540-51-2Relevant articles and documents
A practical synthesis of 3-butyn-1-ol
Yu, Xiao-Chun,Gu, Haining,Xu, Wei-Ming
, p. 467 - 469 (2006)
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Molecular Gating of an Engineered Enzyme Captured in Real Time
Kokkonen, Piia,Sykora, Jan,Prokop, Zbynek,Ghose, Avisek,Bednar, David,Amaro, Mariana,Beerens, Koen,Bidmanova, Sarka,Slanska, Michaela,Brezovsky, Jan,Damborsky, Jiri,Hof, Martin
, p. 17999 - 18008 (2018)
Enzyme engineering tends to focus on the design of active sites for the chemical steps, while the physical steps of the catalytic cycle are often overlooked. Tight binding of a substrate in an active site is beneficial for the chemical steps, whereas good accessibility benefits substrate binding and product release. Many enzymes control the accessibility of their active sites by molecular gates. Here we analyzed the dynamics of a molecular gate artificially introduced into an access tunnel of the most efficient haloalkane dehalogenase using pre-steady-state kinetics, single-molecule fluorescence spectroscopy, and molecular dynamics. Photoinduced electron-transfer-fluorescence correlation spectroscopy (PET-FCS) has enabled real-time observation of molecular gating at the single-molecule level with rate constants (kon = 1822 s-1, koff = 60 s-1) corresponding well with those from the pre-steady-state kinetics (k-1 = 1100 s-1, k1 = 20 s-1). The PET-FCS technique is used here to study the conformational dynamics in a soluble enzyme, thus demonstrating an additional application for this method. Engineering dynamical molecular gates represents a widely applicable strategy for designing efficient biocatalysts.
Acid-Catalyzed Intramolecular Ring-Opening Reactions of Cyclopropanated Oxabenzonorbornadienes with Carboxylic Acid Nucleophiles
Carlson, Emily,Ho, Angel,Koh, Samuel,Macleod, Matthew P.,Pounder, Austin,Tam, William
, (2021/12/02)
The present work demonstrates the ability of carboxylic acid tethered cyclopropanated oxabenzonorbornadienes (CPOBDs) to undergo ring-opening reactions in mild acidic conditions. The optimized reaction conditions involve the use of pTsOH in DCE at 90 °C. Two regioisomers are formed but the reactions are highly regioselective towards type 3 ring-opened products. It was observed that substitution at the C5 and aryl positions of CPOBD significantly hinders the ring-opening reactions leading to decreased yields of ring-opened products, although high regioselectivity for the Type 3 ring-opened products is still maintained. Herein, the first examples of acid-catalyzed intramolecular ring-opening reactions of CPOBD with carboxylic acid nucleophiles are reported.
Synthetic method of furazolidone metabolite AOZ
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Paragraph 0028-0030, (2020/07/13)
The invention discloses a preparation method of 3-amino-2-oxazolidinone (AOZ). The method comprises the following steps: 1) carrying out a reaction on ethylene glycol and PBr3 to obtain 2-bromoethanol; 2) in the presence of an alkali, carrying out a reaction on NH2NH2Boc and 2-bromoethanol to obtain Boc protected 2-hydrazinoethanol; 3) in the presence of an alkali, carrying out a reaction on Boc protected 2-hydrazinoethanol and diethyl carbonate to obtain Boc protected 3-amino-2-oxazolidinone; and 4) performing deprotection on the Boc group in the Boc protected 3-amino-2-oxazolidinone to obtain 3-amino-2-oxazolidinone. According to the method, the yield of AOZ in the synthesis process is obviously increased, and separation and purification are facilitated.