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SYNTHON APPROACH

SYNTHON APPROACH. Presented by Prof. Dr. A G Nikalje Head Department of Pharmaceutical Chemistry, Y.B. Chavan College Of Pharmacy Dr. Rafiq Zakaria Campus Aurangabad. TERMINOLOGIES. Synthon : An idealized fragment (cation or anion) formed by disconnection.

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SYNTHON APPROACH

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  1. SYNTHON APPROACH Presented by Prof. Dr. A G Nikalje Head Department of Pharmaceutical Chemistry, Y.B. Chavan College Of Pharmacy Dr. Rafiq Zakaria Campus Aurangabad

  2. TERMINOLOGIES • Synthon: An idealized fragment (cation or anion) formed by disconnection. • Target Molecule: A molecule to be synthesized. • Analysis/ Retro synthetic analysis: It is a process of break down of target molecule into available starting materials by FGI and disconnection. • Disconnection: An operation which involve breaking of bond between two atom to form possible starting materials. The symbol for FGI / disconnection is ( / ) • Reagent: Compound used in the practice of synthon. 2

  3. STEPS FOR DESIGNING A SYNTHESIS

  4. ANALYSIS • Recognize the functional groups in the target molecule. • Disconnect by known reliable methods using FGI if necessary to produce the right functional group. • Repeat as necessary to reach available starting materials. 4

  5. SYNTHESIS • Write out the plan according to the analysis, adding reagents and conditions. • Check that a rational order of events have been chosen. • Check the points about chemo selectivity so unwanted or side reactions don’t occur. (if necessary use protecting groups) • Modify the plan according to unexpected failures or successes in the laboratory. 5

  6. Aromatic electrophilic substitution

  7. Reagents for aromatic electrophilic substitution

  8. Aromatic side chains by functional group interconversion

  9. Aromatic side chains by functional group interconversion

  10. Aromatic compounds made by nucleophilic displacement of diazonium salt

  11. Direction and activation in aromatic electrophilic substitutuion

  12. Synthons for 1,n-di X synthesis

  13. 1) PARACETAMOL STEP 1: ANALYSIS

  14. STEP 2: SYNTHESIS PARACETAMOL

  15. 2)SACCHARINE STEP 1: ANALYSIS

  16. STEP 2: SYNTHESIS SACCHARINE

  17. N-(3,4-dichlorophenyl)propanamide ; Herbicide 3) PROPANIL: IUPAC name STEP 1: ANALYSIS

  18. STEP 2: SYNTHESIS PROPANIL

  19. 4) TRIMETHOPRIM STEP 1: ANALYSIS 19

  20. STEP 2: SYNTHESIS 20

  21. 5) FENTANYL: IUPAC Name N-(1-(2-Phenylethyl)-4-piperidinyl)-N-phenylpropanamide STEP 1: ANALYSIS 21

  22. STEP 2: SYNTHESIS 22

  23. 6) NIFEDIPINE STEP 1: ANALYSIS 23

  24. STEP 2: SYNTHESIS 24

  25. 7) ASPIRIN STEP 1: ANALYSIS 25

  26. STEP 2: SYNTHESIS Oxidation FC Alkylation 26

  27. 8) SALBUTAMOL STEP 1: ANALYSIS C-C 27

  28. STEP 2: SYNTHESIS AlCl3 FC Acylation TM 28

  29. 9) BENZOCAINE STEP 1: ANALYSIS 29

  30. STEP 2:SYNTHESIS 30

  31. 10) PROPRANOLOL STEP 1: ANALYSIS 31

  32. STEP 2: SYNTHESIS

  33. 11.RosiglitazoneAnalysis: C-O C-N

  34. Synthesis: Chloropyridine Rosiglitazone

  35. Best of luck 35

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