A convenient synthesis of chiral 1,2,4-oxadiazoles from N-protected (α-aminoacyl)benzotriazoles
نویسندگان
چکیده
منابع مشابه
One-pot synthesis of enantiomerically pure N-protected allylic amines from N-protected α-amino esters
An improved protocol for the synthesis of enantiomerically pure allylic amines is reported. N-Protected α-amino esters derived from natural amino acids were submitted to a one-pot tandem reduction-olefination process. The sequential reduction with DIBAL-H at -78 °C and subsequent in situ addition of organophosphorus reagents yielded the corresponding allylic amines without the need to isolate t...
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Some new macrocyclic dibenzotrioxadiamides, dibenzotetraoxadiamide, dibenzopentaoxadiamide, dibenzothiatrioxadiamide, tribenzotrioxadiamides and tetrabenzohexaoxadiamide (14-21), (26) and (27) have been prepared. These compounds were obtained in the macrocyclization step by reacting the diamine (4) with appropriak dicaxboxylic acid dichlorides (5-13) and (24). The cyclization does not requ...
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N, N΄-3, 4-di(methylamino)-1, 2, 5-oxadiazole (1f) was prepared by dehydration of N, N΄-3, 4-di(methylamino)glyoxime (2f) in aqueous potassium hydroxid at 170-180 ˚C. Under similar conditions N, N΄-3, 4-di(benzylamino)-1, 2, 5-oxadiazole (1c) and N, N΄-3, 4-di(isopropylamino)...
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Peptidomimetics based on hydrazino derivatives of α-amino acids represent an important class of peptidic foldamers with promising biological activities, like protease inhibition and antimicrobial activity. However, the lack of straightforward method for the synthesis of optically pure hydrazino acids and efficient incorporation of hydrazino building blocks into peptide sequence hamper wider exp...
متن کاملSynthesis of Chiral TFA-Protected α-Amino Aryl-Ketone Derivatives with Friedel-Crafts Acylation of α-Amino Acid N-Hydroxysuccinimide Ester.
Chiral N-protected α-amino aryl-ketones are one of the useful precursors used in the synthesis of various biologically active compounds and can be constructed via Friedel-Crafts acylation of N-protected α-amino acids. One of the drawbacks of this reaction is the utilization of toxic, corrosive and moisture-sensitive acylating reagents. In peptide construction via amide bond formation, N-hydroxy...
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ژورنال
عنوان ژورنال: Arkivoc
سال: 2005
ISSN: 1551-7012
DOI: 10.3998/ark.5550190.0006.705