- PEGYLATION PROCESS
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The present invention relates to the attachment of a polyethylene glycol (PEG) moiety to a target substrate. Processes for such attachment will be hereinafter referred to as "PEGylation" of the substrate. In particular, the present invention relates to a process for direct covalent PEGylation of a substrate, comprising the reaction of a halogenated PEG with the substrate wherein the halogen of the halogenated PEG acts as a leaving group in the PEGylation reaction.
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- Studies on Synthesis and Anticancer Activity of Selected N-(2-Fluoroethyl)-N-nitrosoureas
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An activated carbamate, 2-nitrophenyl (2-fluoroethyl)nitrosocarbamate (3), was used to advantage in the synthesis of the water-soluble (2-fluoroethyl)nitrosoureas 6a-d from 2-aminoethanol, (1α,2β,3α)-2-amino-1,3-cyclohexanediol, cis-2-hydroxycyclohexanol, and 2-amino-2-deoxy-D-glucose.In a variation of this method, 2,4,5-trichlorophenyl (2-fluoroethyl)carbamate (4) was used to prepare the urea from which the essentially water-insoluble N'-(2,6-dioxo-3-piperidinyl)-N-(2-fluoroethyl)-N-nitrosourea (6e) was derived.The anticancer activity of these nitrosoureas was determined against the murine tumors B16 melanoma and Lewis lung carcinoma and found to be significant and comparable to their chloroethyl counterparts.On the basis of results from both systems, the dihydroxycyclohexyl derivative 6b may be the most effective.
- Johnston, Thomas P.,Kussner, Conrad L.,Carter, Ronald L.,Frye, Jerry L.,Lomax, Nancita R.,et al.
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p. 1422 - 1426
(2007/10/02)
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