- Synthesis and chemical constitution of diphenoxyphosphoryl derivatives and phosphonium salts as coupling reagents for peptide segment condensation
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The reactions of diphenoxyphosphoryl chloride ((PhO)2P(O)Cl) and different chlorophosphonium salts ([R3PCl]X, R = (CH3)2N, pyrrolidine, X = PF6-, BF4-), respectively, with 7-aza-1-hydroxybenzotriazole (HOAt), 1-hydroxybenzotriazole (HOBt), hydroximinomalonitrile (HOxDCO), and ethyl hydroximinocyanoacetate (HOxO) are described. The structures of the new compounds, which are useful coupling reagents for epimerization-free peptide segment condensation, are discussed on the basis of their 1H, 13C, 31P NMR, and IR spectra. The reactions of (PhO)2P(O)Cl lead to mixtures of O- and N-phosphorylated isomers of varying ratios. Contrary, reactions of chlorophosphonium salts yield exclusively one isomer.
- Hoffmann, Frank,Jaeger, Lothar,Griehl, Carola
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- PyBOP: A NEW PEPTIDE COUPLING REAGENT DEVOID OF TOXIC BY-PRODUCT
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PyBOP (benzotriazolyloxy-tris-phosphonium hexafluorophosphate), an analog of BOP where dimethylamino groups are replaced with pyrrolidino, is the only analog exhibiting equivalent properties in peptide bond formation.It can be used instead of BOP for the sake of safety.
- Coste, J.,Le-Nguyen, D.,Castro, B.
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- Pyrazinone thrombin inhibitors
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein A is
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- Novel spiro compounds
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Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.
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