- USE OF A GABAA RECEPTOR ALLOSTERIC ENHANCER IN MEDICINE
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An application of a GABAA receptor allosteric enhancer in medicine. Specifically provided is use of the GABAA receptor allosteric enhancer shown in formula (I) in preparation of drugs for sedatives, hypnosis, treatment or prevention of anxiety, depression, insomnia, nausea, vomiting, migraine, schizophrenia, convulsions, and
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Paragraph 0015-0019
(2021/10/15)
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- GABAA Receptor allosteric enhancement compounds and their preparation and use
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A GABA A receptor allosteric enhancer compound and preparation and a use thereof are disclosed. The compound has a structure represented by formula (1). R 1 and R 2 are each independently selected from isopropyl and n-propyl; and when R 1 is n-propyl, R 2 is not isopropyl.
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Paragraph 0085-0086; 0092-0093
(2020/03/17)
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- Commercial manufacturing of propofol: Simplifying the isolation process and control on related substances
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A commercially viable manufacturing process for propofol (1) is described. The process avoids acid-base neutralization events during isolation of intermediate, 2,6-di-isopropylbenzoic acid (3) and crude propofol, and thus simplifies the synthesis on industrial scale to a considerable extent. Syntheses of five impurities/related substances (USP and EP) are also described.
- Pramanik, Chinmoy,Kotharkar, Sandeep,Patil, Pradip,Gotrane, Dinkar,More, Yogesh,Borhade, Ajit,Chaugule, Balaji,Khaladkar, Tushar,Neelakandan,Chaudhari, Ashok,Kulkarni, Mukund G.,Tripathy, Narendra K.,Gurjar, Mukund K.
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p. 152 - 156
(2014/05/20)
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- Alumina-Catalyzed Reactions of Hydroxyarenes and Hydroaromatic Ketones. 9. Reaction of Phenol with 1-Propanol
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At 250-350 deg C in the presence of alumina, phenol (1) reacts with excess 1-propanol to give mainly (>90percent) C-alkylation to form mono- to penta-n-propylphenols plus some O-alkylations to form n-propyl aryl ethers. The principal component of the product mixture from 1 is 2,6-di-n-propylphenol (26-50 mol percent yield). With 4-n-propylphenol as substrate (instead of 1), tri-, tetra-, and penta-n-propylphenols are formed in 48-79percent combined yield. On the average, only 3percent of the total C3H7 groups in the product mixture are isopropyl ones. Deoxygenation is not observed. It is proposed that the principal products result from an SN2-type reaction mechanism which involves nucleophilic attack (variously by C-2, C-4, C-6, or O) of an adsorbed ambident phenoxide ion onto C-1 of an adsorbed n-propoxide group. n-Propylation at C-3 and C-5 of the phenol ring results from surface-catalyzed dienone-phenol rearrangement.Isopropylation may occur via a side reaction of SN1 type.
- Klemm, LeRoy H.,Taylor, Dennis R.
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p. 4320 - 4326
(2007/10/02)
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- Synthesis, Biological Evaluation, and Preliminary Structure-Activity Considerations of a Series of Alkylphenols as Intravenous Anesthetic Agents
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Following our discovery of the intravenous (iv) anesthetic activity of 2,6-diethylphenol in mice, a series of alkylphenols was examined in this species and the most active analogues were further evaluated in rabbits.The synthesis of compounds which were not commercially available was accomplished by adaptations of standard ortho-alkylation procedures for phenols.Structure-activity relationships were found to be complex, but, in general, potency and kinetics appeared to be a function of both the lipophilic character and the degree of steric hindrance exerted by ortho substituents.The most interesting compounds were found in the 2,6-dialkyl series, and the greatest potency was associated with 2,6-di-sec-alkyl substitution.In particular, 2,6-diisopropylphenol (ICI 35868) emerged as a candidate for further development and has subsequently been shown to be an effective iv anesthetic agent in man.
- James, Roger,Glen, John B.
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p. 1350 - 1357
(2007/10/02)
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