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US 5,329,048 AGranted
Process of preparing tetraamino intermediates
AssigneeThe DuPont Merck Pharmaceutical Company
InventorJung-Hui Sun
Life of this patent
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Abstract
This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methy1-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.
Claims1
A method for preparing a compound of the formula:
- ##STR11## said method comprising:
- (a) reacting t-BOC-alanine with 1,1' carbonyldiimidazole followed by reaction with ethylenediamine to yield a compound of the formula:
- ##STR12## (b) removing the t-BOC group of (I) with mineral acid followed by reduction of the dihydrochloride salt with diborane in refluxing tetrahydrofuran followed by neutralization of the acid salt with sodium ethoxide to yield a compound of the formula (IV).
Dependencies are inferred from the claim text.