- Method for preparing derivatives of benzamide under microwave condition in aqueous phase
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The invention discloses a method for preparing derivatives of benzamide under a microwave condition in an aqueous phase. A coupling reaction is carried out between substituted benzoic acid and amine under the microwave condition in the aqueous phase. The method for preparing the derivatives of benzamide is environmentally friendly, easy and convenient to operate, safe, low in cost and efficient. Compared with the prior art, the method can be applicable to a large number of functional groups, is high in yield, produces fewer by-products, and further is easy to operate, safe, low in cost and environmentally friendly. A formula is shown in the description.
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Paragraph 0019; 0027
(2019/03/28)
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- Cyclodehydration of N -(aminoalkyl)benzamides under mild conditions with a hendrickson reagent analogue
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Methods for the cyclodehydration of N-(aminoalkyl)benzamides are few and employ harsh reaction conditions. We have found that the easily prepared phosphonium anhydrides 1 (Hendrickson reagent) or 2 can be used for cyclodehydration of N-(aminoalkyl)benzamides under very mild conditions (room temperature) to produce five-, six-, and seven-membered cyclic amidines. Good yields are obtained by employing a temporary trityl group protection strategy. Cyclic analogue 2 can be used when the product cyclic amidine is organic-soluble, thus producing water-soluble byproducts.
- Loughlin, Wendy A.,Jenkins, Ian D.,Petersson, Maria J.
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p. 7356 - 7361
(2013/08/23)
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- Structural analysis of ATP analogues compatible with kinase-catalyzed labeling
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Kinase-catalyzed protein phosphorylation is an important biochemical process involved in cellular functions. We recently discovered that kinases promiscuously accept γ-modified ATP analogues as cosubstrates and used several ATP analogues as tools for stud
- Suwal, Sujit,Senevirathne, Chamara,Garre, Satish,Pflum, Mary Kay H.
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p. 2386 - 2391
(2013/02/23)
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- CDI-mediated monoacylation of symmetrical diamines and selective acylation of primary amines of unsymmetrical diamines
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A highly efficient and green protocol for monoacylation of symmetrical diamines and chemoselective acylation of primary amines of unsymmetrical diamines has been developed.
- Verma, Sanjeev K.,Ghorpade, Ramarao,Pratap, Ajay,Kaushik
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p. 326 - 329
(2012/04/10)
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- Efficient and continuous monoacylation with superior selectivity of symmetrical diamines in microreactors
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Efficient and continuous monoacylation of symmetrical diamines performed in microreactors yielded superior selectivity to that predicted by statistical considerations. It is highly valuable that the kinetically controlled product in high yields was achieved without any special catalyst at ambient temperature.
- Maurya, Ram Awatar,Hoang, Phan Huy,Kim, Dong-Pyo
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scheme or table
p. 65 - 68
(2012/03/26)
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- New Potent Bisubstrate Inhibitors of Histone Acetyltransferase p300: Design, Synthesis and Biological Evaluation
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Bisubstrate-type compound Lys-CoA has been shown to inhibit the p300 histone acetyl transferase activity efficiently and may constitute a lead compound for a novel class of anticancer therapeutics. Based on this strategy, we synthesized a series of CoA derivatives and evaluated these molecules for their activity as p300 histone acetyltransferases inhibitor. The best activity was obtained with compound 3 bearing a C-5 spacing linker that connects the CoA moiety to a tert-butyloxycarbonyl (Boc) group. Based on docking simulations, this inhibitor exhibits favorable interactions with two binding areas, namely pockets P1 and P2, within the active site.
- Kwie, Franciane Ho A.,Briet, Martine,Soupaya, David,Hoffmann, Pascal,Maturano, Marie,Rodriguez, Frederic,Blonski, Casimir,Lherbet, Christian,Baudoin-Dehoux, Cecile
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scheme or table
p. 86 - 92
(2011/09/15)
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- Imidazole-catalyzed monoacylation of symmetrical diamines
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Figure Presented. An imidazole-catalyzed protocol for monoacylation of symmetrical diamines has been developed. The protocol gave selective monoacylation of aliphatic (cyclic and acyclic) primary and secondary diamines. In the reaction, imidazole acts as both catalyst and a leaving group. Different monoacylated piperazines and other diamines were synthesized at room temperature in an ethanol/water solvent system.
- Verma, Sanjeev K.,Acharya,Kaushik
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supporting information; experimental part
p. 4232 - 4235
(2010/11/04)
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- Phenyl esters, preferred reagents for mono-acylation of polyamines in the presence of water
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In the presence of water, several diamines and one triamine were mono-acylated at ambient to moderate temperatures using phenyl esters and a phenyl carbonate as acylation agents in good to excellent isolated yields. Both linear and cyclic polyamines were suitable substrates, and the acylating agents can be aryl and alkyl carboxylic acid esters.
- Pappas, Kyrie,Zhang, Xiang,Tang, Wei,Fang, Shiyue
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body text
p. 5741 - 5743
(2009/12/06)
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- Mono-acylation of symmetric diamines in the presence of water
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Simply reacting equal equivalents of symmetric diamines with esters or carbonates in the presence of a suitable amount of water gave mono-acylated products in good to quantitative yields.
- Tang, Wei,Fang, Shiyue
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supporting information; scheme or table
p. 6003 - 6006
(2009/04/11)
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- Selective Monoacylation of Symmetrical Diamines via Prior Complexation with Boron
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(Equation presented) Pretreatment of a symmetrical primary or secondary diamine with 9-BBN prior to the addition of an acyl chloride significantly suppressed undesired diacylation, and the product of monoacylation predominated. The reactive preference is interpreted as the result of a selective deactivation of one nitrogen atom of the diamine by 9-BBN.
- Zhang, Zhongxing,Yin, Zhiwei,Meanwell, Nicholas A.,Kadow, John F.,Wang, Tao
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p. 3399 - 3402
(2007/10/03)
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- A Simple and Economic Synthesis of Monoacylated Alkanediamines by Thermal Transamidation
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N-(ω-Aminoalkyl)amides 2 are easily synthesized by heating mixtures of excess α,ω-alkanediamines 1 and primary amides to temperatures between 150 deg C and 200 deg C, at which thermal transamidation occurs.Under the reaction conditions ammonia is released, and 2 is in equilibrium with the alkanediamine 1 and the α,ω-bis(acylamino)alkane 3.Thus, thermal transamidation is a practicable way to overcome the problem of diacylation which appears as an often recognized problem even in the latest literature.
- Zaragoza-Doerwald, Florencio,Kiedrowski, Guenter von
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p. 917 - 918
(2007/10/02)
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