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Nucleophilic ring-opening in a carbohydrate nitrocyclopropane: A stereospecific approach to chiral isoalkyl structures

✍ Scribed by Hans H. Baer; Ursula Williams; Bruno Radatus


Publisher
Elsevier Science
Year
1988
Tongue
English
Weight
917 KB
Volume
174
Category
Article
ISSN
0008-6215

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✦ Synopsis


Chemical reactions to open the cyclopropane ring in (1R)-1,2-dideoxy-3,4:5,6-di-O-isopropylidene-1,2-C-methylene-1-nitro-D-m annitol (1) were investigated. Catalytic hydrogenation over Pd-C produced the corresponding 1-amino compound, isolated as its N-acetyl derivative, but failed to cleave the ring. However, ring opening succeeded by nucleophilic addition of sodium thiophenoxide to 1, giving 1,2-dideoxy-3,4:5,6-di-O-isopropylidene-1-nitro-2-C- (phenylthio)methyl-D-mannitol. The latter reacted further with thiophenoxide to furnish phenyl 2-deoxy-3,4:5,6-di-O-isopropylidene-2-C-(phenylthio)methyl-D- mannothiohydroximate. Raney nickel converted both of these thio sugar derivatives into the same product, namely, 1-acetamido-1,2-dideoxy-3,4:5,6-di-O-isopropylidene-2-C-methyl-D-mannito l. The use of these transformations for the design of stereospecific syntheses of chiral isoalkyl structures is proposed.