944088-87-3Relevant academic research and scientific papers
PROCESSES OF PREPARING ASYMMETRIC DINITROBENZAMIDE MUSTARD COMPOUNDS, INTERMEDIATE COMPOUNDS USEFUL THEREIN AND PRODUCTS OBTAINED THEREFROM
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Page/Page column 19; 22; 29, (2008/06/13)
The invention relates to methods of preparing compounds of formula (II) wherein Z represents -OR1 or -N(R2)R2a-, where R1 is lower alkylene (C1-C6), R2 is lower alkyl or H and R
Synthesis of asymmetric halomesylate mustards with aziridineethanol/alkali metal halides: application to an improved synthesis of the hypoxia prodrug PR-104
Yang, Shangjin,Atwell, Graham J.,Denny, William A.
, p. 5470 - 5476 (2008/01/07)
Aromatic asymmetric halomesylate mustards are efficiently prepared by reaction of activated aromatic chlorides with aziridineethanol/alkali metal halides, followed by mesylation of the haloalcohol. The reaction conditions are sufficiently mild to be compatible with a range of different substituents and protecting groups, including carboxylate and phosphate esters, and have been used in an improved synthesis of the anticancer bromomesylate mustard PR-104, now in clinical trials.
