(-)-6,6-乙二氧撑-1,10-二甲基-1(9)-八氢萘酮-2的合成

乙基乙烯基酮与4,4-乙二氧撑-2-甲基环乙酮2 c的手性亚胺进行不对称Michael加成,生成2,2-双取代环烷酮5,5经过克莱森缩合得到(-)-6,6-乙二氧撑-1,10-二甲基-1(9)-八氢萘酮-2(-)(1 c)。     

Michael addition of ethyl acrylate and acetone over solid bases

The catalytic behaviour of the superbases Na/NaOH/-Al₂O₃ and Cs_xO/-Al₂O₃ as well as of the basic zeolites Na/NaX and Cs_xO/CsX were investigated in the Michael addition of ethyl acrylate and acetone. The reactions were carried out in the liquid phase at catalyst loadings varying from 0.05 to 0.1 mol ester/g catalyst.     

MCM-41 Heterogenized Chiral Amines as Base Catalysts for Enantioselective Michael Reaction

Cinchonidine and cinchonine have been grafted onto pure silica MCM-41. It has been shown that both supported alkaloids are active catalysts for the Michael addition of ethyl 2-oxocyclopentanecarboxylate and methyl vinyl ketone, anchored cinchonidine being more active and enantioselective than anchored cinchonine. The study of the influence of the polarity of the solvent and reaction temperature on the optical induction shows that there is not a direct correlation between solvent polarity and enantioselectivity, and the maximum optical yield was obtained between 278 and 273 K.     

微波辅助合成1-(3-羟丙基)-4-哌啶酮

以3-羟基丙胺和丙烯酸甲酯为起始原料,在微波辅助下进行Michael加成、Dieckmann环合和脱羧反应合成了1-(3-羟丙基)-4-哌啶酮.并对Michael加成、Dieckmann环合和脱羧反应的工艺参数进行了优化,通过核磁共振波谱对目标化合物和中间体的结构进行表征.得到的最优Michael加成工艺条件为:n(3-羟基丙胺):n(丙烯酸甲酯)=1.0:2.4,微波辐射功率为120 W,反应温度40℃,反应时间30 min.在该条件下制备3-[(2-甲氧羰乙基)(3-羟丙基)氨基]丙酸甲酯的收率为92.6％;在微波辐射功率为200 W下,Dieckmann环合反应和脱羧反应分别为20和25 min,以88.5％的收率得到1-(3-羟丙基)-4-哌啶酮;目标产物总收率为82.0％.     

一类核苷类似物关键中间体的合成

对一类核苷类似物的关键中间体———(4R,5R) 4 (N 甲基羟氨基) 5 [(叔丁基二苯基硅烷基)氧甲基] 3,4 二氢 2(5H) 呋喃酮的合成进行了研究。以L 抗坏血酸为原料,经Pd/C催化加氢和缩酮保护,生成5,6 O 异亚丙基 L 古洛糖酸 1,4 内酯,产率74 3%。该内酯经NaIO4氧化、Wittig反应、水解成环和柱色谱分离,得(R) (+) 5 羟甲基 2 (5H) 呋喃酮,产率43 0%。最后该呋喃酮再经硅烷保护和羟胺Michael加成,即得到目标化合物。这7步反应的总产率27 9%。     

A new method for the synthesis of tetrahydrothiophene-S,S-dioxide derivatives: the Michael ring closure reaction between halomethyl (E)-β-styryl sulfones and CH-acids

Bromomethyl and chloromethyl (E)-β-styryl sulfones enter a Michael ring closure reaction with sodium enolates prepared from dimethyl malonate, malononitrile and ethyl acetoacetate. The condensation results in formation of substituted tetrahydrothiophene-S,S-dioxides. It is a new instance of α-haloalkyl sulfones transformations, which are not connected with Ramberg–Bäcklund reaction.     

No More Stopping

The dissolution of the conventional breaking points in the construction and completion phases of a building's delivery has blurred ‘the distinction between the production of design intent and the transmission of information’. Here Richard Garber , Director of the School of Architecture at the New Jersey Institute of Technology (NJIT), advocates that architects should use this as an opportunity to widen their remit, gaining agency and with it responsibility and the financial rewards to practice. Here he draws from the examples of UNStudio, GLUCK+ and his own New-York based practice, GRO Architects.     

El Sur Global: Future Resilient City

Shifting the focus from futuristic visions, Alfredo Brillembourg and Hubert Klumpner with Alexis Kalagas of interdisciplinary design practice Urban-Think Tank urge us to ‘forget about utopia’, for in the most part the urban environment of 2050 is already built. Architects’ sights need to be set on the sometimes grim and unfolding reality of favelas and the world's informal cities.     

To a Curator of Beautiful and Healthy Lives: A Note to Myself

How might architectural thinking and processes shift over the next 35 years? How might the architect's role be redefined with shifting ethical values? Could the architect be viewed as less of a design professional and more of a curator engaged in the development of healthy holistic environments, catering for all of society's needs? DaeWha Kang , an architect from 2050, writes to his earlier self, critiquing the work that he undertook in independent practice and as a design director at Zaha Hadid Architects in the mid-2010s. He describes how his design methodologies have evolved in the intervening years.