- 2-METHYL-QUINAZOLINES
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The present invention describes 2-methyl-quinazoline compounds of general formula (I), methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions. The 2-methyl substituted quinazoline compounds of general formula(I) effectively and selectively inhibit the Ras-Sos interaction without significantly targeting the EGFR receptor. They are therefore useful for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, such as cancer as a sole agent or in combination with other active ingredients.
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Page/Page column 109
(2018/10/19)
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- TETRAZOLINONE COMPOUND AND USE THEREOF
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The compound represented by formula (1): wherein R4 and R5 each represents a hydrogen atom, a halogen atom, or a C1-C3 alkyl group; R6 represents a C1-C4 alkyl group, a C3-C6 cycloalkyl group, or the like; R7, R8, and R9 each represents a hydrogen atom, a halogen atom, or the like; R10 represents a C1-C3 alkyl group, or the like; R13 represents a C1-C3 alkyl group, or the like; and Q represents a phenyl group, or the like; has an excellent control effect on pests.
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Paragraph 0847; 0867
(2015/11/16)
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- Selective catalytic hydrogenation of polycyclic aromatic hydrocarbons promoted by ruthenium nanoparticles
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Ru nanoparticles stabilised by PPh3 are efficient catalysts for hydrogenation of polycyclic aromatic hydrocarbons (PAHs) containing 2-4 rings under mild reaction conditions. These compounds were partially hydrogenated with good to excellent selectivities just by optimizing the reaction conditions. The influence of the nature of substituents present in different positions of naphthalene on the selectivity of hydrogenation was also studied. Hydrogenation of products containing substituents at position 1 is slower than that of products containing substituents at position 2. In all cases, hydrogenation takes place mainly on the less substituted ring.
- Bresó-Femenia, Emma,Chaudret, Bruno,Castillón, Sergio
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p. 2741 - 2751
(2015/05/27)
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- Efficient synthesis of substances related to cinacalcet hydrochloride via heck coupling
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Efficient synthetic methods to process substances related to cinacalcet hydrochloride 1, generated during the preparation, were described. The compounds were identified as [1-(7,8-dihydro-naphthalen-1-yl)-ethyl]-[3-(3- trifluoromethyl-phenyl)-propyl]-amine hydrochloride 2,[1-(5,6,7,8-tetrahydro- naphthalen-1-yl)-ethyl]-[3-(3-trifluoromethyl-phenyl)-propyl]-amine hydrochloride 3 and [1-(naphthalen-2-yl)-ethyl]-[3-(3-trifluoromethyl-phenyl)- propyl]-amine hydrochloride 4. All were prepared from commercially available materials in several linear steps and characterized by their respective spectral data.
- Lei, Fan,Qu, Boyi,Li, Xiaolong,Guo, Li,Guan, Mei,Hai, Li,Jin, Hui,Wu, Yong
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p. 2879 - 2885
(2014/09/29)
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- Annulation of aromatic imines via directed C-H bond activation
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A directed C-H bond activation approach to the synthesis of indans, tetralins, dihydrofurans, dihydroindoles, and other polycyclic aromatic compounds is presented. Cyclization of aromatic ketimines and aldimines containing alkenyl groups tethered at the meta position relative to the imine directing group has been achieved using (PPh3)3RhCl (Wilkinson's catalyst). The cyclization of a range of aromatic ketimines and aldimines provides bi- and tricyclic ring systems with good regioselectivity. Different ring sizes and substitution patterns can be accessed through the coupling of monosubstituted, 1,1- or 1,2-disubstituted, and trisubstituted alkenes bearing both electron-rich and electron-deficient functionality.
- Thalji, Reema K.,Ahrendt, Kateri A.,Bergman, Robert G.,Ellman, Jonathan A.
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p. 6775 - 6781
(2007/10/03)
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- Aromatic alkenylation using electrophilic organogallium reagent generated from allenylsilane and GaCl3
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Aromatic hydrocarbons are alkenylated with silylallene in the presence of GaCl3 at -90°C. Organometallic electrophiles generated from the allene and GaCl3 are the active species in this reaction. A modest level of ortho-selectivity is observed. While the silylallene reacts exclusively at the 2-position, 1,2-alkadiene reacts at the 1-position predominantly.
- Kido, Yoshiyuki,Yonehara, Fumi,Yamaguchi, Masahiko
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p. 827 - 833
(2007/10/03)
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- 188. Addition of Carbon Nucleophiles to Tricarbonylchromium Complexes of 1,2-Dihydrocyclobutabenzene, Indane, 1,2,3,4-Tetrahydronaphthalene and ortho-Xylene
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3-Substituted 1,2-dihydrocyclobutabenzenes (bicycloocta-1,3,5-triene) are readily accessible from (1) via a two-step sequence which involves addition of a nucleophile and oxidation of the intermediate anionic
- Kuendig, E. Peter,Grivet, Chantal,Wenger, Eric,Bernardinelli, Gerald,Williams, Alan F.
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p. 2009 - 2023
(2007/10/02)
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- Chemistry of the podocarpaceae LXXI. Preparation, structure, and reactions of some (arene)tricarbonylchromium(0) complexes. Crystal structure of α-tricarbonylchromium(0)
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Tricarbonylchromium(0) (7), tricarbonylchromium(0) (11) and (benzene)tricarbonylchromium(0) (10) were prepared and examined.Complex 7 was obtained as a mixture of diastereomers, an X-ray structural determination showing that the α-isomer possesses a near eclipsed conformation, in agreement with the conformation in solution deduced from 400 MHz 1H NMR analysis.Carbanions derived from 1,3-dithiane, 2-methyl-1,3-dithiane and 2-(2,2-dimethoxyethyl)-1,3-dithiane (24), and the dianion derived from 2,2'-methylenebis-1,3-dithiane (27) were prepared and brought into reaction with the complexes.Compounds 23 and 33 resulted from regioselective attack on 7 at the site predicted.Treatment with methyl electrophiles of the dithianyl η5-intermediate leading to 22 did not give products of acetyl incorporation.Arene lithiation-electrophilic quenching of 7 gave a mixture of compound 6 and its C(14) regioisomer along with the novel ketone 39 and its C(14) regioisomer.
- Cambie, Richard C.,Clark, George R.,Gallagher, Stewart R.,Rutledge, Peter S.,Stone, Martin J.,Woodgate, Paul D.
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p. 315 - 338
(2007/10/02)
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