- Polymer-supported palladium-imidazole complex catalyst for hydrogenation of substituted benzylideneanilines
-
The polymer-supported palladium-imidazole complex catalyst was synthesized and characterized by various techniques such as elemental analysis, IR spectroscopy and TG analysis. The physico-chemical properties such as bulk density, surface studies by BET me
- Udayakumar,Alexander,Gayathri,Shivakumaraiah,Patil,Viswanathan
-
-
Read Online
- SOX11 INHIBITORS FOR TREATING MANTLE CELL LYMPHOMA
-
Disclosed are compounds that are chemical inhibitors of SOX11. The compounds disclosed are useful in treatment of various cancers.
- -
-
-
- Lewis acid solid catalysts for the synthesis of methylenedianiline from aniline and formaldehyde
-
A catalyst containing Hf4+ and Zn2+ supported on silica has been found to be highly effective for the synthesis of methylenedianiline (MDA), an indispensable precursor in the polyurethane industry. Its performance was further improved when the silica support was replaced by silica-alumina, which resulted in a catalyst that was both active and selective, as indicated by the high MDA yield and high 4,4′–MDA/(2,2′–MDA + 2,4′–MDA) isomer ratio obtained. Furthermore, the catalyst also gave an appreciable oligomeric MDA (OMDA) yield and was noticeably more stable than the zeolites that were used in comparative tests: it could be used in at least five consecutive runs without any significant loss in activity. The combination of Br?nsted and Lewis acidity strongly increases the overall activity and yields a catalyst that represents a remarkably stable and reusable alternative to the commonly studied systems for this reaction.
- Cheung, Ka Yan,De Baerdemaeker, Trees,De Vos, Dirk,Gordillo, Alvaro,Marquez, Carlos,Parvulescu, Andrei-Nicolae,Tomkins, Patrick
-
p. 114 - 123
(2021/06/16)
-
- Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as new potent and selective human sirtuin 2 inhibitors
-
Human sirtuin 2 (SIRT2) plays pivotal roles in multiple biological processes such as cell cycle regulation, autophagy, immune and inflammatory responses. Dysregulation of SIRT2 was considered as a main aspect contributing to several human diseases, including cancer. Development of new potent and selective SIRT2 inhibitors is currently desirable, which may provide a new strategy for treatment of related diseases. Herein, a structure-based optimization approach led to new 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacetamide derivatives as SIRT2 inhibitors. SAR analyses with new synthesized derivatives revealed a number of new potent SIRT2 inhibitors, among which 28e is the most potent inhibitor with an IC50 value of 42?nM. The selectivity analyses found that 28e has a very good selectivity to SIRT2 over SIRT1 and SIRT3. In cellular assays, 28e showed a potent ability to inhibit human breast cancer cell line MCF-7 and increase the acetylation of α-tubulin in a dose-dependent manner. This study will aid further efforts to develop highly potent and selective SIRT2 inhibitors for the treatment of cancer and other related diseases.
- Yang, Lingling,Ma, Xiaobo,Yuan, Chen,He, Yanying,Li, Ling,Fang, Sha,Xia, Wei,He, Tao,Qian, Shan,Xu, Zhihong,Li, Guobo,Wang, Zhouyu
-
p. 230 - 241
(2017/04/19)
-
- N-(4-substituted phenyl)-2-substituted acetamide compound and is use as SIRT2 protein inhibitor
-
The invention discloses a compound shown in the formula I or its pharmaceutically acceptable salt, crystalline form and solvate. X represents a group shown in the description, Y represents a group shown in the description, R1, R2 and R3 independently represent H, hydroxyl, halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl or phenyl, and R4 represents aryl, heteroaryl, substituted aryl or substituted heteroaryl. The novel compound shown in the formula I has good inhibition activity to SIRT2 and tumors, has a good medicinal value and provides a novel potential choice for clinical medication.
- -
-
Paragraph 0167; 0169
(2017/08/02)
-
- A convenient and general reduction of amides to amines with low-valent titanium
-
Low-valent titanium readily prepared in situ from TiCl4 and Mg powder in THF is found to be an active agent for the reduction of amides which were previously considered to be inert towards low-valent titanium. The reaction proceeds under very mild conditions, and is applicable to all types of amides, primary, secondary and tertiary, to produce the corresponding amines in good to excellent yields. This new finding provides a practical, convenient and general method for the important transformation of amides to amines. A plausible reaction mechanism is proposed.
- Zhang, Tongxin,Zhang, Yan,Zhang, Weixi,Luo, Meiming
-
supporting information
p. 2775 - 2780
(2014/03/21)
-
- PRODUCTION OF MIXTURES OF METHYLENEDIANILINE AND ITS HIGHER HOMOLOGUES USING CALCINED METAL OXIDE-SILICA CATALYSTS
-
The present disclosure relates to compositions, systems, and methods of forming an amine (e.g., methylenedianiline (MDA)) using an acid catalyst including, for example, a metal oxide-silica catalyst calcined at temperature(s) of about ≥ 500°C to form a solid acid silica-metal oxide catalyst. A metal oxide of a solid acid silica-metal oxide catalyst may comprise alumina. A process for making a solid acid silica-metal oxide catalyst may comprise calcining an amorphous alumina-silica material at temperature(s) of about ≥ 500°C and/or under an anhydrous and/or inert atmosphere. A rearrangement reaction of the condensation product of aniline and formaldehyde in the presence of a solid acid silica-metal oxide catalyst may yield more MDA and/or more desirable isomer(s) of MDA than reactions performed with a corresponding catalyst calcined at temperature(s) of less than 500°C.
- -
-
Page/Page column 17
(2010/04/03)
-
- Reductive amination of aromatic aldehydes and ketones with nickel boride
-
The reductive amination of aromatic aldehydes and ketones with nickel boride was investigated. The reactions of aromatic aldehydes and ketones with primary amines produced corresponding secondary amines in the presence of in situ generated nickel boride. The secondary amines were found to remain inert in the system.
- Saxena, Ira,Borah, Ruli,Sarma, Jadab C.
-
p. 503 - 504
(2007/10/03)
-
- Preparation of N,O-Aminals as Synthetic Equivalents of H2C=NAr and (H2C=NHAr)+ ions: Neutral- and Acid-promoted Transformations
-
A general method for the synthesis of N, O-aminals derived from primary aromatic amines is described.The reactivity of these compounds under neutral and acidic conditions has been studied and the title compounds can be envisaged as general purpose H2C=NAr or (H2C=NAr)+ equivalents.N,O-Aminals have been converted into perhydrotriazines by moderate heating and into bis(4-aminoaryl)methane derivatives or N-benzylarylamines, respectively, when heated in acidid media with pH control.Reduction od N,O-acetals with sodium cyanoborohydride has revealed that the C-O bond is broken exclusively in acidic media.
- Barluenga, Jose,Bayon, Ana M.,Campos, Pedro,Asensio, Gregorio,Gonzalez-Nunez, Elena,Molina, Yolanda
-
p. 1631 - 1636
(2007/10/02)
-
- TRINUCLEAR INTERMEDIATES IN ANILINE-FORMALDEHYDE CONDENSATION
-
The trinuclear intermediate products 4-(4-anilinomethylanilinomethyl)aniline and 4-aniline were isolated and identified by TLC during investigation of the aniline-formaldehyde condensation in the presence of acidic catalysts.The transformation of these compounds and of 4-anilinomethylaniline in methanol and under the conditions of acid aniline-formaldehyde condensation and rearrangement are described.It was established that the fromation of polyamines is possible not only as a result of the initial reaction of the final diamines with formaldehyde but also of the reaction of protonated anilinomethylanilines with aromatic amines present in the reaction mixture.
- Ringel', Kh.,Popov, L.K.,Ushakova, M.B.
-
p. 882 - 885
(2007/10/02)
-
- Alkylidene Transfer from Monochloroalkylmercury(II) Compounds to Aromatic Amines; Selective C-Alkylation
-
αα-Diarylalkane derivatives have been synthesized from monochloroalkylmercury(II) compounds in a noncarbenoid alkylidene transfer reaction which takes place selectively on the aromatic ring.A mechanism is suggested for this process.Intermediate products are prepared by alternative routes to ascertain their participation in the course of the reaction.As a consequence, two different aryl groups can be successively incorporated into the alkane molecule.
- Barluenga, Jose,Campos, Pedro J.,Roy, Miguel A.,Asensio, Gregorio
-
p. 1420 - 1426
(2007/10/02)
-