- Synthesis and evaluation of biological activities of aziridine derivatives of urea and thiourea
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In the present paper, we report the synthesis and evaluation of in vitro antimicrobial activities of aziridine-thiourea derivatives. A series of aziridines in reaction with isocyanates and isothiocyanates to obtain urea and thiourea derivatives were used.
- Kowalczyk, Aleksandra,Pieczonka, Adam M.,Rachwalski, Micha?,Lésniak, Stanis?aw,Staczek, Pawe?
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- A new route towards N-(α-methoxybenzyl)aziridines
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A new synthesis of N-(α-methoxyarylmethyl)-2,2-dimethylaziridines is presented. Different benzaldehydes were converted into the corresponding imines upon reaction with 2-bromo-2-methylpropylamine. Treatment of the latter imines with sodium methoxide affor
- D'hooghe, Matthias,Hofkens, Arn,De Kimpe, Norbert
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- Efficient Direct Synthesis of Aziridine-Containing Chiral Tridentate Ligands by the Iminium-Mediated Self-Ring Opening Reaction of Enantiopure Aziridines and Salicylaldehydes
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An efficient method for the direct synthesis of aziridine-containing chiral tridentate ligands was developed from enantiopure aziridines and salicylaldehydes. The method achieved the regiospecific cleavage of more substituted C?N bonds of aziridines through an iminium-mediated self-ring opening reaction of aziridines with up to 95% yield and complete inversion of configuration. The (S)-2-alkylaziridine-derived tridentate ligands displayed excellent activity and stereoselectivity in the zinc trifluoromethanesulfonate-catalyzed asymmetric aldol reactions of acetone and aromatic aldehydes. (Figure presented.).
- Chen, Xingpeng,Lin, Chao,Du, Hongguang,Xu, Jiaxi
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p. 1647 - 1661
(2019/02/27)
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- Ti-Catalyzed Radical Alkylation of Secondary and Tertiary Alkyl Chlorides Using Michael Acceptors
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Alkyl chlorides are common functional groups in synthetic organic chemistry. However, the engagement of unactivated alkyl chlorides, especially tertiary alkyl chlorides, in transition-metal-catalyzed C-C bond formation remains challenging. Herein, we describe the development of a TiIII-catalyzed radical addition of 2° and 3° alkyl chlorides to electron-deficient alkenes. Mechanistic data are consistent with inner-sphere activation of the C-Cl bond featuring TiIII-mediated Cl atom abstraction. Evidence suggests that the active TiIII catalyst is generated from the TiIV precursor in a Lewis-acid-assisted electron transfer process.
- Wu, Xiangyu,Hao, Wei,Ye, Ke-Yin,Jiang, Binyang,Pombar, Gisselle,Song, Zhidong,Lin, Song
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supporting information
p. 14836 - 14843
(2018/11/10)
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- An improved and mild wenker synthesis of aziridines
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The conventional Wenker synthesis of aziridines from vicinal amino alcohols has been modified by employing mild reaction conditions. Amino alcohols were converted into their hydrogen sulfates with chlorosulfonic acid. The sulfates were cyclized with sodium hydroxide, and even with non-nucleophilic sodium carbonate. The current, improved method extends the scope of the typical Wenker synthesis and is applicable to unstable amino alcohols in hot sulfuric acid and to unstable sulfates which favor elimination and hydroxide displacement in the presence of strong base. Georg Thieme Verlag Stuttgart.
- Li, Xinyao,Chen, Ning,Xu, Jiaxi
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experimental part
p. 3423 - 3428
(2010/11/21)
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- Substituted 3-aminosyndone imines, a process for their preparation and their use
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Substituted 3-aminosydnone imines of the formula I STR1 and their pharmacologically acceptable acid addition salts, in which A denotes, for example, --CH2 --, R1 denotes hydrogen or the radical --COR5, R2, R3 denote alkyl having 1 to 4 C atoms, R5 denotes, for example, an aliphatic radical having 1 to 4 C atoms, and methods for preparing such compounds by cyclization of a compound of the formula II STR2 and if desired subsequent acylation. The invention also includes formulations containing effective amounts of such compounds, and methods for administering same to patients for the control and prophylaxis of cardiovascular disorders.
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- Mercury-photosensitized decomposition of 2-azetidinone and 4,4-dimethyl-2-azetidinone
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The mercury-photosensitized decompositions of 2-azetidinone(AZ) and 4,4-dimethyl-2-azetidinone(DMAZ) have been studied at 453 and 423 K and at pressures from 750 to 18000 Pa and from 640 to 5000 Pa, respectively. The major products from AZ were carbon monoxide and ethylene, while ammonia was a minor product. The yields of carbon monoxide and ethylene increased linearly with increasing reaction time and light intensity; they were independent of the AZ pressure. These results suggest that carbon monoxide and ethylene are trie primary products. The major products from DMAZ were carbon monoxide, isobutene, and 2,2dimethylaziridine; ethane, isobutane, and propylene were the minor products. The yields of carbon monoxide, isobutene, and dimethylaziridine increased linearly with increasing reaction time and light intensity at 3800 Pa, showing that these products are the primary ones. The formation of minor products was not linear with time. The quantum yields of carbon monoxide and isobutene were independent of the DMAZ pressure, while the relative yield of dimethylaziridine to that of carbon monoxide increased and those of the minor products decreased with an increase in pressure. Plausible mechanisms were proposed.
- Yamamoto, Shunzo,Kanetsuki, Akihide,Sueishi, Yoshimi,Nishimura, Norio
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p. 2911 - 2915
(2007/10/02)
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- Reactions with Aziridines, 42. - The Regioselectivity of the Ring Opening of Activated 2,2-Dimethylaziridines by Carbanions of the β-Dicarbonyl Type. Influence of the Size of the Nucleophile
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The aziridine ring of the 1-acyl-2,2-dimethylaziridines 1a-c is cleaved abnormally (between N and CMe2) by the substituted ethyl cyanoacetates 3M, P (M = methyl, P = phenyl) in ethanolic ethoxide solution, while the ring is not cleaved by diethyl malonate
- Buchholz, Berthold,Stamm, Helmut
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p. 1239 - 1244
(2007/10/02)
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- Aziridino containing nitro imidazoles and pharmaceutical compositions
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A compound of formula I STR1 in which formula: R1 represents hydrogen or an alkyl group; R2 -R5 represent hydrogen, alkyl aryl, aralkyl or alkaryl group; and n is 1.
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