- Preparation method of iloperidone intermediate
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The invention relates to a preparation method of an iloperidone intermediate. The preparation method comprises the following steps of (1) adding potassium hydroxide into methyl alcohol, and adding (2,4-difluorophenyl)-(4-piperidyl)ketoxime hydrochloride; (2) heating, and reacting for 2 to 3h at the controlled temperature of 50 to 60 DEG C; (3) cooling to room temperature, adding anhydrous MgSO4, stirring for 0.8 to 1.2h, sucking and filtering, and performing vacuum concentration on filtrate; (4) adding acetone, stirring for 0.4 to 0.6h at the room temperature, filtering, dripping a saturated HCl methyl alcohol solution while stirring the filtrate, so as to adjust a pH (potential of hydrogen) value to 2-3, sucking and filtering, and drying, so as to obtain a white solid, wherein the water content of methyl alcohol is less than 0.5%.
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Paragraph 0039; 0040
(2017/07/19)
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- Aralkylpiperidine (or piperazinecarboxylic) and its derivatives used for treating hypercalcemia schinzopherenia
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PROBLEM TO BE SOLVED: To provide an agent for treating schizophrenia and related neuropsychiatric diseases.SOLUTION: This invention provides an aralkylpiperidine (or piperazine) derivative represented by formula (1), where A ring is a 5-7 membered heterocycle including N, with the heterocycle including a hetero atom arbitrarily selected from O, S, N; X is O, an amino group or a substituted amino group; Z is CH, N or C; Y is O, N or S; n is an integer of 1-5; and R1-R6 are H, a C1-C4 alkyl group or the like.
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Paragraph 0088
(2018/12/01)
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- ARALKYL SUBSTITUTED PIPERIDINE OR PIPERAZINE DERIVATIVES AND THEIR USE FOR TREATING SCHIZOPHRENIA
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The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.
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- 1,2-benzisoxazole compounds
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Compounds of formula I STR1 in which m represents an integer from 0 to 5, n represents an integer from 1 to 2, p is equal to 0, 1 or 2, X, Y and Z, which may be identical or different, each represent a hydrogen atom, a halogen atom, a linear or branched alkyl radical, a trifluoromethyl radical, an alkoxy radical, an alkylthio radical or a hydroxyl radical, and R represents a 2-benzofuranyl or 2,3-dihydro-2-benzofuranyl radical (it being possible for each to be substituted on the benzene ring), a 2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b']difuran-2-yl radical, a 4-oxo-4H-chromen-2-yl radical (optionally substituted on the benzene ring), a benzocyclobutenyl radical of formula A or an indanyl radical of formula B: STR2 (in which: R1 and R2, which may be identical or different, each represent a hydrogen atom, a halogen atom, a trifluoromethyl radical, an alkyl radical, an alkoxy radical, a hydroxyl radical, a hydroxyalkyl radical or an alkylthio radical, or together form a methylenedioxy radical or an ethylenedioxy radical, and R3 represents a hydrogen atom or a linear or branched alkyl radical having 1 to 6 carbon atoms), or a radical of formula C: STR3 (in which R4, R5 and R6, which may be identical or different, each represent a hydrogen atom, a halogen atom, a trifluoromethyl radical, a hydroxyl radical, an alkyl radical, an alkoxy radical or an alkylthio radical, their optical isomers and their addition salts with a pharmaceutically acceptable organic or inorganic acid.
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