- Preparation method of loratadine intermediate 3-[2-(3-chlorphenyl) ethyl]-2-pyridinecarbonitrile
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The invention provides a preparation method as shown in a formula I and a preparation method of 3-[2-(3-chlorphenyl) ethyl]-2-pyridinecarbonitrile. The invention provides a novel method for preparing a loratadine intermediate.
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- Preparation method of loratadine intermediate
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The invention provides a preparation method of a loratadine intermediate, and belongs to the technical field of chemical medicine preparation. The preparation method comprises the following steps: by taking trimethyl-2-cyanopyridine as an initial synthesis raw material, protecting cyano by tert-butyl alcohol to obtain an intermediate 2, performing nucleophilic substitution on the intermediate 2 and benzyl chloride to obtain an intermediate 3, performing deprotection by using phosphorus oxychloride to obtain an intermediate 4, and finally performing addition with a Grignard reagent and obtaining a key intermediate 1 of loratadine under an acidic condition.
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Paragraph 0007; 0013; 0015; 0025; 0029
(2021/04/29)
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- Preparation method of loratadine
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The invention provides a preparation method of loratadine. The method comprises the following steps: taking 2-cyano-3-methylpyridine as a raw material, and carrying out Ritter reaction, m-chlorobenzylchloride condensation, POCl3 deprotection group, Grignard reaction, cyclization and ethyl chloroformate substitution to obtain 4(8-chlorine-5, 6-dihydro-11H-benzo-[5, 6]cycloheptano[1, 2-b]pyridine-11-subunit)-1-piperidine carboxylic acid ethyl ester. According to the invention, a post-treatment process is innovated, and a new cyclization system is adopted to catalyze the reaction, so that the use of high-cost and high-toxicity strong acid is avoided, and a milder and more economical synthesis method is provided for industrial production.
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Paragraph 0029; 0046-0048
(2021/02/10)
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- Preparation process of 3-[2-(3-chlorphenyl)ethyl]-2-pyridinecarboxylic acid
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The invention provides a preparation process of 3-[2-(3-chlorphenyl)ethyl]-2-pyridinecarboxylic acid (as shown in formula II). The reaction equation is as shown in the description, wherein substituent R is hydrogen, tertiary butyl, phenyl or substituted p
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Paragraph 0037; 0040; 0041
(2016/11/14)
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- Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors:Design, synthesis, and biological data of inhibitors with improved physicochemical properties
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We recently described a promising novel class of p38 mitogen activated protein (MAP) kinase inhibitors with dibenzepinone-scaffolds. To optimize their physicochemical properties, characterized by calculated log P values and measured lipophilicity (chromatographic hydrophobicity index=CHI), we synthesized aza-analogue dibenzepinones. Here, we present the synthesis and biological data of compounds with the novel aza-dibenzepinone scaffolds. Although these aza-analogues revealed an improved aqueous solubility, introduction of nitrogen was not effective in the p38 MAPK enzyme assay.
- Karcher, Solveigh C.,Laufer, Stefan A.
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supporting information; experimental part
p. 1778 - 1782
(2010/03/01)
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- DIPEPTIDYL PEPTIDASE-IV INHIBITORS
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The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
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Page/Page column 56-57
(2008/06/13)
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- Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
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A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 Also disclosed are novel compounds of the formulas: Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
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- Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
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A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 STR1 Also disclosed are novel compounds of the formulas: STR2 Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
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- Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
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A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: STR1 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R20)(R21)(R46), and 5.3, 5.3A and 5.3B, wherein R is --N(R25)(R48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
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- Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
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A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound containing a tricyclic ring system to a biological system. In particular, the method inhibits cellular growth in a mammal such as a human being. Novel compounds of the formula: STR1 are disclosed. Also disclosed are processes for making 3-substituted compounds of Formula 4.0. Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formula 4.0.
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- Bis-benzo or benzopyrido cyclohepta piperidene, piperidylidene and piperazine compounds, compositions and methods of use
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Bis-benzo or benzopyrido piperidene, piperidylidene and piperazine compounds of the formula: STR1 and pharmaceutically acceptable salts thereof are disclosed, wherein Z represents --(C(Ra)2)m --Y--(C(Ra)2)n -- or STR2 The compounds of Formula I possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.
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- Heterocyclic n-oxide derivatives of substituted benzo[5,6]cycloheptapyridines, compositions and methods of use
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Heterocyclic N-oxide derivatives of substituted benzo[5,6]cycloheptapyridines, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.
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- 6,11-Dihydro-11-(N-substituted-4-piperidylidene)-5H-benzo(5,6)cyclohepta(1,2-B)pyridines and compositions and methods of use
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Derivatives of 6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.
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- Antihistaminic fluoro substituted benzocycloheptapyridines
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Certain benzocycloheptapyridine compounds with fluorine substitution across the exocyclic double bond are prepared and they are useful as antihistaminic agents.
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- ANTIHISTAMINIC 8-(HALO)-SUBSTITUTED 6,11-DIHYDRO-11-(4-PIPERIDYLIDENE)-5H-BENZO[5,6]CYCLOHEPTA[1,2-b]PYRIDINES
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Disclosed are 7- and/or 8-(halo or trifluoromethyl)-substituted-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridines and the pharmaceutically acceptable salts thereof, which possess antihistaminic properties with substantially no sedative properties. Methods for preparing and using the compounds and salts are described
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