- 4-anilinoquinazoline derivative and albumin conjugates thereof
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a pharmaceutical composition for preventing, treating, or ameliorating one or more symptoms of a malignant tumor associated with EGFR mutation and/or K-RAS mutation is provided. The pharmaceutical composition includes a 4-anilinoquinazoline derivative having a formula (I) where A is iodine when m is 1 and n is zero, or A is albumin when m is an integral ranging from 1 to 7 and n is 1.
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Page/Page column 8
(2019/04/26)
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- Synthesis of novel poly(ethylene glycol)-containing imidazolium-functionalized phosphine ligands and their application in the hydrosilylation of olefins
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A series of polyethylene glycol-containing imidazolium-functionalized phosphine ligands (mPEG-im-PPh2) were successfully synthesized and used in the rhodium-catalyzed hydrosilylation of olefins. The results indicate that the RhCl3/mPEG-im-PPh2 catalytic system exhibits both excellent activity and selectivity for the β-adduct. In addition, the catalytic system may be recycled at least six times.
- Zhang, Guodong,Li, Jiayun,Yang, Chuang,Niu, Congbai,Bai, Ying,Liu, Yu,Peng, Jiajian
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- Synthesis and biological assay of erlotinib analogues and BSA-conjugated erlotinib analogue
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A series of erlotinib analogues that have structural modification at 6,7-alkoxyl positions is efficiently synthesized. The in vitro anti-tumor activity of synthesized compounds is studied in two non-small cell lung cancer (NSCLC) cell lines (A549 and H1975). Among the synthesized compounds, the iodo compound 6 (ETN-6) exhibits higher anti-cancer activity compared to erlotinib. An efficient method is developed for the conjugation of erlotinib analogue-4, alcohol compound, with protein, bovine serum albumin (BSA), via succinic acid linker. The in vitro anti-tumor activity of the protein attached erlotinib analogue, 8 (ETN-4-Suc-BSA), showed stronger inhibitory activity in both A549 and H1975 NSCLC cell lines.
- Boobalan, Ramalingam,Liu, Kuang-Kai,Chao, Jui-I.,Chen, Chinpiao
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supporting information
p. 1784 - 1788
(2017/04/04)
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- Further insights into the chemistry of niobium and tantalum pentahalides with 1,2-dialkoxyalkanes: Synthesis of bromo- and iodoalkoxides, spectroscopic and computational studies
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The room temperature reactions of a series of 1,2-dialkoxyalkanes ROCH 2CH(R′)OR′′ with MX5 (M = Nb, Ta; X = Br, I) in 1:1 ratio result in single C-O bond cleavage and high-yield formation of the halo-alkoxides MBr4[κ2-OCH 2CH(R′)OR′′] or [NbI4{κ 1-OCH2CH(R′)OR′′}]2, and equimolar amounts of the corresponding alkyl halides RX. The reaction of NbBr5 with 1,2-dimethoxyethane, dme, proceeds with preliminary formation of the ionic species [NbBr4(κ2-dme) (κ1-dme)][NbBr6], 3b, which has been identified by solution NMR at low temperature and conductivity analyses. The gas-phase structure of 3b has been optimized by DFT calculations, confirming that the dme ligands adopt bidentate and monodentate coordination, respectively. Although the formation of NbOBr3(dme), 4b, 1,4-dioxane and MeBr from NbBr 5/dme (ratio 1:2) is an exoergonic process (calculated ΔGr° = -115.96 kcal mol-1), it is inhibited at room temperature. High temperature conditions enhance the production of 1,4-dioxane at the expense of selectivity. The dinuclear species NbOBr3(dme)NbBr5 (Nb-O-Nb), 5b, (X-ray) has been isolated in modest yield as byproduct of the room temperature reaction of NbBr5 with dme. In general, the 1:2 molar reactions of NbX5 (X = Br, I) with ROCH2CH(R′) OR′′ occur with the exclusion of nearly one equivalent of organic reactant.
- Bini, Riccardo,Marchetti, Fabio,Pampaloni, Guido,Zacchini, Stefano
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experimental part
p. 1412 - 1419
(2011/06/22)
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- A systematic study on the activation of simple polyethers by MoCl 5 and WCl6
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MoCl5, 1a, and WCl6, 1b, activate 1,3-dioxolane at room temperature in chlorinated solvents: the compound [MoOCl 3{OC(H)OCH2CH2Cl}]2, 2, has been isolated from MoCl5/dioxolane. The mixed oxo-chloro species WOCl 4, 1c, reacts with 1,3-dioxolane, selectively giving the coordination adduct WOCl4(κ1-C3H6O 2), 3. Dimethoxymethane, CH2(OMe)2, undergoes activation including C-H bond cleavage when reacted with 1a to give the molybdenum complexes [MoOCl3{OC(H)OMe}]2, 4, and Mo 2Cl5(OMe)5, 5. The reactions of 1b with CH 2(OR)2 (R = Me, Et) proceed via O-abstraction with formation of the oxo-derivatives WOCl4[O(R)CH2Cl] (R = Me, 6a; R = Et, 6b) in admixture with equimolar amounts of RCl. The reactions of 1a,b with CMe2(OMe)2 lead to mesityl oxide, MeC(O)CHC(Me)2. A series of simple diethers of general formula ROCH2(CHR′)OR′′ are activated by 1a,b in CDCl 3, usually via cleavage of C-O bonds at high temperature. The complex WCl5(OCH2CH2OMe), 7, has been detected in solution as an intermediate species in the course of the degradation of 1,2-dimethoxyethane (dme) by 1b. The activation of CH(OMe)3 by 1 is limited to C-O bonds and selectively gives methyl chloride and methylformate, which has been found coordinated in WOCl4[OC(H)OMe], 8. The organic fragments produced in the reactions have been detected by GC-MS and NMR analyses, upon hydrolysis of the reaction mixtures. Compounds 2 and 5, which have had their molecular structures ascertained by X-ray diffraction, represent rare examples of crystallographically-characterized dinuclear Mo(v) species containing both halides and oxygen ligands.
- Dolci, Sara,Marchetti, Fabio,Pampaloni, Guido,Zacchini, Stefano
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experimental part
p. 5367 - 5376
(2010/08/04)
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- EFFICIENT AND/OR SELECTIVE METHYLATION BY DIAZOMETHANE OF ALCOHOLS, HALO ALCOHOLS, GLYCOLS, AMINO ALCOHOLS AND MERCAPTO ALCOHOLS WITH THE USE OF A PROTON-EXCHANGED X-TYPE ZEOLITE AS AN ACID-BASE BIFUNCTIONAL CATALYST
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Reactions of diazomethane with butanol, allyl alcohol and β- and γ-halo alcohols led to efficient methylation (giving the corresponding methyl ethers) with the use of a proton-excahnged X-type zeolite compared with H2SO4.The reactions with propylene and isobutylene glycols using the zeolite provided regioselective methylation of the primary OH rather than the secondary or tertiary OH, whereas regioselectivity was not observed in the reactions using H2SO4.The reactions with 2-aminoethanol and 2-mercaptoethanol showed high chemoselective S-methylation and N-monomethylation, respectively, in the presence of the zeolite instead of H2SO4.The mechanism for the reactions is proposed to involve acid-base bifunctional catalysis of the zeolite in which the acidic site reacts with diazomethane to form its conjugate acid, and the nucleophilicity of OH and SH groups is enhanced by the interaction of the basic site with the proton of the groups.
- Takeuchi, Hiroshi,Kishioka, Hiroaki,Kitajima, Kunio
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p. 121 - 126
(2007/10/02)
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- Studies on the Mechanism of the Chlorohydrination of Olefins
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We studied the rate-determining and the product-determining steps of the chlorohydrination of olefins with Cl2/H2O and HOCl.In competitive kinetic experiments with 3-ethylpent-2-ene and cyclohexene we determined the relative rate constants krel=1,5 (with Cl2/H2O) and krel=infinite (with HOCl).This shows that the rate-determining steps of the chlorohydrination with Cl2/H2O and with HOCl are different.In order to investigate the product-determining steps we determined the proportion of alkyl-(2-chloroethyl)-ethers 3 and ethylene chlorohydrine 2 in the reaction of ethylene with Cl2 and with HOCl in alcohol/water-mixtures.The proportion of both the reaction products 3/2 was independent of the chlorinating agent used.Also the proportion of MARKOVNIKOV and anti-MARKOVNIKOV products in the chlorohydrination of propylene with Cl2/H2O or HOCl was independent of the type of chlorinating agent.In the chlorohydrination of cyclohexene both agents (Cl2/H2O and HOCl) yielded only the trans-chlorohydrine.From the results obtained it may be concluded that the product-determining step of chlorohydrination is the same for both the chlorinating agents studied.
- Buss, E.,Rockstuhl, A.,Schnurpfeil, D.
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p. 197 - 208
(2007/10/02)
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- Process for preparing vicinal dialkoxyalkanes
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A process is disclosed for preparing vicinal dialkoxyalkanes by reacting a vicinal dihaloalkane with an alkanol in the presence of a hydrogen halide absorbing agent which is substantially insoluble in the alkanol.
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