basic knowledge about synthesis of drug.

1. Presented by :
Al Imran
B.Pharm(DIU)
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

5. Example
Indynaprost
(Experimental
aggregation inhibitor)
Cylopentadiene

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