Introduction to Computer Aided Drug Design (CADD) and QSAR Basics

a. Introduction to Computer Aided Drug Design (CADD): history, different techniques and applications. b. Quantitative Structure Activity Relationships: basics, history and development of QSAR. c. Physicochemical parameters and methods to calculate physicochemical parameters: Hammett equation and electronic parameters (sigma), lipophilicity effects and parameters (log P, pi substituent constant), steric effects (Taft steric and MR parameters). d. Experimental and theoretical approaches for the determination of these physicochemical parameters.

Unit 2: Quantitative Structure Activity Relationships: Applications

a. Hansch analysis, Free Wilson analysis and relationship between them, advantages and disadvantages. b. Deriving 2D-QSAR equations. c. 3D-QSAR approaches and contour map analysis. d. Statistical methods used in QSAR analysis and importance of statistical parameters.

Unit 3: Molecular Modeling and Docking

a. Molecular and quantum mechanics in drug design. b. Energy minimization methods: comparison between global minimum conformation and bioactive conformation. c. Molecular docking and drug receptor interactions: rigid docking, flexible docking and extra precision docking. Agents acting on enzymes such as DHFR, HMG-CoA reductase and HIV protease, cholinesterase (AChE and BChE).

Unit 4: Molecular Properties and Drug Design

a. Prediction and analysis of ADMET properties of new molecules and its importance in drug design. b. De novo drug design: receptor/enzyme interaction and its analysis, receptor/enzyme cavity size prediction, predicting the functional components of cavities, fragment based drug design. c. Homology modeling and generation of 3D structure of protein.

Unit 5: Pharmacophore Mapping and Virtual Screening

a. Concept of pharmacophore, pharmacophore mapping, identification of pharmacophore features and pharmacophore modeling; conformational search used in pharmacophore mapping. b. In silico drug design and virtual screening techniques: similarity based methods and pharmacophore based screening, structure based in silico virtual screening protocols.

MPC204T Pharmaceutical Process Chemistry

Subject notes: MPC204T Pharmaceutical Process Chemistry notes

Unit 1: Process Chemistry

Introduction, synthetic strategy. Stages of scale up process: bench, pilot and large scale process. In-process control and validation of large scale process. Case studies of some scale up process of APIs. Impurities in API, types and their sources including genotoxic impurities.

Unit 2: Unit Operations

a) Extraction: liquid equilibria, extraction with reflux, extraction with agitation, counter current extraction. b) Filtration: theory of filtration, pressure and vacuum filtration, centrifugal filtration. c) Distillation: azeotropic and steam distillation. d) Evaporation: types of evaporators, factors affecting evaporation. e) Crystallization: crystallization from aqueous and nonaqueous solutions, factors affecting crystallization, nucleation. Principle and general methods of preparation of polymorphs, hydrates, solvates and amorphous APIs.

Unit 3: Unit Processes I

a) Nitration: nitrating agents, aromatic nitration, kinetics and mechanism of aromatic nitration, process equipment for technical nitration, mixed acid for nitration. b) Halogenation: kinetics of halogenations, types of halogenations, catalytic halogenations. Case study on industrial halogenation process. c) Oxidation: introduction, types of oxidative reactions, liquid phase oxidation with oxidizing agents. Nonmetallic oxidizing agents such as H2O2, sodium hypochlorite, oxygen gas, ozonolysis.

Unit 4: Unit Processes II

a) Reduction: catalytic hydrogenation, heterogeneous and homogeneous catalyst; hydrogen transfer reactions, metal hydrides. Case study on industrial reduction process. b) Fermentation: aerobic and anaerobic fermentation. Production of i. antibiotics: penicillin and streptomycin; ii. vitamins: B2 and B12; iii. statins: lovastatin, simvastatin. c) Reaction progress kinetic analysis. i. Streamlining reaction steps, route selection; ii. characteristics of expedient routes, characteristics of cost-effective routes, reagent selection, families of reagents useful for scale-up.

Unit 5: Industrial Safety

a) MSDS (Material Safety Data Sheet), hazard labels of chemicals and Personal Protection Equipment (PPE). b) Fire hazards, types of fire and fire extinguishers. c) Occupational Health and Safety Assessment Series (printed OHSAS-1800, read OHSAS 18001) and ISO-14001 (Environmental Management System), effluents and its management.

Practicals and Seminar

Semester 3 and 4

Semester 3 and Semester 4 are common to all M.Pharm specialisations. They cover Research Methodology and Biostatistics (MRM301T), journal club, discussion and presentation, and research work. The full common structure is given on the M.Pharm Common Semester 3 and 4 Syllabus page.