- Preparation method of N - 9 - fluorenylmethoxycarbonyl - N ' - trityl - L - histidine
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The invention relates to the technical field of medical intermediate synthesis, in particular to a synthetic method of N - 9 - fluorenylmethoxycarbonyl - N ' - trityl - L - histidine, which comprises the following steps: taking L - histidine as a raw material and protecting a - amino groups on histidine by using a silane protective agent. A silane protecting substance Nim - trityl histidine is obtained by reaction with triphenylchloromethane, followed by addition of water to the silane protecting group. The silane protecting substance Nim - trityl histidine is reacted with 9 - fluorenylmethoxycarbonyl protecting reagent to give the target product N - 9 - fluorenylmethoxycarbonyl - N ' - trityl - L - histidine. The N - 9 -fluorenylmethoxycarbonyl - N ' - trityl - L - histidine preparation method provided by the invention is simple and convenient to operate, high in yield and low in comprehensive production cost, and is suitable for industrial large-scale production.
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Paragraph 0012; 0028; 0030-0032; 0034-0035
(2021/09/21)
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- DIPHENYLMETHANE COMPOUND
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Compounds having a diphenylmethane skeleton are superior in broad utility and stability, and are useful as a protecting reagent (anchor) of amino acid and/or peptide in the liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide(-CONHR)-type, and in organic synthetic reaction methods (particularly peptide liquid phase synthetic methods), and may be contained in a kit for peptide liquid phase synthesis.
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- Efficient procedure for the preparation of oligomer-free N-fmoc amino acids
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A two-step method is presented for the peptide-free, high-purity, and high-yield synthesis of N-Fmoc amino acids. The first step involves the preparation of stable dicyclohexylammonium-amino acid ionic adduct in acetone. Subsequently, the ionic adducts, on reaction with Fmoc-Nosu under mild alkaline conditions, give dipeptide-free N-Fmoc amino acids. The positive charge of the dicyclohexylammonium counterion in the ionic salt has a longer radius, moderating the nucleophilicity of the carboxylate ion of the amino acid and preventing by-products by arresting the formation of mixed anhydrides, the precursors of oligopeptide impurities.
- Nowshuddin, Shaik,Rao,Reddy, A. Ram
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experimental part
p. 2022 - 2031
(2009/11/30)
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- GLP-2 compounds, formulations, and uses thereof
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The present invention relates to novel human glucagon-like peptide-2 (GLP-2) peptides and human glucagon-like peptide-2 derivatives which have a protracted profile of action as well as polynucleotide constructs encoding such peptides, vectors and host cells comprising and expressing the polynucleotide, pharmaceutical compositions, uses and methods of treatment.
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- Application of the Trt and Fmoc Groups for the Protection of Polyfunctional α-Amino Acids
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Simple methods for the preparation of ditrityl amino acids 3 and their application for the synthesis of the peptides 9-27 are described.Selective detritylation of 3 and of the synthesized ditrityl peptides is achieved with 1percent trifluoroacetic acid in dichloromethane.The resulting Nα-detritylated amino acids 5 were converted into the corresponding fluorenylmethoxycarbonyl amino acids 6 under Schotten-Baumann conditions using fluorenylmethyl chloroformate.
- Barlos, Kleomenis,Mamos, Petros,Papaioannou, Dionysios,Patrianakou, Stella,Sanida, Chariklia,Schaefer, Wolfram
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p. 1025 - 1030
(2007/10/02)
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