- BIOREVERSABLE PROMOIETIES FOR NITROGEN-CONTAINING AND HYDROXYL-CONTAINING DRUGS
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Disclosed are promoieties of the following formula which can be used to form prodrugs of nitrogen-containing or hydroxyl-containing drug or a pharmaceutically active agent: (I) and pharmaceutical compositions comprising the prodrugs.
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Page/Page column 155; 156
(2015/06/18)
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- The comparison of protecting methods to the amino group in 2-Aminomethylphenylacetic acid
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2-Aminomethylphenylacetic acid is an important intermediate of ceforanide, and this article compared two different protecting agents for protecting the amino group in 2-aminomethylphenylacetic acid by BOC (Di-tert butyl dicarbonate) or acetacetic ester, a
- Zhao, Yougui,Wang, Ronggeng,Liu, Mei
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p. 1637 - 1640
(2014/05/06)
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- PEPTIDES AND PEPTIDOMIMETIC COMPOUNDS, THE MANUFACTURING THEREOF AS WELL AS THEIR USE FOR PREPARING A THERAPEUTICALLY AND/OR PREVENTIVELY ACTIVE PHARMACEUTICAL COMPOSITION
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Peptides, peptidomimetics and derivatives thereof of the general formula I: H2N-GHRPX1-β-X4X5X6X7X8X9X10-X11 (I), in which X1-X10 denote one of the 20 genetically coded amino acids, wherein X8, X9 and X10 may also denote a single chemical bond;X11 denotes OR1 in which R1 equals hydrogen or (C1-C10) alkyl NR2R3 with R2 and R3 are equal or different and denote hydrogen, (C1-C10) alkyl, or a residue —W-PEG5-60K, in which the PEG residue is attached via a suitable spacer W to the N-atom, ora residue NH—Y-Z-PEG5-60K, in whichY denotes a chemical bond or a genetically coded amino acids from the group S, C, K or R andZ denotes a spacer, via which a polyethylene glycol (PEG)-residue can be attached, and their physiologically acceptable salts, andβ denotes an amino acid, or a peptidomimetic element, which induces a bend or turn in the peptide backbone.
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- Preparation of amides from acids and resin bound azides: Suppression of intramolecular lactam formation
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A new method for the formation of amides on solid phase has been developed. The procedure involves the reaction between activated acids in solution and resin bound iminophosphoranes generated from the corresponding azides and tributylphosphine. The method is particularly attractive when starting from δ azido acids since amides can form without internal cyclization to the lactam.
- Tang, Zhilian,Pelletier, Jeffrey C.
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p. 4773 - 4776
(2007/10/03)
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