Presented by
Ch.Vamsi Anil Krishna(10AB1R0026)
Adderss:
Dept of Pharmaceutical Chemistry
Vignan Pharmacy College,Vadlamudi...
 Introduction
 Resolution Methods
 Resolving agents
 Stereoselectivity of action
 Chiral drug sales
 Chiral BIOCKBUS...
Chromatography
Widely used in development laboratories
Applicable to >99% of small molecules at analytical scale
Used i...
Methods for Preparing Chiral Compounds
Chromatography
A small scale
separation of the
chiral compounds in
labs.
Handling of chromatography
Kinetic Resolution
 Evalution of an historical process(> 100 years)
 Based upon different reaction rates of the isomers
...
Diastereomer Crystallisation
Most widely used technique in industry
Widely used in development
Cheap additives
Only on...
Resolving Agents
Stereoselectivity of action
S
Dextro
(+)
R
Levo
(-)
 Out 100 drugs sold
in 1994:
 Pure enantiomer
20%
 Racemate
21%
 No chiral
33%
 Out 100 drugs sold
in 1997:
 Pure en...
Racemic Mixture Single-enantiomer
Amphetamine(Benzedrine) Dextroamphetamine(Dexedrine)
Bupivacaine(Marcain) Levobupivacain...
Racemic Mixture Single-enantiomer
Modafinil(Provigil) Armodafinil(Nuvigil)
Ofloxacin(Floxin) Levofloxacin(Levaquin)
Omepra...
$ MILLIONS 1998 1999 2000
Cardio vascular $21,906 $24,805 $26,012
Antibiotics 19,756 20,907 23,265
Cancer 8,006 9,420 13,3...
Chiral technology is a rapidly
developing area
Chiral technology represents a huge
commercial business opportunity
that ha...
MARKET OF CHIRAL DRUGS
Single–enantiomer drug sales show a continuous growth worldwide
and many of the top selling drugs ...
 It is necessary to consider the chiral nature of a com-pound in
drug Research.
 Enantiomers of all chiral bioactive mol...
Chiral drug separation
Bingyun LiDonald T. Haynie Engineering and Physics, Bionano
systems Engineering Labo Biomedical ra...
This work was supported by
A.VISWANATH M.pharm (Ph.D)
Dept of Pharamaceutical chemisrty.
My beloved PRINCIPAL
Dr.P.SRINIVA...
Thank you
Chiral resolution by ch.vamsi anil krishna(Tinky)
Chiral resolution by ch.vamsi anil krishna(Tinky)
Chiral resolution by ch.vamsi anil krishna(Tinky)
Chiral resolution by ch.vamsi anil krishna(Tinky)
Chiral resolution by ch.vamsi anil krishna(Tinky)
Chiral resolution by ch.vamsi anil krishna(Tinky)
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Chiral resolution by ch.vamsi anil krishna(Tinky)

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this presentation gives the brief informatio about chiral compounds and its market , seperation and importance

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Chiral resolution by ch.vamsi anil krishna(Tinky)

  1. 1. Presented by Ch.Vamsi Anil Krishna(10AB1R0026) Adderss: Dept of Pharmaceutical Chemistry Vignan Pharmacy College,Vadlamudi, Guntur, Andhra Pradesh, India.
  2. 2.  Introduction  Resolution Methods  Resolving agents  Stereoselectivity of action  Chiral drug sales  Chiral BIOCKBUSTER DRUGS  Conclusion
  3. 3. Chromatography Widely used in development laboratories Applicable to >99% of small molecules at analytical scale Used in manufacturing scale
  4. 4. Methods for Preparing Chiral Compounds Chromatography
  5. 5. A small scale separation of the chiral compounds in labs.
  6. 6. Handling of chromatography
  7. 7. Kinetic Resolution  Evalution of an historical process(> 100 years)  Based upon different reaction rates of the isomers  Theoretically 100% yield Technology applied on limited scale to date
  8. 8. Diastereomer Crystallisation Most widely used technique in industry Widely used in development Cheap additives Only one isomer recovered per stage
  9. 9. Resolving Agents
  10. 10. Stereoselectivity of action S Dextro (+) R Levo (-)
  11. 11.  Out 100 drugs sold in 1994:  Pure enantiomer 20%  Racemate 21%  No chiral 33%  Out 100 drugs sold in 1997:  Pure enantiomer 30%  Racemate 9%  No chiral 57%
  12. 12. Racemic Mixture Single-enantiomer Amphetamine(Benzedrine) Dextroamphetamine(Dexedrine) Bupivacaine(Marcain) Levobupivacaine (Chirocaine) Cetirizine(Zyrtec/ Reactine) Levocetirizine(Xyzal) Citalopram(Celexa/ Cipramil) Escitalopram(Lexapro/ Cipralex) Methylphinidate(Ritalin) Dexmethylphenidate(Focalin)
  13. 13. Racemic Mixture Single-enantiomer Modafinil(Provigil) Armodafinil(Nuvigil) Ofloxacin(Floxin) Levofloxacin(Levaquin) Omeprazole(Prilosec) Esomeprazole(Nexium) Salbutamol(Ventolin) Levalbuterol(Xopenex) Zopiclone(Imovane) Eszopliclone(Lunesta)
  14. 14. $ MILLIONS 1998 1999 2000 Cardio vascular $21,906 $24,805 $26,012 Antibiotics 19,756 20,907 23,265 Cancer 8,006 9,420 13,360 Central Nervous System 7,027 8,592 13,720 Antiviral 6,131 7,540 13,446 Gastrointestinal 1,718 2,998 5,355 TOTAL $6,45,44 $74,262 $95,198
  15. 15. Chiral technology is a rapidly developing area Chiral technology represents a huge commercial business opportunity that has yet to be fully realised
  16. 16. MARKET OF CHIRAL DRUGS Single–enantiomer drug sales show a continuous growth worldwide and many of the top selling drugs are marketed as single enantiomers  Annual sales of chiral drugs: $133billion(2000), $172billion(2005)
  17. 17.  It is necessary to consider the chiral nature of a com-pound in drug Research.  Enantiomers of all chiral bioactive molecules must be separated and tested.  The FDA and regulatory authorities in Europe, China, and Japan have provided guidelines indicating that only the active enantiomer of a chiral drug should be brought to market.
  18. 18. Chiral drug separation Bingyun LiDonald T. Haynie Engineering and Physics, Bionano systems Engineering Labo Biomedical ratory, Center for Applied Physics Studies, Louisiana Tech University, Ruston, Louisiana, U.S.A The impact of chiral technology on the pharmaceutical industry ANDY RICHARDS & RAY McCAGUE
  19. 19. This work was supported by A.VISWANATH M.pharm (Ph.D) Dept of Pharamaceutical chemisrty. My beloved PRINCIPAL Dr.P.SRINIVASA BABU
  20. 20. Thank you
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