Protection for the AMINE.pptx
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The document discusses various protecting groups used for amino groups in organic synthesis. It describes qualities of a good protecting group and highlights common protecting groups for amines like carbamates, amides, and cyclic imides. Specific protecting groups covered in detail include t-butyl carbamate, 9-fluorenylmethyloxycarbonyl, benzyloxycarbonyl, formamide, and phthalimide. The document concludes by providing examples of applications of protecting groups in peptide synthesis and synthesis of drugs.
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Protection for amino group and amino acid
The document discusses protecting groups in organic synthesis. It provides characteristics that a good protecting group should have such as being selectively introduced and removed in good yields without affecting other functional groups. Common protecting groups for amino groups are discussed, including carbamates like Boc and Cbz which are installed under mild conditions and removed under acidic or basic conditions. Other protecting groups for amines mentioned are amides, formamides, acetamides, and sulfonamides which are stable but removed under strong acidic or basic conditions. The document provides examples of protecting group introduction and removal in peptide and amine synthesis.
AMINO ACID & PEPTIDES
This power point contain introduction, all synthesisStrecker synthesis
(Amido-malonate
Reductive amination of alpha keto acids) (Solid phase (Merrifield)
Solution phase) of amino and and peptides.
Protection for the carbonyl group ^0carboxyl group.pptx
This document discusses protecting groups for carbonyl and carboxylic acid functional groups. It describes common protecting groups like esters, amides, and tert-butoxycarbonyl that protect carboxylic acids from reacting under reaction conditions. For carbonyl protection, it discusses acetals, ketals, dithioacetals, and hemiacetals/thioacetals that prevent reactions at the carbonyl carbon. The key qualities of protecting groups and mechanisms of introduction and removal are provided for different protecting groups to selectively modify functional groups in multifunctional molecules.
protecting groups
This document discusses protecting groups used in organic synthesis. Protecting groups are introduced to block the reactivity of functional groups during multi-step synthesis. Common protecting groups discussed include silyl, acetal, and ester protecting groups for alcohols, ketals and acetals for aldehydes and ketones, esters for carboxylic acids, and carbamates for amino groups. The qualities of good protecting groups and their selective introduction and removal are explained.
PROTECTINGANDBDEPROTECTING GROUPS IN ORGANIC SYNTHESIS [M.PHARM]
Protecting groups are introduced onto reactive functional groups in organic molecules to block their reactivity during multi-step syntheses. Good protecting groups are readily introduced and removed selectively while keeping the protected group stable during other reactions. Common protecting groups discussed include silyl, acetal, ketal, ester, and carbamate groups for alcohols, aldehydes, ketones, carboxylic acids, and amines respectively. Protecting group selection and applications provide selective reactivity needed for complex molecule synthesis.
Protection for carboxylic group & Protection for the Amino group
Protection for carboxylic group & Protection for the Amino groupCollege of Pharmacy,Sri Ramakrishna Institute of Paramedical Sciences,Coimbatore
Protecting groups are introduced to temporarily block reactive sites on molecules to allow for selective reactivity in multi-step organic syntheses. Common protecting groups include esters for carboxylic acids (e.g. methyl esters), acetals for carbonyls, and alkyl/acyl/sulfonyl groups for amines. Protecting groups must be stable but also removable, without affecting other functionality. For example, a ketone might be protected as an acetal to allow for reduction of an ester without reducing the ketone as well.Protecting groups
This document discusses the use of protecting groups in organic synthesis. It provides examples of common protecting groups for alcohols, including trialkylsilyl ethers, benzyl ethers, and acetate esters. Methods for introducing and removing these protecting groups are described. The document also discusses protecting groups for amines, such as Boc and phthaloyl, along with their introduction and removal conditions. Finally, examples of acetal and ketal protecting groups for carbonyl compounds are briefly mentioned.
Sch 504 protecting_groups_in_organic_synthesis by pradeep kumar .M.SC,APSET,(...
Protecting groups are molecular frameworks that are introduced onto reactive functional groups in organic molecules to block their reactivity during chemical transformations of other parts of the molecule. The document discusses various commonly used protecting groups for alcohols, aldehydes/ketones, carboxylic acids, and amines. Protecting groups must be stable under reaction conditions but also removable under mild conditions when no longer needed. Examples of protecting groups discussed include tert-butyldimethylsilyl ethers, acetals, esters like methyl and benzyl esters, and carbamates like tert-butyloxycarbonyl and benzyloxycarbonyl.
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Protection for amino group and amino acid
The document discusses protecting groups in organic synthesis. It provides characteristics that a good protecting group should have such as being selectively introduced and removed in good yields without affecting other functional groups. Common protecting groups for amino groups are discussed, including carbamates like Boc and Cbz which are installed under mild conditions and removed under acidic or basic conditions. Other protecting groups for amines mentioned are amides, formamides, acetamides, and sulfonamides which are stable but removed under strong acidic or basic conditions. The document provides examples of protecting group introduction and removal in peptide and amine synthesis.
AMINO ACID & PEPTIDES
This power point contain introduction, all synthesisStrecker synthesis
(Amido-malonate
Reductive amination of alpha keto acids) (Solid phase (Merrifield)
Solution phase) of amino and and peptides.
Protection for the carbonyl group ^0carboxyl group.pptx
This document discusses protecting groups for carbonyl and carboxylic acid functional groups. It describes common protecting groups like esters, amides, and tert-butoxycarbonyl that protect carboxylic acids from reacting under reaction conditions. For carbonyl protection, it discusses acetals, ketals, dithioacetals, and hemiacetals/thioacetals that prevent reactions at the carbonyl carbon. The key qualities of protecting groups and mechanisms of introduction and removal are provided for different protecting groups to selectively modify functional groups in multifunctional molecules.
protecting groups
This document discusses protecting groups used in organic synthesis. Protecting groups are introduced to block the reactivity of functional groups during multi-step synthesis. Common protecting groups discussed include silyl, acetal, and ester protecting groups for alcohols, ketals and acetals for aldehydes and ketones, esters for carboxylic acids, and carbamates for amino groups. The qualities of good protecting groups and their selective introduction and removal are explained.
PROTECTINGANDBDEPROTECTING GROUPS IN ORGANIC SYNTHESIS [M.PHARM]
Protecting groups are introduced onto reactive functional groups in organic molecules to block their reactivity during multi-step syntheses. Good protecting groups are readily introduced and removed selectively while keeping the protected group stable during other reactions. Common protecting groups discussed include silyl, acetal, ketal, ester, and carbamate groups for alcohols, aldehydes, ketones, carboxylic acids, and amines respectively. Protecting group selection and applications provide selective reactivity needed for complex molecule synthesis.
Protection for carboxylic group & Protection for the Amino group
Protection for carboxylic group & Protection for the Amino groupCollege of Pharmacy,Sri Ramakrishna Institute of Paramedical Sciences,Coimbatore
Protecting groups are introduced to temporarily block reactive sites on molecules to allow for selective reactivity in multi-step organic syntheses. Common protecting groups include esters for carboxylic acids (e.g. methyl esters), acetals for carbonyls, and alkyl/acyl/sulfonyl groups for amines. Protecting groups must be stable but also removable, without affecting other functionality. For example, a ketone might be protected as an acetal to allow for reduction of an ester without reducing the ketone as well.Protecting groups
This document discusses the use of protecting groups in organic synthesis. It provides examples of common protecting groups for alcohols, including trialkylsilyl ethers, benzyl ethers, and acetate esters. Methods for introducing and removing these protecting groups are described. The document also discusses protecting groups for amines, such as Boc and phthaloyl, along with their introduction and removal conditions. Finally, examples of acetal and ketal protecting groups for carbonyl compounds are briefly mentioned.
Sch 504 protecting_groups_in_organic_synthesis by pradeep kumar .M.SC,APSET,(...
Protecting groups are molecular frameworks that are introduced onto reactive functional groups in organic molecules to block their reactivity during chemical transformations of other parts of the molecule. The document discusses various commonly used protecting groups for alcohols, aldehydes/ketones, carboxylic acids, and amines. Protecting groups must be stable under reaction conditions but also removable under mild conditions when no longer needed. Examples of protecting groups discussed include tert-butyldimethylsilyl ethers, acetals, esters like methyl and benzyl esters, and carbamates like tert-butyloxycarbonyl and benzyloxycarbonyl.
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Clarithromycin is a macrolide antibiotic and a CYP3A4 inhibitor.Target: Antibacterial; CYP3A4Clarithromycin is a macrolide antibiotic used to treat pharyngitis, tonsillitis, acute maxillary sinusitis, acute bacterial exacerbation of chronic bronchitis, pneumonia (especially atypical pneumonias associated with Chlamydophila pneumoniae), skin and skin structure infections. Clarithromycin prevents bacteria from growing by interfering with their protein synthesis. It binds to the subunit 50S
Chapter 6.ppt
The document discusses the structure and properties of amino acids. It notes that amino acids are the building blocks of proteins and contain both an amino group and a carboxyl group. There are 20 standard amino acids that are used in protein synthesis. Amino acids share a common core structure but differ in their variable side chains. They can be classified based on the polarity of their side chains and whether they are essential or non-essential to humans. The document also discusses the nomenclature and abbreviations of amino acids, as well as some specialized amino acids like selenocysteine.
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1) Sulphonamides - The minimum structural requirement is the sulphanilamide skeleton, with essential amino and sulphonyl groups. Activity decreases with substitutions on the benzene ring.
2) Penicillins - The β-lactam ring and thiazolidine ring are essential for activity. Modifications to the acylamino side chain can enhance stability, spectrum of activity, and resistance to β-lactamase.
3) Further sections will discuss the structure-activity relationships
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There are 20 standard amino acids that are involved in protein synthesis. Each amino acid contains a carboxyl group, amino group, hydrogen atom, and a unique side chain. They differ from each other based on their side chains. Amino acids are classified based on their chemical structure, polarity, nutritional requirements, and metabolic fate. They perform important functions as monomers of proteins and in various biochemical processes.
Proteins and-amino-acids 1
Proteins are polymers of amino acids and are essential to life. There are 20 standard amino acids that are incorporated into proteins during translation. Amino acids contain an amino group, a carboxyl group, and a side chain that determines their properties. They exist as zwitterions at physiological pH and can be classified based on structure, polarity, and metabolic fate. Essential amino acids cannot be synthesized in the body and must come from diet, while non-essential ones can be synthesized.
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Context. With a mass exceeding several 104 M⊙ and a rich and dense population of massive stars, supermassive young star clusters
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Protection for the AMINE.pptx
- 1. PROTECTION FOR THE AMINE GROUP PRESENTED BY- INDRAJIT SAMANTA M.PHARM ( PHARMACEUTICAL CHEMISTRY), 1ST SEM, 1ST YEAR DEPARTMENT OF PHARMACEUTICAL CHEMISTRY, SPER, JAMIA HAMDARD, NEW DELHI
- 2. CONTENTS INTRODUCTION Qualities of a Good Protecting Group Protecting Groups for Amino Groups Carbamates as Protecting Groups for Amines Amides as Protecting groups for Amines Cyclic Imides As Protecting Group REFERENCE:
- 3. INTRODUCTION CHEMO SELECTIVITY Which functional groups will react REGIO SELECTIVITY Where it will react
- 4. INTRODUCTION Which functional group reacts first 1. Reaction 2. Condition 3. reagents
- 5. INTRODUCTION WHAT IS A PROTECTING GROUP? A protecting group (PG) is a molecular framework that is introduced onto a specific functional group (FG) in a poly-functional molecule to block its reactivity under reaction conditions needed to make modifications elsewhere in the molecule. R-FG PG R-FG-PG Free functional group (reactive) MUSK FUNCTIONAL GROUP( Unreactive)
- 6. QUALITIES OF A GOOD PROTECTING GROUP IN ORGANIC SYNTHESIS (a) It should be readily, but selectively introduced to the desired functional group in a poly- functional molecule. (b) It should be stable / resistant to the reagents employed in subsequent reaction steps in which the group being masked (protected) is desired to remain deactivated (protected). (c) It should be capable of being selectively removed under mild conditions when its protection is no longer required TACTICAL CONSIDERATIONS Easy & efficient introduction stable throughout reaction, work up & purification efficient and selective removal under mild conditions should not create any stereo-genic centre
- 7. PROTECTING GROUPS FOR AMINO GROUPS The basic problem of peptide synthesis is one of protecting the amino group. In bringing about interaction between the carboxyl group of one amino acid and the amino group of a different amino acid, one must prevent interaction between the carboxyl group and the amino group of the same amino acid. In preparing glycyl alanine, for example, one must prevent the simultaneous formation of glycylglycine. Reaction can be forced to take place in the desired way by attaching to one amino acid a group that renders the NH, unreactive
- 8. PROTECTING GROUPS FOR AMINO GROUPS
- 9. PROTECTING GROUPS FOR AMINO GROUPS Carbamates as Protecting Groups for Amines: Formation:- CLEAVAGE:
- 10. CARBAMATES AS PROTECTING GROUPS FOR AMINES: t-Butyl carbamate (Boc group):- FORMATION: RR’NH + Me3COCOCl Base RR’NCOOCMe3 CLEAVAGE: RR’NCOOCMe3 3M HCl RR’NH
- 11. CARBAMATES AS PROTECTING GROUPS FOR AMINES: 9-Fluorenylmethyl carbamate (Fmoc or 9-fluorenylmethyloxycarbonyl): 9- Fluorenylmethyloxycarbonyl protection is used for an alcohol or amine and it is carried out with an Fmoc-X reagent (X-CI or Nj) in the presence of pyridine or NaHCO3 FORMATION: CLEAVAGE:
- 12. BENZYL CARBAMATE [BENZYLOXY-CARBONYL OR CBZ GROUP (RRNCOOCH2PH)]:- FORMATION: CLEAVAGES:
- 13. AMIDES AS PROTECTING GROUPS FOR AMINES:- Amides are readily prepared from an amine and an acid chloride or anhydride. These are relatively more stable compounds that, classically, are cleaved by heating in strongly acidic or basic solutions. FORMAMIDE: FORMATION: RR’NH + HCOOH DCC, Pyridine RR’NCHO CLEAVAGE:
- 14. AMIDES AMIDES Amide condensation of phenylacetic acid and benzylamine with various catalysts under sealed conditions FORMATION Direct amide condensation of various carboxylic acids and amines by 8a ( SiO2
- 15. CYCLIC IMIDES AS PROTECTING GROUP FOR PRIMARY AMINES:- Phthalimide:- FORMATION:
- 16. CYCLIC IMIDES AS PROTECTING GROUP FOR PRIMARY AMINES:- CLEAVAGE:
- 17. OTHER PROTECTION FOR AMINE
- 18. SYNTHETIC APPLICATIONS 1) synthesis of dipeptide (glycine alanyl )
- 19. APPLICATION: YU’s synthesis of Paroxetine:
- 20. SYNTHETIC APPLICATIONS Romero synthesis of HIV-I protease inhibitor:
- 21. SYNTHETIC APPLICATIONS Synthesis of beta- lactam in preparation of carpetimycin A:
- 22. SYNTHETIC APPLICATIONS SYNTHESIS OF BETA LACTUM ANTIBIOTIC:
- 23. SYNTHETIC APPLICATIONS SYNTHESIS OF 4- HYDROXYPHOSPHONINE :
- 24. SYNTHETIC APPLICATIONS SYNTHESIS OF AZASUGAR:
- 25. SYNTHETIC APPLICATIONS SYNTHESIS OF OTHER DURGS:
- 26. REFERENCES: Hanson, J.R.; Protecting Groups in Organic Synthesis; Sheffield Academic Press; pp 8-80. Morrison, R.T.; Boyd R.N.; Organic Chemistry; Prentice-Hall of India Private Limited; Sixth Edition- 2002; pp. 1147. 2,2,6,6-Tetramethylpiperidin-1-yloxycarbonyl: A Protecting Group for Primary, Secondary, and Heterocyclic Amines, Joseph R. Lizza, Maximilian Bremerich, Stephanie R. McCabe, Peter Wipf, Org. Lett. 2018. https://doi.org/10.1021/acs.orglett.8b02874