0910 Sf Master Bloque1
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The document provides an overview of drug synthesis strategies and methods. It discusses sources of drugs including total synthesis, isolation from natural sources, and chemical modification of natural products. Retrosynthetic analysis is introduced as a strategy for designing synthetic routes, focusing on disconnections, synthons, and guidelines for choosing disconnections. Methods for controlling stereochemistry including protecting groups, stereoselective and stereospecific reactions are also summarized.
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To characterize the antioxidants in food, it is necessary to know:
-How much antioxidant is contained in the food.
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-If the antioxidants in the blood make their way to the intended body cells.
-Do the antioxidants help the cells to defend themselves against oxygen radicals? May it be given by increasing the production of the cell's own defense enzymes or by direct chemical neutralization of the radicals?
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To characterize the antioxidants in food, it is necessary to know:
- How much antioxidant is contained in the food.
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- If the antioxidants in the blood make their way to the intended body cells.
- Do the antioxidants help the cells to defend themselves against oxygen radicals? May it be given by increasing the production of the cell's own defense enzymes or by direct chemical neutralization of the radicals?
iNSTITUT KURZ performs all laboratory analysis of antioxidants in food!
VISIT OUR WEBSITE: www.institut-kurz.com/
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To characterize the antioxidants in food, it is necessary to know:
-How much antioxidant is contained in the food.
-Are the antioxidants absorbed from the food to the blood?
-If the antioxidants in the blood make their way to the intended body cells.
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0910 Sf Master Bloque1
- 1. ASSIGNATURA 564520: Medicaments i nutrició / Drugs & nutrition Medicinal Chemistry (20h) Synthetic drugs (10h)-Part 1 MASTER ON DRUGS, COSMETICS AND FOOD QUALITY Dr. Antonio Delgado Universitat de Barcelona October 2009
- 3. Introduction to drug synthesis: Design and strategies
- 4. Drugs “ Chemical compounds of known structure used for therapeutic or diagnostic purposes” Also commonly used for abused substances. Synonymous with medicine, pharmaceutical Obtained by application of the principles and tactics of Organic Synthesis Most of the drugs are synthetic organic compounds (carbon skeleton)
- 8. About synthetic sequences Linear vs convergent synthesis Linear synthesis Convergent synthesis
- 9. Construction of the carbon skeleton Retrosynthetic analysis
- 10. Construction of the carbon skeleton Retrosynthetic analysis: Strategic disconnections and synthon generation Reagent Real species Synthon ( “virtual”) Ionic or radical fragment arising from a disconnection
- 11. Equivalence between synthons and reagents
- 12. Reagents Different disconnection approaches are possible for a single synthetic operation Synthons
- 13. Guidelines for choosing a disconnection
- 14. Guidelines for choosing a disconnection
- 15. Guidelines for choosing a disconnection
- 16. Transformación de grupos funcionales Quimioselectividad Una reacción quimioselectiva diferencia entre grupos funcionales identicos o de reactividad muy parecida 3
- 17. Reacción no quimioselectiva
- 18. Guidelines for choosing a disconnection Two functional groups are involved in the same disconnection Example of a 1,2-disconnection 4
- 19. Guidelines for choosing a disconnection Example of a 1,3-disconnection
- 20. Guidelines for choosing a disconnection Other 1,3-disconnections
- 21. Guidelines for choosing a disconnection 1,4-disconnections
- 22. Construcción del esqueleto carbonado Control de la regioselectividad Eligiendo los reactivos adecuados se puede preparar el regioisómero que interesa REGIOISÓMEROS Compuestos que difieren en la disposición de los sustituyentes
- 23. Chirons contain chiral information of the target compound Construction of the carbon skeleton Retrosynthetic analysis: Chiron: the chiral version of a synthon
- 24. Algo del chiral pool: concepto y ejemplos El “chiral pool”
- 25. El “chiral pool”
- 26. El “chiral pool”
- 29. Reduction of carbonyl derivatives
- 30. The versatility of acyl chlorides
- 33. Protecting groups in peptide synthesis Directionality in peptide bond formation
- 34. Protecting groups in peptide synthesis Reactivity control
- 35. Carbamates: amine protecting groups in peptide synthesis
- 36. Other amine protecting groups
- 37. Carboxylic acid protecting groups
- 41. Control de los centro s estereogénico s Reacción estereoselectiva : Se forma mayoritariamente un estereoisómero. Según la naturaleza del diastereómero que se forme, la reacción será diastereoselectiva o enantioselectiva diastereoselectiva enantioselectiva
- 43. Examples of stereospecific reactions S N 2 and E 2 reactions
- 44. Examples of stereospecific reactions Alkene halogenation Alkene epoxidation
- 45. Stereoselective reactions can be diastereoselective or enantioselective Diastereoselective: one diastereoisomer predominates Enantioselective: one enantiomer predominates diastereoselective enantioselective
- 46. A model to predict the diastereoselectivity in carbonyl additions: The Felkin-Ahn model
- 48. Diastereoselective synthesis Preferred hydride attack
- 49. Diastereoselective synthesis Microorganisms as chiral reagents: double diastereoselection