- NON-COORDINATING ANION TYPE ACTIVATORS FOR USE WITH POLYOLEFIN POLYMERIZATION CATALYSTS
-
The present disclosure is related to activator compounds represented by: [Ar(E11R11R22H)xx(E22R33R44)yy][QR55R66R77R88]zz In the formula Ar is a C66-C3030 aromatic hydrocarbyl group, provided that if Ar is a multicyclic ring, then each E11 and each E22 are substitutions on a single ring. Also, x is 1 to 4; y is 0 to 3; z = x; and x+y is 2 to 6. Each of E11 and E22 are independently selected from nitrogen or phosphorous and Q is selected from group 13 of the Periodic Table of the Elements. Additionally, each of R11, R22, R33 and R44 are independently selected from C11-C4040 aliphatic hydrocarbyl, substituted C11-C4040 aliphatic hydrocarbyl and each of R55, R66, R77, and R88 is independently a C66-C2424 hydrocarbyl or a C66-C2424 substituted hydrocarbyl. The present disclosure also relates to catalyst systems including a catalyst and the activator compound. Also, the present disclosure relates to methods of polymerizing olefins.
- -
-
-
- COLLECTIONS OF PEPTIDES, PEPTIDE AGENTS, AND METHODS OF USE THEREOF
-
The present disclosure provides powerful technologies for the development, production, characterization, and/or use of stapled peptide compositions. Among other things, the present disclosure provides strategies for defining amino acid sequences particularly amenable or useful for stapling, as well as technologies, reagents, and systems for developing, producing, characterizing, and/or using stapled peptides having such amino acid sequences.
- -
-
Paragraph 0345; 0349
(2020/03/15)
-
- Synthesis method of N-methylamine compound
-
The invention discloses a synthesis method of an N-methylamine compound. The synthesis method is characterized in that a carbamyl imidazole compound is used as a raw material; a NaBH4/I2 is used for performing backflow in tetrahydrofuran to prepare an N-methyl structure compound. The used reduction system NaBH4/I2 has the advantages of environment-friendly effect, performance stability, high conversion rate and the like. The synthesis method has the beneficial effects that (1) the synthesis method has wide applicability; amine can be used as the raw material; carboxylic acid can also be used as the raw material; (2) the product yield is high and reaches as high as 82 percent; (3) a synthetic agent is simple and can be easily obtained; the cost is low; the process is simple; the reaction conditions are mild; the synthesis method is suitable for industrial production. A concrete reaction formula is shown in the description, wherein R1 and R2 are identical or different atoms or groups, and are respectively and independently selected from one of hydrogen atoms, C1-C20 straight-chain or branch-chain alkane, C5-C10 naphthenic groups, aryl groups and substituted aryl groups; monosubstitution or multi-substitution is performed on aromatic rings of the substituted aryl groups. In addition, KBH4 is also applicable to the reaction.
- -
-
Paragraph 0079-0082
(2018/09/08)
-
- Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent
-
We report a series of tubulin targeting agents, some of which demonstrate potent antiproliferative activities. These analogs were designed to optimize the antiproliferative activity of 1 by varying the heteroatom substituent at the 4′-position, the basicity of the 4-position amino moiety, and conformational restriction. The potential metabolites of the active compounds were also synthesized. Some compounds demonstrated single digit nanomolar IC50 values for antiproliferative effects in MDA-MB-435 melanoma cells. Particularly, the S-methyl analog 3 was more potent than 1 in MDA-MB-435 cells (IC50 = 4.6 nM). Incubation of 3 with human liver microsomes showed that the primary metabolite of the S-methyl moiety of 3 was the methyl sulfinyl group, as in analog 5. This metabolite was equipotent with the lead compound 1 in MDA-MB-435 cells (IC50 = 7.9 nM). Molecular modeling and electrostatic surface area were determined to explain the activities of the analogs. Most of the potent compounds overcome multiple mechanisms of drug resistance and compound 3 emerged as the lead compound for further SAR and preclinical development.
- Xiang, Weiguo,Choudhary, Shruti,Hamel, Ernest,Mooberry, Susan L.,Gangjee, Aleem
-
p. 2437 - 2451
(2018/04/16)
-
- The iridium-catalyzed synthesis of symmetrically and unsymmetrically alkylated diamines under mild reaction conditions
-
An iridium catalyst - stabilized by an anionic P,N ligand - was used for the symmetrical and unsymmetrical monoalkylation of para-, meta-, and ortho-benzenediamines. Benzyl and aliphatic alcohols were used as alkylating reagents. 28 derivatives were synthesized. 14 of them are new compounds. Furthermore, the alkylation of the pharmacological important diamine Dapson (dapsone) is described. 14 dapsone derivatives were synthesized among them 9 new compounds. Copyright
- Michlik, Stefan,Hille, Toni,Kempe, Rhett
-
experimental part
p. 847 - 862
(2012/05/04)
-
- A facile and practical copper powder-catalyzed, organic solvent-and ligand-free ullmann amination of aryl halides
-
A facile and practical method that the copper powder-catalyzed Ullmann amination of aryl halides with aqueous methylamine under organic solvent-and ligand-free condition at 100 °C and in air gave N-arylamines as sole products in good to excellent yields. The presence of a small amount of air is essential. Other aliphatic primary amines show good to very high reactivity. Secondary amines and aniline are not reactive. Sensitive substituents (i.e., CHO, MeCO, CN and Cl) are tolerable in the reaction.
- Jiao, Jiao,Zhang, Xi-Ru,Chang, Ning-Hui,Wang, Jie,Wei, Jun-Fa,Shi, Xian-Ying,Chen, Zhan-Guo
-
supporting information; experimental part
p. 1180 - 1183
(2011/04/24)
-
- Polycationic states of oligoanilines based on Wurster's blue
-
Polycations of two oligoanilines based on Wurster's blue, N,N',N-tris[4-(dimethylamino)phenyl]-N,N',N-trimethyl1,3,5-benzenetriamine (2) and N,N'-bis(3-{N-[4-(dimethylamino)phenyl]-N-methylamino}phenyl)-N,N'-dimethyl- pphenylenediamine (3), have been generated efficiently by a stepwise oxidation procedure, Their redox behavior was characterized in terms of the embedded p-phenylenediamine (PD) units and their intramolecular connectivity, EPR analysis of the oxidized 2 and 3 species revealed the existence of high-spin species in solution. It was found that spin multiplicities of the dominant polycationic species of 2 and 3 formed by 3 equiv, of oxidant can be assigned to quartet: and doublet states, respectively on the basis of pulsed EPR spectroscopy, These results demonstrate that the intramolecular connectivity between the spin-containing units decisively influences the spin preference of the multispin systems based on oligoanilines.
- Ito, Akihiro,Sakamaki, Daisuke,Ino, Haruhiro,Taniguchi, Aya,Hirao, Yasukazu,Tanaka, Kazuyoshi,Kanemoto, Katsuichi,Kato, Tatsuhisa
-
experimental part
p. 4441 - 4450
(2010/03/03)
-
- Electronic interactions in tertiary oligophenylureas
-
The syntheses, structures, and spectroscopy of a series of oligomeric tertiary oligophenylureas possessing one to five phenyl rings are reported. A convergent synthetic method employing tertiary monoamine and diamine building blocks is employed. NMR and molecular modeling are indicative of folded structures for all of the oligophenylureas in which adjacent phenyl rings have a splayed face-to-face geometry. NMR chemical shifts, absorption and emission maxima, and electrochemical oxidation potentials are all dependent upon the number of phenyl rings. The addition of a first inner phenyl has a pronounced effect on the chemical shifts, while a second and third inner phenyl have diminished effects. The oxidation potentials of the oligophenylureas display an abrupt decrease upon the addition of the second inner phenyl. The absorption and emission spectra are relatively insensitive to the addition of one to three inner phenyl rings. The electronic structures of the oligophenylureas possessing one to eight rings have been analyzed using ZINDO calculations. The frontier orbitals of the ureas with one to three phenyl rings are localized on a single phenyl ring (the inner ring for the three-ring urea), whereas the frontier orbitals of the higher oligomers are delocalized over two phenyl rings. In all cases, urea-localized n,π* transitions are lower in energy than the phenyl-localized n,π* transitions. The changes in properties with added phenyl rings parallel those previously observed for multilayered cyclophanes; however, they are less pronounced because of weaker coupling between the phenyl rings of the oligophenylureas.
- Lewis, Frederick D.,Kurth, Todd L.,Delos Santos, Grace B.
-
p. 4893 - 4899
(2008/03/14)
-
- Chemical process
-
Aromatic amines (e.g., aniline) are selectively alkylated in an ortho nuclear position by reaction with an olefin (e.g., ethylene) in the presence of an aluminum anilide catalyst. Hydrogen halides (e.g., HCl) are added to increase the reaction rate.
- -
-
-