- Synthesis of non-symmetrical 3,4-diaryl-substituted pyrroles: Implementation for the preparation of lamellarin R
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A straightforward method for synthesising symmetrical and non-symmetrical 3,4-diaryl-substituted pyrroles is proposed, consisting of (i) the condensation reaction between phenylacetonitriles and aldehydes to give acrylonitriles, (ii) the conjugate additio
- Zavala-Gómez, Héctor,Ramírez-Rodríguez, Armando,Vázquez, Alfredo
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p. 677 - 683
(2018/01/08)
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- Highly active g-C3N4 as a solid base catalyst for knoevenagel condensation reaction under phase transfer conditions
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In a promising approach, heterogeneous g-C3N4 as a solid base catalyst exhibits appreciable activity in Knoevenagel condensations at room temperature for the synthesis of substituted stilbene in presence of a crown-ether phase transfer catalyst. High yield of the product substituted stilbene were isolated in a very short reaction time period (～30 min). The solid base g-C3N4 catalyst was proven to be recyclable for several runs. Various aromatic substrates were screened using heterogeneous base g-C3N4 catalyst, exhibiting appreciable corresponding product yield (～99%) at room temperature.
- Sharma, Priti,Sasson, Yoel
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p. 25589 - 25596
(2017/07/10)
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- A process for preparing two aromatic ring substituted olefins method
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The invention relates to an efficient environment-friendly catalyst, and a new method for preparing double-(hetero)aromatic-ring substituted alkene under a room-temperature condition by taking water as a reaction medium. The method comprises: taking n-propylamine supported by super-paramagnetism nanometer particles and modified by ion atmosphere as a catalyst, and under the conditions of room temperature, normal pressure and water reaction medium, performing Knoevenagel condensation reaction on an (hetero)aromatic-ring substituted active alkene substance and an aromatic aldehyde, so as to obtain a corresponding double-(hetero)aromatic-ring substituted alkene derivative. The reaction yield is not obviously reduced after the supported catalyst is repeatedly used for 8 times. The method is simple in operation, high in yield, simple in catalyst recovery, good in reusability of the catalytic reaction system and mild in reaction conditions, and has good industrialization prospect.
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Paragraph 0049-0051
(2017/06/08)
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- A Paal-Knorr approach to 3,4-diaryl-substituted pyrroles: Facile synthesis of lamellarins O and Q
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A very simple, yet efficient synthetic methodology, to obtain 3,4-diaryl-substituted pyrroles is described. The approach is based on the Knoevenagel condensation between arylacetonitriles and substituted aromatic aldehydes, followed by conjugate addition of cyanide to afford succinonitriles in excellent yields. The products thus obtained were subjected to DIBAL-H reduction, followed by cyclization under acidic conditions to produce the corresponding pyrroles in good overall yields. The utility of this protocol is exemplified by the synthesis of the marine alkaloids lamellarins O and Q.
- Ramirez-Rodriguez, Armando,Mendez, Jose M.,Jimenez, Cristina C.,Leon, Fernando,Vazquez, Alfredo
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p. 3321 - 3326,6
(2012/12/12)
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- Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold
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Employing a structure-based strategy, we have designed a new class of potent small-molecule inhibitors of the anti-apoptotic proteins Bcl-2 and Bcl-xL. An initial lead compound with a new scaffold was designed based upon the crystal structure of Bcl-xL an
- Zhou, Haibin,Chen, Jianfang,Meagher, Jennifer L.,Yang, Chao-Yie,Aguilar, Angelo,Liu, Liu,Bai, Longchuan,Cong, Xin,Cai, Qian,Fang, Xueliang,Stuckey, Jeanne A.,Wang, Shaomeng
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experimental part
p. 4664 - 4682
(2012/07/28)
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