- Tunable Synthesis of α-Amino Boronic Esters from Available Aldehydes and Amines through Sequential One-Pot Dehydration and Copper-Catalyzed Borylacylation
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Copper-catalyzed multicomponent borylacylation of imines with acid chlorides and bis(pinacolato)diboron was developed for the preparation of synthetically useful and pharmacologically relevant α-amino boronic acid derivatives. Starting from a range of acid chlorides and imines with aryl, heteroaryl, and alkyl substituents, most of these ligand-free reactions proceeded smoothly at room temperature in moderate to good yields. Furthermore, a facile and convenient one-pot, multistep access to the direct synthesis of α-amino boronic acid derivatives from available aldehydes and amines was also developed.
- Xia, Qi,Chang, Hua-Rong,Li, Juan,Wang, Jia-Yi,Peng, Yan-Qing,Song, Gong-Hua
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p. 2716 - 2724
(2020/01/31)
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- CuO nanoparticle catalysed synthesis of 2H-indazoles under ligand free conditions
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A CuO nano catalysed one-pot synthesis of 2H-indazoles has been devised from easily accessible starting materials viz. 2-bromobenzaldehydes, primary amines and sodium azide under ligand free conditions. The nano CuO catalyst played an important role during the formation of the intermolecular C-N bond followed by the intramolecular N-N bond, providing 2H-indazoles. This method has a broad substrate scope with a high tolerance of a variety of functional groups. The catalyst can be recycled up to three times, however with slight decreases in the yields each time.
- Khatun, Nilufa,Gogoi, Anupal,Basu, Pallabita,Das, Prasenjit,Patel, Bhisma K.
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p. 4080 - 4084
(2014/01/06)
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- Regioselective Cu(I)-catalyzed tandem A3-coupling/ decarboxylative coupling to 3-amino-1,4-enynes
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An efficient and novel copper-mediated protocol for the synthesis of 3-amino-1,4-enynes from glyoxylic acid, an amine, and an alkyne was developed. This new reaction involving two sequential C-C bond formations is air and moisture tolerant and proceeds via a tandem A3-coupling and a selective decarboxylative coupling.
- Feng, Huangdi,Ermolat'Ev, Denis S.,Song, Gonghua,Van Der Eycken, Erik V.
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supporting information; experimental part
p. 1942 - 1945
(2012/05/31)
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- Synthesis of symmetric 1,4-diamino-2-butynes via a Cu(I)-catalyzed one-pot A3-coupling/decarboxylative coupling of a propiolic acid, an aldehyde, and an amine
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A novel microwave-assisted approach for the one-pot Cu(I)-catalyzed A 3-coupling/decarboxylative coupling (PA2-coupling) of a propiolic acid, an aldehyde, and an amine, resulting in the formation of diversely substituted 1,4-diamino-2-butynes,is described. It is noteworthy that this new multicomponent coupling provides an efficient access to introduce alkyl and aryl group at the 1,4-position of the 1,4-diamino-2-butynes.
- Feng, Huangdi,Ermolat'ev, Denis S.,Song, Gonghua,Van Der Eycken, Erik V.
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experimental part
p. 5149 - 5154
(2012/07/14)
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- COMPOUNDS FOR IMPROVING LEARNING AND MEMORY
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The present invention provides a compound of Formula I: (I) and methods for improving memory in a subject by administering a therapeutically effective amount of the compound.
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Page/Page column 3; 19
(2009/12/23)
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- Design and synthesis of novel, conformationally restricted HMG-CoA reductase inhibitors
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Using structure-based design, a novel series of conformationally restricted, pyrrole-based inhibitors of HMG-CoA reductase were discovered. Leading analogs demonstrated potent inhibition of cholesterol synthesis in both in vitro and in vivo models and may
- Pfefferkorn, Jeffrey A.,Choi, Chulho,Song, Yuntao,Trivedi, Bharat K.,Larsen, Scott D.,Askew, Valerie,Dillon, Lisa,Hanselman, Jeffrey C.,Lin, Zhiwu,Lu, Gina,Robertson, Andrew,Sekerke, Catherine,Auerbach, Bruce,Pavlovsky, Alexander,Harris, Melissa S.,Bainbridge, Graeme,Caspers, Nicole
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p. 4531 - 4537
(2008/02/12)
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- The cleavage of 1-amino-2'-nitrobenzylphosphonates in a basic medium. Formation of the 3-amino-2,1-benzisoxazole derivatives
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Treatment of 1-amino-2'-nitrobenzylphosphonic acids with aqueous sodium hydroxide caused a C-P bond cleavage, with formation of 3-amino-2,1-benzisoxazole derivatives (3). The leaving phosphorus moiety was identified here as phosphoric acid. In the case of basic hydrolysis of corresponding esters, new cyclic phosphorus compounds (derivatives of benzoxazaphosphorin-3,1,2 P(v)-one-2) were obtained. The cyclic products were formed as a result of the subsequent reaction of anthranil derivatives with leaving phosphorus fragment, presumably metaphosphate, These benzoxazaphosphorins (cormpounds 4) were converted by means of aqueous hydrochloric acid to 3-amino-2,1-benzisoxazole derivatives.
- Boduszek, Bogdan,Halama, Agnieszka,Zon, Jerzy
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p. 11399 - 11410
(2007/10/03)
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