Aryloxymethylcarbonochloridate ester intermediates for use in synthesizing pro drugs and their use therefor

作者: Frantz J. Lund

DOI:

关键词: StereochemistryRing (chemistry)AlkylProdrugArylHydrogenOxygenGroup (periodic table)SubstituentChemistry

摘要: The present invention relates to hitherto unknown intermediate of formula, in which R 1 stands for hydrogen or a straight branched aliphatic C -C 20 carbon chain an aryl aralkyl group, and "ar" meaning aromatic heterocyclic, 5- 6-membered ring substituent containing 2 hetero atoms selected among O, S N, optionally being further substituted, its interrupted by like oxygen, carbonyl group(s); 3 alkyl. intermediates can be used one step method producing prodrugs where D-H =drug itself.

参考文章(8)
Walter-Wielant Wiersdorff, Rolf Kretzschmar, Harald Weifenbach, Karl-Heinz Geiss, Wolfgang Worstmann, Dieter Lenke, Novel carbamates, their preparation, and pharmaceutical formulations containing these compounds ,(1980)
John David Nordstrom, Novel monomers and polymers ,(1966)
Louis A. Carpino, Michael Philbin, Reagents for rapid peptide synthesis ,(1990)
Jose Alexander, Robyn Cargill, Stuart R. Michelson, Harvey Schwam, (Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes Journal of Medicinal Chemistry. ,vol. 31, pp. 318- 322 ,(1988) , 10.1021/JM00397A008
Stewart Fh, Formation of depsipeptide ester bonds by accelerated active ester coupling. Chemistry & Industry. ,vol. 46, pp. 1960- 1961 ,(1967)
Patrice Marie-Joseph Le Roy, Jean-Pierre Georges Senet, Allyl-acrylic monomers, their preparation and polymers derived therefrom ,(1977)