- 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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p. 299 - 309
(2007/10/03)
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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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