title: Synthesis of 1-aldofosfamide-perhydrothiazines.
abstract: Aldofosfamide-perhydrothiazine derivatives are a new class of prodrugs which spontaneously, with half-life times of 2 to > 12 h hydrolyse to the corresponding aldophosphamide in aquous solution. Synthesis of 1-aldofosfamide-perhydrothiazine (N,N'-(2-chloroethyl)-phosphorodiamide-2-(2'-[4'-carboxy-1',3'- perhydrothiazinyl])-ethylester) and a derivative, in which one 2-chlorethyl group of the alkylating function is substituted by a mesyl-ethyl-group (N-(2-Chloroethyl)-N'-(methanesulphonylethyl)- phosphorodiamide-2-(2'-[4'-carboxy-1',3'-perhydro-thiazinyl] )-ethylester), is described.
authors.affiliation: Johann Wolfgang Goethe-Universität, Universitätsklinikum, Frankfurt/Main, Germany.
authors.forename: J
authors.initials: J
authors.lastname: Zimmermann
authors.forename: H H
authors.initials: HH
authors.lastname: Bauer
authors.forename: H J
authors.initials: HJ
authors.lastname: Hohorst
authors.forename: G
authors.initials: G
authors.lastname: Voelcker
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D009682:Magnetic Resonance Spectroscopy; D010752:Phosphoramide Mustards / Q000138:chemical synthesis*; D011355:Prodrugs / Q000138:chemical synthesis*; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization; D013843:Thiazines / Q000138:chemical synthesis*
chemical_list: D000970:Antineoplastic Agents; D010752:Phosphoramide Mustards; D011355:Prodrugs; D013843:Thiazines