We have explored a method to convert a muraymycin biosynthetic intermediate 3 to an anticancer drug lead 2 for in vivo and thorough preclinical studies. Cu(OAc) forms a stable complex with the amide 4 and prevents electrophilic reactions at the 2-((3-aminopropyl)amino)acetamide moiety. Under the present conditions, the desired 5″-primary amine was selectively protected with (Boc)O to yield 6. The intermediate 6 was converted to 2 in two steps with 90% yield.
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| http://dx.doi.org/10.1021/acs.orglett.8b03716 | DOI Listing |
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