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Tetrahydropyranyl (THP) is an excellent protective group for hydroxy and thiol moieties but rarely used in solid-phase peptide synthesis (SPPS). Discover its advantages, e.g., over O/S t Bu and Trt.
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Collect information about the most common side reactions during Fmoc SPPS and how to avoid them! Choose your building blocks and conditions wisely to avoid unnecessary trouble!
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Mix & Match. Discover typically employed protecting groups used to temporarily mask reactive functional moieties during solid-phase peptide synthesis to prevent undesired side-reactions.
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Wondering about the difference between Boc and Fmoc chemistry in solid phase peptide synthesis? Don't worry: in this short overview we will guide you through the basics of both strategies.
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Use the possibilities of Linkerology® to boost the efficacy of your drug! We illustrate how the drug Gepirone (Exxua TM ), a medication to treat major depressive disorders, can be conjugated.
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You are looking for a building block suitable to control the folding characteristics of your peptide or want to add a pH-sensitive conformational switch? Discover aminoprolines and their properties!
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REACH regulation for the handling of N , N -dimethylformamide (DMF), the most commonly used solvent for solid-phase peptide synthesis (SPPS). Read more about consequences and alternatives!
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Discover possibilities to fight chronic pain diseases by employing linker technologies. Check out the options for multiple drug conjugation in combination with different release mechanisms.
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You want to attach your small molecule to a certain carrier? Let’s analyze the functional groups present and discuss Linkerology® possibilities for permanent or trigger-inducible, tracelessly-cleavable linkage.
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You want to get an overview about the various resins available at Iris Biotech as well as their specifications, differences, and applications? Read on for further information and details.
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The Dawson Linker and its variants provide access to C-terminal peptide thioesters which are crucial components of Native Chemical Ligation reactions. Read on to discover all derivatives available at Iris Biotech!
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Interested in the introduction of Sarcosine (N-methylglycine), e.g. for hydrophilicity increase of your derivative of choice or for PEG replacement? Check-out our available Sarcosine building blocks!
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Herein, we present building blocks for the synthesis of protected hydroxylamine derivatives which can be further used for bio-conjugation and various other applications. Read on to find out more!
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Frustrated by aspartimide formation during peptide synthesis? Iris Biotech presents aspartate derivatives with bulky side chain protecting groups that minimize the formation of aspartimide-related side-products.
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The new disulfide-based protecting group sec-isoamyl mercaptan (SIT) is fully compatible with Fmoc- and Boc-SPPS and can easily be removed reductively upon addition of dithiothreitol.
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Interested in the formation of peptide thioesters for Native Chemical Ligation? Read on to find out more about the use of Dawson Linker derivatives as thioester surrogates compatible with Fmoc SPPS.
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Iris Biotech presents the next-generation of hydrolysis-stable phosphono-analogs of pSer, pThr and pTyr. Fluorination renders the phosphonic acid more acidic and thus an even better mimic of the parent phosphoamino acid.
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The presence of phenyl groups in APIs is connected with various disadvantages. An increasingly popular solution is the use of BCP as a phenyl ring bioisostere. Find out more about this highly diversifiable motif.
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Phosphorylation of serine, threonine and tyrosine is counted among the most important posttranslational modifications that occur in organisms.
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The azido group can be reduced to an amino function and hereby serve as masked amino group. It is of particular use if additional orthogonalities are needed. Azido is stable towards treatment with piperidine (Fmoc deprotection), Pd(0) (Alloc removal) and acidic treatmet (cleavage of Mtt, Trt or other acid sensitive groups). However, as it is a pseudohalogenide, care has to be taken during coupling steps, as HATU will cause high racemization. This can be avoided using collidine or other non-nucleophilic bas...
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α-Methyl and alkyl-amino acids can be produced by a number of platforms, where the (2S,4S)-4-methyl-2-phenyloxazolidin-5-one scaffold is one of the most popular one.
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Amino protected amino-PEG-acids can be used for the PEGylation of solid particles in order to create hydrophilic and reactive surfaces with no non-specific binding issues.
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Benzotriazol activated carboxylic acids:
Fast reaction (within minutes) at room temperature with amines and other nucleophiles under addition of base (in both water and non- aqueous solvents).
Stable to racemization when coupling with nucleophiles.
High solubility in organic solvents like DMF and DCM.
Stable in water.
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Phthalimidooxy PEG-based cross linkers form stable oximes with aldehydes, also latent ones as present in carbohydrates. Their reactivity is sufficiently mild for a broad used in creating conjugates with sensitive biologics.
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Building Blocks for the synthesis of 2,3-diaminobutanoic acid containing peptides or for Click reactions.
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Spermines and other Biogenic Polyamines interact due to their multi cationic structure with DNA!
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Reported applications:
Introduction of 9-fluorenylmethyloxycarbonyl, trichloroethoxycarbonyl, and benzyloxycarbonyl amine protecting groups into O-unprotected hydroxylamino acids using succinimidyl carbonates; Anelka Paquet; Can. J. Chem. ; 1982; 60: 976.
Widely Applicable Deprotection Method of 2,2,2-Trichloroethoxycarbonyl (Troc) Group Using Tetrabutylammonium Fluoride; Cheng-yuan Huanga; Ning Wanga; Katsumasa Fujikia; Yuji Otsukaa; Masao Akamatsua; Yukari Fujimotoa; Koichi Fukasea; Journal o...
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Abstract: N alpha-9-Fluorenylmethoxycarbonyl-N epsilon-4=methyltrityl-lysine, [Fmoc-Lys(Mtt)-OH], was prepared in two steps from lysine, in 42% overall yield.
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