1234372-12-3Relevant articles and documents
Synthesis of enantiopure 1,2-azido and 1,2-amino alcohols via regio- and stereoselective ring-opening of enantiopure epoxides by sodium azide in hot water
Wang, Hai-Yang,Huang, Kun,De Jesús, Melvin,Espinosa, Sandraliz,Pi?ero-Santiago, Luis E.,Barnes, Charles L.,Ortiz-Marciales, Margarita
, p. 91 - 100 (2016/02/09)
A practical and convenient method for the efficient and regio- and stereoselective ring-opening of enantiopure monosubstituted epoxides by sodium azide under hydrolytic conditions is reported. The ring-opening of enantiopure styryl and pyridyl (S)-epoxides by N3- in hot water takes place preferentially at the internal position with complete inversion of configuration to produce (R)-2-azido ethanols with up to 99% enantio- and regioselectivity, while the (S)-adamantyl oxirane provides mainly the (S)-1-adamantyl-2-azido ethanol in excellent yield. In general, 1,2-amino ethanols were obtained in high yield and excellent enantiopurity by the reduction of the chiral 1,2-azido ethanols with PPh3 in water/THF, and then converted into the Boc or acetamide derivatives.
A preparation method of the compound hydroxy bromine
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Paragraph 0031; 0087-0089, (2018/02/04)
The present invention discloses a hydroxyl bromine compound preparation method comprising the following steps: in the presence of a catalyst, a compound shown as the formula I and N-brombenzamide are reacted in a liquid mixture of an organic solvent and water to obtain a compound shown as the formula II, wherein R1 are hydrogen or C1-C3 alkyl group; R2 are hydrogen or C1-C3 alkyl group; and R3 are hydrogen or C1-C4 alkyl group. A styrene type substrate and the N-brombenzamide are used as raw materials for effectively synthesizing a series of hydroxyl bromine compounds in the effect of (DHQD) 2PHAL. The raw materials are simple and easy to get, the nucleophile water is non-toxic and harmless, reaction conditions are mild, operation is simple, the method is atomic economic, enantiomer excess can reach up to 88%, the yield can reach up to 94%, the compounds has regioselectivity completely different from that of epoxy ring opening products, meanwhile the introduced C-Br bond and C-O bond both can be further transformed, and the method has great value.
Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors
Drai, Tonko,Molanov, Kreimir,Sachdev, Vinay,Malnar, Martina,Heimovi, Silva,Patankar, Jay V.,Obrowsky, Sascha,Levak-Frank, Sanja,Habu, Ivan,Kratky, Dagmar
, p. 722 - 734 (2014/12/12)
Two new trans-(3R,4R)-amino-β-lactam derivatives and their diastereoisomeric mixtures were synthesized as ezetimibe bioisosteres and tested in in vitro and in vivo experiments as novel β-lactam cholesterol absorption inhibitors. Both compounds exhibited l
