- 2-ARYLMETHYLAZETIDINE CARBAPENEM DERIVATIVES AND PREPARATION THEREOF
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A 2-arylmethylazetidine carbapenem derivative of formula ( I ) or a pharmaceutically acceptable salt thereof exhibits a wide spectrum of antibacterial activities against Gram-positive and Gram-negative bacteria and excellent antibacterial activities against resistant bacteria such as methicillin-resistant Staphylococcus aureus (MRSA) and quinolone-resistant strains (QRS).
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Page/Page column 12
(2008/06/13)
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- New Synthesis of Propargylic Amines from 2-(Bromomethyl)aziridines. Intermediacy of 3-Bromoazetidinium Salts
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A new, efficient, and straightforward synthesis provides propargylamines in high overall yields (64-77%) by transformation of 1-(arylmethyl)-2-(bromomethyl)aziridines into N,N-di(arylmethyl)N-(2-propynyl)amines via N-(2,3-dibromopropyl)amines and N-(2-bromo-2-propenyl)amines. The conversion of N-(2,3-dibromopropyl)amines into N-(2-bromo-2-propenyl)amines is based on a novel analogue of the Hofmann elimination. A Yamaguchi-Hirao alkylation, a Sonogashira coupling, or a hydroarylation reaction further functionalized these propargylamines toward potentially interesting compounds for medicinal and agrochemical use.
- D'Hooghe, Matthias,Van Brabandt, Willem,De Kimpe, Norbert
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p. 2703 - 2710
(2007/10/03)
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- Novel Syntheses of 1,3,3-Trinitroazetidine
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Alternative methods for the synthesis of 1,3,3-trinitroazetidine (TNAZ) from epichlorohydrin, and benzhydrylamine have been developed.These approaches employ N-sulfonyl-3-(hydroxyimino)azetidines as penultimate intermediates and represent an improvement over previously published methods which require either diazo containing intermediates or involve low yielding procedures.Parallel methods employing N-benzhydryl- and N-benzyl-3-(hydroxyimino)azetidine were also investigated as alternate routes to TNAZ
- Katritzky, Alan R.,Cundy, Darren J.,Chen, Jie
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p. 271 - 276
(2007/10/02)
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- Preparation of 3-Azetidinols with Non-Bulky 1-Alkyl Substituents
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Cyclization of either the tetrahydropyranyl or trimethylsilyl ether of 1-(alkylamino)-3-chloro-2-propanols 1 followed by cleavage of the azetidinyl ether provides a general method for the preparation of 1-alkyl-3-azetidinols.Unhindered amines provide a more facile preparation of derivatives of 1, or its ethers, than do hindered amines, while hindered derivatives of 1 undergo more facile ring closure.
- Higgins, Robert H.,Eaton, Quentin L.,Worth, Leroy,Peterson, Myra V.
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p. 255 - 259
(2007/10/02)
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