- Preparation method of 4-methylpiperidine salt
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The invention relates to a preparation method of 4-methylpiperidine salt. According to the invention, 1,5-dihalide-3-pentanone is used as an initial raw material, through a wittig reaction, halogenated amine hydrolysis, salt forming with acid, the 4-methylpiperidine salt is obtained with high efficiency. The preparation method has the beneficial effects that the raw material source is wide, cost is low, operation is simple, a solvent is recycled and reused, the waste liquid discharge capacity is less, the product recovery rate is high, and industrialization is easily realized.
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Paragraph 0029; 0031; 0035; 0037
(2018/09/12)
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- METHOD OF PRODUCING 1-TRIAZOLE-2-BUTANOL DERIVATIVES
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PROBLEM TO BE SOLVED: To provide a novel method of producing 1-triazole-2-butanol derivatives useful as pharmaceuticals. SOLUTION: A method of producing a 1-triazole 2-butanol derivative represented by formula (1) comprises reacting a compound represented by formula (2) with 4-methylenepiperidine (3) in the presence of a metal salt (excluding lithium salts). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
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Paragraph 0036-0037
(2018/05/15)
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- Development of a Robust Process for the Preparation of High-Quality 4-Methylenepiperidine Hydrochloride
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An efficient route for the preparation of 4-methylenepiperidine hydrochloride 1 was designed, and then a process feasible for large-scale production was developed with a total yield of 83.5% at a purity of 99.9%.
- Zhu, Fuqiang,Aisa, Haji A.,Zhang, Jian,Hu, Tianwen,Sun, Changliang,He, Yang,Xie, Yuanchao,Shen, Jingshan
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- Efinaconazole preparation method
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The invention discloses an efinaconazole preparation method, wherein the chemical name of the efinaconazole is (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazole-1-yl) butane-2-ol, and the chemical formula is C18H22F2N4O. According to the present invention, the preparation process has characteristics of simple process, easily available raw materials and simple designand development, can effectively avoid the disadvantages of difficult obtaining of the raw material and the catalyst and not high yield, is suitable for industrialization, can promote the economic and technological development of efinaconazole bulk drugs, is economical and environmental protection, can reduce the production cost, and is suitable for mass production.
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Paragraph 0008; 0011-0013
(2018/09/08)
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- Preparation of a spiroisoxazolinopiperidinylbenzamide-based scaffold
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A route to spiroisoxazolinopiperidinylbenzamides has been developed. N-Boc-4-piperidone underwent a Wittig olefination and Boc-deprotection followed by a nucleophilic substitution reaction with 4-fluoro-3-nitrobenzoic acid to yield the starting scaffold 3
- Milinkevich, Kristin A.,Kurth, Mark J.
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experimental part
p. 3019 - 3023
(2010/03/05)
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- Bicyclic Benzimidazole Compounds and Their Use as Metabotropic Glutamate Receptor Potentiators
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Compounds of Formula I: wherein A, B, D, L, R1, R2, R3, R4, m, and n are as defined for Formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
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Page/Page column 66
(2009/08/14)
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- CANNABINOID RECEPTOR LIGANDS
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There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.
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Page/Page column 54
(2010/02/05)
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- Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity
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We previously reported the discovery of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1′-[(2,4-dimethyl-3 -pyridinyl)carbonyl]-4′-methyl-1,4′-bipipefidine N-oxide 1 (SCH 351125) as an orally bioavailable human CCR5 antagonist for the treatment of HIV-1 infec
- Palani, Anandan,Shapiro, Sherry,Josien, Hubert,Bara, Thomas,Clader, John W.,Greenlee, William J.,Cox, Kathleen,Strizki, Julie M.,Baroudy, Bahige M.
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p. 3143 - 3160
(2007/10/03)
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- Synthesis and antifungal activities of (2R,3R)-2-aryl-1-azolyl-3- (substituted amino)-2-butanol derivatives as topical antifungal agents
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2-Aryl-1-azolyl-3-(substituted amino)-2-butanol derivatives I were prepared by ring-opening reaction of epoxides II with excess amine, and their antifungal activities were evaluated as topical agents. Azolyl-cyclic amine derivatives with a methylene group showed extremely strong activity with a broad spectrum in vitro. In general, anti-Trichophyton mentagrophytes activities of most of the topical antifungal agents are substantially reduced by addition of keratin (a major constituent of the keratinized tissue). However, the triazole derivative (2R,3R)-2-(2,4-difluorophenyl)-3-(4- methylenepiperidino)-1-(1H-1,2,4-triazol-1-yl)-2-butanol ((-)-40, KP-103) showed very little deactivation by addition of keratin. This biological characteristic of triazole derivative (-)-40 resulted in excellent therapeutic efficacy on dermatophytosis superior to that of the corresponding imidazole derivative ((-)-41).
- Ogura, Hironobu,Kobayashi, Haruhito,Nagai, Kiyoshi,Nishida, Tokiko,Naito, Takanobu,Tatsumi, Yoshiyuki,Yokoo, Mamoru,Arika, Tadashi
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p. 1417 - 1425
(2007/10/03)
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