105-10-2Relevant articles and documents
NON-COORDINATING ANION TYPE ACTIVATORS FOR USE WITH POLYOLEFIN POLYMERIZATION CATALYSTS
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, (2021/02/12)
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.
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
Xiang, Weiguo,Choudhary, Shruti,Hamel, Ernest,Mooberry, Susan L.,Gangjee, Aleem
, p. 2437 - 2451 (2018/04/16)
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.
The iridium-catalyzed synthesis of symmetrically and unsymmetrically alkylated diamines under mild reaction conditions
Michlik, Stefan,Hille, Toni,Kempe, Rhett
experimental part, p. 847 - 862 (2012/05/04)
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
