- Chiral c-KIT inhibitor drug key intermediate and preparation method thereof
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The invention relates to a preparation method of a c-KIT inhibitor shown in a formula (III), key intermediates shown in a formula (I) and a formula (II) and a preparation method of the intermediates,and definitions of substituent groups in the formula (I)
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Paragraph 0138; 0140; 0143; 0144
(2020/07/24)
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- Triazole alcohol derivative as well as preparation method and application thereof
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The invention relates to a triazole alcohol derivative as well as a preparation method and application thereof. The chemical structure of the triazole alcohol derivative is shown as a formula I, R1 represents a benzene ring or a substituted benzene ring, and substituent groups of the substituted benzene ring can be located at all positions of the benzene ring, can be mono-substituted or multi-substituted, and can be selected from a) halogen which is F and Cl; b) an electron withdrawing group which is cyano or trifluoromethyl; c ) a lower alkyl of 1-4 carbon atoms or a halogen substituted loweralkyl; and d) lower alkoxy of 1-4 carbon atoms or halogen substituted lower alkoxy. The compound of the invention has strong antifungal activity, has the advantages of low toxicity, wide antibacterial spectrum and the like, and can be used for preparing antifungal drugs.
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Paragraph 0101; 0110; 0115-0116
(2020/03/11)
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- Synthetic method for antifungal drug intermediate (2R,3S)-1-(1,2,4-triazol)-2-difluorophenyl-2,3-epoxybutane
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The invention discloses a synthetic method for an antifungal drug intermediate (2R,3S)-1-(1,2,4-triazol)-2-difluorophenyl-2,3-epoxybutane. The synthetic method comprises the following steps: (1) reacting a compound IV with a Grignard reagent to obtain a compound III; (2) employing a one-pot reaction to react the compound III with trimethylsulfoxonium iodide and 1,2,4-triazole and then react with p-toluenesulfonic acid, so as to obtain a compound II; and (3) reacting the compound II with methanesulfonyl chloride under an alkali condition to generate the target compound I, wherein the Grignard reagent is 2,4-difluorophenylmagnesium bromide or 2,5-difluorophenylmagnesium bromide, and the structural formula of the compound IV is shown in the specification. According to the synthetic route, the reaction conditions are mild and easy to control, the reaction route is simple, the related solvents in the reaction process all are common solvents, the reaction conversion rate is high, and the method possesses extremely high feasibility, is beneficial for industrialized batch production, and possesses extremely large exploitation potential and extremely good application prospect.
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Paragraph 0043; 0049; 0055; 0061; 0067
(2016/10/07)
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- Pyrazolinone deriv., producing the same herbocide agent contains, as an active component, (by machine translation)
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PROBLEM TO BE SOLVED: excellent and weed control effect, and its durability is excellent in crop-has a herbicide effect between weeds, herbicide compounds useful as an active component. SOLUTION: pyrazolinone deriv. eq. (1) shown at, its manufacturing met
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Paragraph 0076
(2017/03/28)
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- ANTIFUNGAL COMPOUND PROCESS
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The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
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Page/Page column 89
(2015/11/10)
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- ANTIFUNGAL COMPOUND PROCESS
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The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
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Page/Page column 74
(2015/11/10)
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- OPTICALLY ACTIVE HALOHYDRIN DERIVATIVE AND PROCESS FOR PRODUCING OPTICALLY ACTIVE EPOXY ALCOHOL DERIVATIVE FROM THE SAME
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The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxyalcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.
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Page/Page column 22-23
(2008/06/13)
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- Process for the preparation of 2-hydroxyalkyl halophenones
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2-Benzyloxyalkyl halophenones of the formula (3): wherein X1and X2are each independently H, Cl or F, provided that at least one of X1and X2is Cl or F; one of R3and R4is H and the other is optionally substituted benzyloxy; and R5is an unsubstituted alkyl, preferably a C1-6alkyl group. The compounds are useful as intermediates for preparing 2-hydroxyalkyl halophenones.
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- AMINOMETHYLPYRROLIDINE DERIVATIVES HAVING AROMATIC SUBSTITUENTS
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This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both. In the formula, R2, R3: hydrogen atom, an alkyl group; R4, R5, R6: hydrogen atom, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R7, R8: hydrogen atom, an alkyl group; R9: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R10: hydrogen atom, an alkylthio group; R11: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X1: halogen atom, a hydrogen atom; A1: nitrogen atom, C-X2; X2: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A2, A3:>C=C(-A1=)-N(-R9)-,>N-C(-A1=)=C(-R9)-; R10 and R9 or R9 and X2 may be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.
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- Process for the preparation of 2-hydroxyalkyl halophenones
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A process is provided for the preparation of compounds of Formula (1): wherein X1and X2are each independently H, Cl or F, provided that at least one of X1and X2is Cl or F; one of R1and R2is H and the other is OH; and R5is an unsubstituted alkyl, preferably a C1-6alkyl, group. The process comprises condensing a 2-chloroalkanoic acid with an optionally substituted benzyl alcohol to form a 2-(optionally substituted benzyloxy) alkanoic acid, converting the condensation product to the corresponding acid chloride and then either reacting the acid chloride with a compound of the Formula (2) in the presence of a source of copper (I) to give a compound of Formula (3) wherein one of R3and R4is H and the other is optionally substituted benzyloxy; or reacting the acid chloride with a compound of Formula (4): A—NH—B wherein A and B independently represent substituted alkyl, alkoxy, aryl or oxyaryl groups, or are linked to form a heterocyclic ring to form an amide, and then reacting the amide with a compound of Formula (2) to give a compound of Formula (3). The optionally substituted benzyl group from the compound of Formula (3) can removed by hydrogenation.
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- Triazole derivatives
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The present invention relates to a novel glycerol derivative and a process for preparing the same, and a process for preparing a triazole derivative. According to the present invention, an optical active 2-arylglycerol derivative which is a novel and useful as a synthetic intermediate of medicament can be provided and furthermore, (R)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazole-1-yl)-propane-1,2-diol which is useful as an antifungal agent can be prepared.
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