89943-28-2Relevant academic research and scientific papers
Solvent- and Catalyst-Free Aza-Michael Addition of Imidazoles and Related Heterocycles
Gobec, Florian,Kodolitsch, Katharina,Slugovc, Christian
, (2020/05/18)
This work demonstrates the scope and limitations of the aza-Michael addition of imidazoles and related heterocycles with electron deficient olefins under solvent- and catalyst-free conditions. The reaction proceeds at 80 °C within hours towards completion as long as the azole derivative is sufficiently soluble in the Michael acceptor, which has been used in small excess. Workup only comprises evaporation of surplus Michael-acceptor, and no additional solvents are necessary for purifying the products.
A process for the preparation of pyrazole derivatives
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Paragraph 0194-0199, (2017/02/23)
The invention relates to a method for preparing a pyrazole derivative. The method comprises the following steps: (1) sequentially adding 5mol% of cesium carbonate, 0.3mmol of ketene, 0.45mmol of pyrazol and 1.5mL of 1,4-dioxane into a dried Schlenk reacti
Guanidine-based task-specific ionic liquids as catalysts for aza-Michael addition under solvent-free conditions
Ying, Anguo,Zheng, Ming,Xu, Haidan,Qiu, Fangli,Ge, Changhua
experimental part, p. 883 - 890 (2012/04/17)
An efficient and facile protocol for aza-Michael addition of aliphatic and aromatic amines to electron-deficit alkenes using [TMG][Lac] as catalyst under solvent-free conditions was established.
Aza-Michael addition of aliphatic or aromatic amines to α,β-unsaturated compounds catalyzed by a DBU-derived ionic liquid under solvent-free conditions
Ying, An-Guo,Liu, Luo,Wu, Guo-Feng,Chen, Gang,Chen, Xin-Zhi,Ye, Wei-Dong
experimental part, p. 1653 - 1657 (2009/06/28)
A task-specific ionic liquid, 1,8-diazabicyclo[5.4.0]-undec-7-en-8-ium acetate has been successfully used as a catalyst for aza-conjugate addition of aliphatic or aromatic amines to various electron deficient alkenes under solvent-free conditions and at room temperature. The catalyst can be reused for six times without noticeable loss of activity.
1,8-Diazabicyclo[5.4.0]undec-7-ene (DBU)-promoted efficient and versatile aza-Michael addition
Yeom, Chang-Eun,Kim, Mi Jeong,Kim, B. Moon
, p. 904 - 909 (2007/10/03)
A convenient and versatile method was developed for aza-Michael addition using a substoichiometric amount of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). Various nitrogen nucleophiles were efficiently introduced to α,β-unsaturated carbonyl compounds employing 0.5 equiv of DBU. Furthermore, other heteroatomic nucleophiles could also be introduced successfully under the same reaction conditions.
A fast and highly efficient protocol for Michael addition of N-heterocycles to α,β-unsaturated compound using basic ionic liquid [bmIm]OH as catalyst and green solvent
Xu, Jian-Ming,Qian, Chao,Liu, Bo-Kai,Wu, Qi,Lin, Xian-Fu
, p. 986 - 990 (2007/10/03)
A fast and green protocol for the Michael addition of N-heterocycles to α,β-unsaturated compounds at room temperature was developed using a basic ionic liquid, 1-methyl-3-butylimidazolium hydroxide, [bmIm]OH, as a catalyst and a reaction medium. The react
Promiscuous acylase-catalyzed aza-Michael additions of aromatic N-heterocycles in organic solvent
Qian, Chao,Xu, Jian-Ming,Wu, Qi,Lv, De-Shui,Lin, Xian-Fu
, p. 6100 - 6104 (2008/03/12)
A novel and efficient enzymatic promiscuous protocol for aza-Michael addition of aromatic N-heterocycles to α,β-unsaturated compounds has been described. The reactions were catalyzed by promiscuous zinc-active-site acylase in organic solvent at 50 °C. The strategy works with a broad range of N-heterocycles to afford the corresponding Michael adduct with good yields in several hours (0.5-6 h). This catalytic promiscuity is the first example of metal-active-site enzyme-catalyzed aza-Michael addition for aromatic N-heterocycles.
Highly efficient aza-Michael reactions of aromatic amines and N-heterocycles catalyzed by a basic ionic liquid under solvent-free conditions
Yang, Lei,Xu, Li-Wen,Zhou, Wei,Li, Lyi,Xia, Chun-Gu
, p. 7723 - 7726 (2007/10/03)
A task-specific basic ionic liquid, [Bmim]OH, has been introduced as a catalyst for the aza-Michael addition of aromatic amines and N-heterocycles to cyclic or acyclic ketones under neat conditions. The catalyst can be recycled for subsequent reactions without any appreciable loss of efficiency.
Studies on β-lactam antibiotics, synthesis and antibacterial activity of novel 1β-methylcarbapenems related to FR21818: 5-membered ring analogs
Azami, Hidenori,Barrett, David,Tanaka, Akira,Sasaki, Hiroshi,Matsuda, Keiji,Sakurai, Minora,Matsumoto, Yoshimi,Tawara, Shuichi,Chiba, Toshiyuki,Sakane, Kazuo
, p. 1409 - 1414 (2007/10/03)
The synthesis and biological activity of the novel series of 1β-methylcarbapenems 1 are described. Most compounds displayed extremely potent antibacterial activity and high renal DHP-I stability. The best compound in this series, FR21818 (1a) displayed ex
