- Method for preparing anti-allergic rhinitis medicine loratadine intermediate
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The invention belongs to the technical field of chemical medicine preparation and particularly relates to a method for preparing an anti-allergic rhinitis medicine, namely a loratadine intermediate. According to the method, ammonium meta-tungstate is adopted as a WO3 precursor, ZrOC12*8H2O is adopted as a ZrO2 precursor, and a WO3/ZrO2 solid super-strong acid is supported by sulfamic acid graftingmodified silica gel, and then a silica gel supported solid acid is prepared. As 8-chlorine-5,6-dihydro-11H-benzo[5,6] cycloheptane[1,2-b] pyridine-11-ketone is prepared from the novel silica gel supported solid acid through catalysis, the problem of excessive wastewater is overcome, the environment protection burden is alleviated, and the reaction yield can be increased.
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Paragraph 0056-0092
(2018/07/30)
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- Ozonolysis of some 8-alkoxyquinolines, and synthesis of a precursor to the non-sedating antihistamine Claritin
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3-Formyl-2-methoxycarbonylpyridine and isopropyl 3-formylpyridine-2-carboxylate have each been efficiently accessed in one step via the ozonolyses of 8-methoxy- or of 8-isopropoxyquinoline under near-ambient conditions. The compounds can be utilized as intermediates for syntheses of the tricyclic ketone 8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-one, a precursor to the important non-sedating antihistamine Claritin.
- Eichler, Mathias C.,Grayson, David H.
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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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- A PROCESS FOR PREPARING BENZOCYCLOHETAPYRIDIN-11-ONES
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A process for the preparation of benzocydoheptapyridin-11-ones of the general formula (III) wherein R1, R2, R3, R4, R5, R6 and R7 are independently selected from one or more of the following groups: hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, which comprises a) reacting a compound of general formula (I), wherein R1, R2, R3, R4, R5, R6 and R7are as defined above, with anhydrous HF/BF3 at a temperature in the range of -100°C to -20°C, to produce a compound of formula (II), wherein R1, R2 R3, R4, R5, R6and R7 are as defined above; and hydrolysing it to compound of formula (III).
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- A PROCESS FOR PREPARING BENZOCYCLOHEPTAPYRIDIN-11-ONES
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A novel method for generating dianions using 3-methylpyridine-2-carboxylic acid derivatives of formula (V) or using their corresponding alkali metal salts of formula (VI), preferably from their lithium salt (Scheme 3) is described. The substituents R, R, R, R, R, R and R in Scheme 3 are defined as herein described above. Preferably the substituents are selected from one or more of hydrogen, halogen or C1-C6 alkyl groups. M is represented by any alkali metal ion, preferably lithium.
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- PROCESS OF SYNTHESIS OF A TRICYCLIC KETONE INTERMEDIATE
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In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen, and intermediates therefor from easily available starting materials by a simple route.
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- Synthesis of intermediates useful in preparing tricyclic compounds
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Disclosed is a process for preparing a compound having the formula: wherein R, R1, R2, R3, and R4are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy, by (A) reacting a compound having the formula ?wherein RA, RC, RD, and REare independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5is aryl or heteroaryl, with a dehydrating agent to produce an imine having the formula: (B) hydrolyzing the imine produced in step (A) to produce the compound having formula (I). Also disclosed are novel intermediates having the formula: ?wherein RA, RB, RC, RD, and REare independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5is aryl or heteroaryl. Also disclosed is a process for preparing a compound having the formula: ?comprising: reacting a compound having the formula: ?with NH2R5in the presence of a palladium catalyst, carbon monoxide, a base, and an ether selected from the group consisting of: CH3OCH2CH2OCH3; CH3OCH2CH2OCH2CH2OCH3; and CH3OCH2CH2OCH2CH2OCH2CH2OCH3, wherein X is H, Br, Cl, or F, and R5is aryl or heteroaryl. The compounds made by these processes are useful intermediates for preparing compounds that are antihistamines or inhibitors of farnesyl protein transferase.
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- Farnesyl protein transferase inhibitors
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Disclosed are compounds of the formula: wherein R8represents a cyclic moiety to which is bound an imodazolylalkyl group; R9represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
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- An anion-induced regio- and chemoselective acylation and its application to the synthesis of an anticancer agent
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Figure presented An efficient Grignard- and organolithium-induced regio- and chemoselective anionic acylation is reported. A number of tricyclic ketones are prepared in good to excellent yields via this method. This method is complementary to the Frieldel-Crafts acylation for electron-deficient substrates. A novel anisole-based Grignard reagent was developed to effect the cyclization of sterically hindered substrates. This novel reagent has been successfully applied to the synthesis of Sch 66336, a candidate for oncologic treatment.
- Poirier, Marc,Chen, Frank,Bernard, Charles,Wong, Yee-Shing,Wu, George G.
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p. 3795 - 3798
(2007/10/03)
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