3073-59-4Relevant articles and documents
Cooperative Binding of Divalent Diamides by N-Alkyl Ammonium Resorcinarene Chlorides
Beyeh, N. Kodiah,Ala-Korpi, Altti,Pan, Fangfang,Jo, Hyun Hwa,Anslyn, Eric V.,Rissanen, Kari
, p. 9556 - 9562 (2015)
N-Alkyl ammonium resorcinarene chlorides, stabilized by an intricate array of hydrogen bonds leading to a cavitand-like structure, bind amides. The molecular recognition occurs through intermolecular hydrogen bonds between the carbonyl oxygen and the amide hydrogen of the guests and the cation-anion circular hydrogen-bonded seam of the hosts, as well as through CH7mellip;π interactions. The N-alkyl ammonium resorcinarene chlorides cooperatively bind a series of di-acetamides of varying spacer lengths ranging from three to seven carbons. Titration data fit either a 1:1 or 2:1 binding isotherm depending on the spacer lengths. Considering all the guests possess similar binding motifs, the first binding constants were similar (K1:102M-1) for each host. The second binding constant was found to depend on the upper rim substituent of the host and the spacer length of the guests, with the optimum binding observed with the six-carbon spacer (K2:103M-2). Short spacer lengths increase steric hindrance, whereas longer spacer lengths increase flexibility thus reducing cooperativity. The host with the rigid cyclohexyl upper rim showed stronger binding than the host with flexible benzyl arms. The cooperative binding of these divalent guests was studied in solution through 1HNMR titration studies and supplemented by diffusion-ordered spectroscopy (DOSY), X-ray crystallography, and mass spectrometry. Cooperative guests: N-Alkyl ammonium resorcinarene chlorides cooperatively bind a series of homoditopic alkyl diamides of varying spacer lengths (see figure). The highest binding was observed with the six-carbon spacer guest. The cooperative binding of these divalent guests was studied in solution by using 1HNMR titration studies and supplemented by diffusion-ordered NMR spectroscopy (DOSY), X-ray crystallography, and mass spectrometry.
Method for preparing diamide under catalysis of non-noble metal
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Paragraph 0018, (2018/02/04)
The invention discloses a method for preparing diamide under catalysis of non-noble metal. Diamine, a nitrile compound and water are taken as raw materials and subjected to an acylation reaction in presence of a non-noble metal catalyst for preparation of diamide, wherein the non-noble metal catalyst is a transition metal oxide or a supporting transition metal oxide, the transition metal oxide adopts CuO or Cu2O, and a support adopts SiO2 or Al2O3. The diamine conversion rate is 99% or higher and the selectivity is 99% or higher under optimized reaction conditions. The method has the advantages of short reaction time, available catalyst, low catalyst cost, high conversion rate, high reaction selectivity and the like and has very high actual application value.
Lead optimization of HMBA to develop potent HEXIM1 inducers
Zhong, Bo,Lama, Rati,Ketchart, Wannarasmi,Montano, Monica M.,Su, Bin
, p. 1410 - 1413 (2014/03/21)
The potency of a series of Hexamethylene bis-acetamide (HMBA) derivatives inducing Hexamethylene bis-acetamide inducible protein 1 (HEXIM1) was determined in LNCaP prostate cancer cells. Several compounds with unsymmetrical structures showed significantly improved activity. Distinct from HMBA, these analogs have increased hydrophobicity and can improve the short half-life of HMBA, which is one of the factors that have limited the application of HMBA in clinics. The unsymmetrical scaffolds of the new analogs provide the basis for further lead optimization of the compounds using combinatorial chemistry strategy.
