- N-Acyl-N-(4-chlorophenyl)-4-nitrobenzenesulfonamides: Highly selective and efficient reagents for acylation of amines in water
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A variety of N-acyl-N-(4-chlorophenyl)-4-nitrobenzenesulfonamides (1a-e) were synthesized in one pot from 4-chloroaniline under solvent-free conditions and have been developed as chemoselective N-acylation reagents. Selective protection of primary amines in the presence of secondary amines, acylation of aliphatic amines in the presence of aryl amines, and monofunctionalization of primary-secondary diamines as well as selective N-acylation of amino alcohols using these reagents are described. All of the acylation reactions were carried out in water as a green solvent. High stability and easy preparation of these acylating reagents are other advantages of this method.
- Ebrahimi, Sara,Saiadi, Safoura,Dakhilpour, Simin,Mirsattari, Seyed Nezamoddin,Massah, Ahmad Reza
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- COMPOSITIONS AND METHODS FOR MODULATING HEXIM1 EXPRESSION
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The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives of formula I, that induce Hexamethylene bis-acetamide inducible protein 1 (HEXIM1 ) was determined in cancer cells. The method of inducing HEXIM1 expression and cell differentiation in cancer and HIV cells are disclosed. Optimization of HMBA analogs that are symmetrical and unsymmetrical are also discussed.
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Paragraph 00187
(2015/09/23)
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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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experimental part
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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- 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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- 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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- NOVEL UNSYMMETRICAL N,N-BIS(METHYLENE)BIPHOSPHONIC ACIDS OF α,ω-DIAMINES. PREPARATION AND CHARACTERIZATION OF BIS(METHYLENE)>-BIPHOSPHONIC ACID AND BIS(METHYLENE)>-BIPHOSPHONIC ACID
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Reaction of ethylenediamine with phosphorous acid and formaldehyde in molar ratio 1:2:2 gives bis(methylene)>biphosphonic acid (2a) as the major product.Similarly, reaction of hexamethylenediamine with phosphorous acid and formaldehyde in molar ratio 1:2:2 yields bis(methylene)>biphosphonic acid (2b) which is isolated either as bis(methylene>biphosphonic acid (3b) or as bis(methylene)>biphosphonic acid (4b).Removal of the carbobenzoxy group with HBr 3b or the benzoyl group with HCl from 4b gives pure bis(methylene)>biphosphonic acid (2b).All compounds were characterized by 13C NMR, 31P NMR and elemental analysis.
- Redmore, Derek,Dhawan, Balram
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p. 233 - 238
(2007/10/02)
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