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Presented by :
Name : Al Imran
Roll : 27
Reg. : 225487
Sem. : 5th
Dhaka International University
Synthesis of Drug
Making drug
Considerations:
Drug must be able to be absorbed
into the body(A)
Drug must be distributed to the
right target(D)
We must know how the drug is
metabolized(M)
We must know how the drug get
excreted(E)
We must understand the toxicities
of the drug(T)

*Involves the use of organic synthesis
*Conversation of existing molecules into other useful
molecules
*A series of steps that lead from one or more starting
materials. Culminating in a finished product
*Drug chemistry
1. conversion of little molecules (leads)
into bigger molecules
2. synthesis of unnatural product from
natural product
3. modification of existing structures
Example
Paclitaxel (taxol): anti-cancer drug and rare
natural product
Example
Indynaprost
(Experimental
aggregation inhibitor)
Cylopentadiene
 Formation of C-C bond ( or removal of bonds, ex: alkenes to alkanes
oMethods and strategies
 Skeletal rearrangement
 Functional groups inter conversion (FGI)
*oxidation
*reduction
*substitution
*elimination
*addition
*others
General guidelines
Synthesis of Aspirin
acetylsalicylic acid, ASA
1.Phenolate ion reaction with CO2
under pressure to form o-hydroxy
benzoic acid (salicylic acid).
2. Salicylic acid reacts with acetic
anhydrite to form ASA.
Synthesis of paracetamol from phenol
(acetaminophen
In a small-scale laboratory, paracetamol is prepared by a
three-reaction sequence. First, nitration of phenol with
sodium nitrate gives a mixture of two isomers, from which
the wanted 4-nitrophenol (bp 279 °C) can easily be
separated by steam distillation. In this electrophilic
aromatic substitution reaction, phenol's oxygen is strongly
activating, thus the reaction requires only mild conditions
as compared to nitration of benzene itself. The nitro group
is then reduced to an amine, giving 4-aminophenol. This
reaction can be accomplished using sodium borohydride.
Finally, the amine is acetylated with acetic anhydride.The
industrial process is analogous, but hydrogenation is used
instead of the sodium borohydride reduction
synthesis of drug
synthesis of drug

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synthesis of drug

  • 1. Presented by : Name : Al Imran Roll : 27 Reg. : 225487 Sem. : 5th Dhaka International University Synthesis of Drug
  • 2. Making drug Considerations: Drug must be able to be absorbed into the body(A) Drug must be distributed to the right target(D) We must know how the drug is metabolized(M) We must know how the drug get excreted(E) We must understand the toxicities of the drug(T)
  • 3.  *Involves the use of organic synthesis *Conversation of existing molecules into other useful molecules *A series of steps that lead from one or more starting materials. Culminating in a finished product *Drug chemistry 1. conversion of little molecules (leads) into bigger molecules 2. synthesis of unnatural product from natural product 3. modification of existing structures
  • 4. Example Paclitaxel (taxol): anti-cancer drug and rare natural product
  • 6.  Formation of C-C bond ( or removal of bonds, ex: alkenes to alkanes oMethods and strategies  Skeletal rearrangement  Functional groups inter conversion (FGI) *oxidation *reduction *substitution *elimination *addition *others General guidelines
  • 7. Synthesis of Aspirin acetylsalicylic acid, ASA 1.Phenolate ion reaction with CO2 under pressure to form o-hydroxy benzoic acid (salicylic acid). 2. Salicylic acid reacts with acetic anhydrite to form ASA.
  • 8. Synthesis of paracetamol from phenol (acetaminophen
  • 9. In a small-scale laboratory, paracetamol is prepared by a three-reaction sequence. First, nitration of phenol with sodium nitrate gives a mixture of two isomers, from which the wanted 4-nitrophenol (bp 279 °C) can easily be separated by steam distillation. In this electrophilic aromatic substitution reaction, phenol's oxygen is strongly activating, thus the reaction requires only mild conditions as compared to nitration of benzene itself. The nitro group is then reduced to an amine, giving 4-aminophenol. This reaction can be accomplished using sodium borohydride. Finally, the amine is acetylated with acetic anhydride.The industrial process is analogous, but hydrogenation is used instead of the sodium borohydride reduction