- Synthesis method of 2-methoxyl-4-cyanobenzaldehyde
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The invention discloses a synthesis method of 2-methoxyl-4-cyanobenzaldehyde. The method comprises the following steps: 1, carrying out acylating chlorination on 4-methyl-3-methoxybenzoic acid servingas a raw material, and then carrying out aminolysis to
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Paragraph 0041; 0042; 0055; 0067; 0079
(2018/04/03)
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- A convenient and practical synthesis of anisoles and deuterated anisoles by palladium-catalyzed coupling reactions of aryl bromides and chlorides
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Synthesis of anisole: Aryl and heteroaryl halides undergo selective C-O cross-coupling reactions with methanol in the presence of a Pd(OAc) 2/L3 catalyst system. The corresponding ethers were obtained under mild conditions in good yields. The catalytic methodology was also used for the synthesis of labeled deuterated anisoles in good yields (see scheme). Copyright
- Gowrisankar, Saravanan,Neumann, Helfried,Beller, Matthias
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supporting information; experimental part
p. 2498 - 2502
(2012/03/27)
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- ALDOSTERONE SYNTHASE AND/OR 11β-HYDROXYLASE INHIBITORS
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The present invention provides a compound of formula (I). Said compound is inhibitor of CYP11B2 and/or CYP11B1, and thus can be employed for the treatment of a disorder or disease mediated by CYP11B2 and/or CYP11B1.
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Page/Page column 41-42
(2008/06/13)
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- Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-monocyclic arginine surrogates
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Investigations on P2-P3-heterocyclic dipeptide surrogates directed towards identification of an orally bioavailable thrombin inhibitor led us to pursue novel classes of achiral, non-covalent P1-arginine derivatives. The design, synthesis, and biological activity of inhibitors NC1-NC30 that feature three classes of monocyclic P1-arginine surrogates will be disclosed: (1) (hetero)aromatic amidines, amines and hydroxyamidines, (2) 2-aminopyrazines, and (3) 2-aminopyrimidines and 2-aminotetrahydropyrimidines.
- Reiner, John E.,Siev, Daniel V.,Araldi, Gian-Luca,Cui, Jingrong Jean,Ho, Jonathan Z.,Reddy, Komandla Malla,Mamedova, Lala,Vu, Phong H.,Lee, Kuen-Shan S.,Minami, Nathaniel K.,Gibson, Tony S.,Anderson, Susanne M.,Bradbury, Annette E.,Nolan, Thomas G.,Semple, J. Edward
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p. 1203 - 1208
(2007/10/03)
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- Thrombin inhibitors, the preparation and use thereof
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Compounds of the formula and the salts thereof with physiologically tolerated acids and the stereoisomers thereof, in which the substituents have the meanings stated in the description, are described. Also disclosed are intermediates for their preparation. The compounds are suitable for controlling diseases.
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- Thrombin inhibitors
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Thrombin inhibitors of the formula STR1 where R 1, A, B and D have the meaning indicated in the description, and intermediates for the preparation thereof are described.The compounds I are suitable for controlling diseases.
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- A novel series of selective leukotriene antagonists: Exploration and optimization of the acidic region in 1,6-disubstituted indoles and indazoles
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A systematic structure-activity exploration of the carboxylic acid region in a series of indole- or indazole-derived leukotriene antagonists 1 led to several discoveries. Use of the 3-methoxy-p-tolyl fragment (illustrated in acid 1) for connecting the indole and the acidic site provides the most potent carboxylic acids 1, tetrazoles 20, and aryl sulfonimides 21. The aryl sulfonimides are 5-500 times more potent (in vitro and/or in vivo) than the corresponding carboxylic acids 1. The o-tolyl sulfonimides such as 114 show greater oral potency than the phenyl sulfonimides at a given level of in vitro activity. Acidic keto sulfone derivatives 10 (Nu = CH(CO2CH3)SO2Ph) mimic the activity of the sulfonimides.
- Yee,Bernstein,Adams,Brown,Cronk,Hebbel,Vacek,Krell,Snyder
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p. 2437 - 2451
(2007/10/02)
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- Heterocyclic amide derivatives and pharmaceutical use
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The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R1, R2, L, X, Y, Z, A1, Q, A2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process. STR1
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- Triazine derivatives, a process for preparing the derivatives, and herbicides containing the derivatives as the effective component
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A triazine derivative represented by the general formula: STR1 wherein R1 and R2 are each an alkyl group having 1 to 4 carbon atoms, and X1 and X2 are each a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxyl group having 1 to 4 carbon atoms, or an alkylthio group having 1 to 4 carbon atoms. This invention also provides a process for efficiently preparing said triazine derivative and a herbicide containing said triazine derivative as effective component.
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