- Benzo-aza-alkyl aryl piperazine derivative and applications in preparation of drugs
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The invention discloses a benzo-aza-alkyl aryl piperazine derivative and applications in preparation of drugs. The derivative shows the effect on central nervous systems, especially on the double highaffinity activity of a 5-HT acceptor and a Sigma-1 acceptor. Various physiological and pharmacological effects are brought into play in the body; and the compound can be used as a pharmaceuticalactive substance, especially used for anti-depression, anti-anxiety, anti-bipolar affective disorder and anti-neuropathic pain, and can also be used as an intermediate to prepare other pharmaceuticalactive compounds. The compound is fast in effect and small in toxic and side effect, and can meet demands of clinical applications; and the compound is a compound or a free base or salt thereof havingthe following structural formula (IV). The structure of the compound or the free base or salt thereof is shown as the structural formula (IV).
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Paragraph 0103; 0104; 0107; 0108
(2019/02/10)
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- Preparation and characterization of primary amines by potassium borohydride-copper chloride system from nitriles
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Nitriles undergo reduction to primary amines under optimized conditions at 50 °C using 0.25 equiv of copper chloride and 3.0 equiv of potassium borohydride in 80 % isopropanol. The aromatic and aralkyl nitriles could be effectively reduced in yield ranging from 60 to 90 %.
- Jiang, Han,Hu, Jialei,Xu, Xinliang,Zhou, Yifeng
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p. 3564 - 3566
(2015/12/30)
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- 17a-HYDROXYLASE/C17,20-LYASE INHIBITORS
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The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
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- Microwave-assisted protection of primary amines as 2,5-dimethylpyrroles and their orthogonal deprotection
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Primary amines can be readily doubly protected as N-substituted 2,5-dimethylpyrroles. Although this protecting group is stable toward strong bases and nucleophiles, long reaction times are required for both the protection and deprotection steps, generally resulting in low deprotection yields. By employing microwave irradiation, protection and deprotection reaction times are dramatically reduced. Furthermore, deprotection with dilute hydrochloric acid in ethanol increases reaction yields. Diverse deprotection conditions have been developed in conjunction with microwave irradiation, so that protection as an N-substituted 2,5-dimethylpyrrole can be orthogonal to other standard amine protecting groups, such as tert-butyloxycarbonyl (Boc), carbobenzyloxy (Cbz), and 9-fluorenylmethyloxycarbonyl (Fmoc).
- Walia, Amit,Kang, Soosung,Silverman, Richard B
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p. 10931 - 10937
(2013/11/19)
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- 17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
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The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
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Page/Page column 108-109
(2012/04/04)
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- HETEROCYCLIC DERIVATIVES AS MODULATORS OF ION CHANNELS
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The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
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Page/Page column 27-28
(2009/05/28)
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- Mild and selective deprotection of carbamates with Bu4NF
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A new mild method allowing the removal of carbamates using TBAF in THF is reported. Reactions were performed on indole, indoline, N-methyl aniline, aniline and tryptamine derivatives. The observed selectivity according to the carbamates or the substrates is discussed. A mechanism is postulated. Graphical Abstract
- Jacquemard, Ulrich,Bénéteau, Valérie,Lefoix, Myriam,Routier, Sylvain,Mérour, Jean-Yves,Coudert, Gérard
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p. 10039 - 10047
(2007/10/03)
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- A mild and selective method for N-Boc deprotection
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A new mild method to remove N-tert-butyloxycarbonyl groups using TBAF in refluxing THF is reported. In all cases, the corresponding N-free products are obtained in good yields. The reactions are selective for acid- and base-sensitive groups, such as tert-butyl and alkyl esters, aldehydes.
- Routier, Sylvain,Saugé, Laurence,Ayerbe, Nathalie,Coudert, Gérard,Mérour, Jean-Yves
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p. 589 - 591
(2007/10/03)
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- Cholecystokinin Peptidomimetics as Selective CCK-B Antagonists: Design, Synthesis, and in Vitro and in Vivo Biochemical Properties
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Antagonists of cholecystokinin-B (CCK-B) receptors have been shown to alleviate CCK4-induced panic attacks in humans and to potentiate opioid effects in animals.The clinical use of these compounds is critically dependent on their ability to cross the blood-brain barrier.In order to improve this property, new, peptoid-derived CCK-B antagonists, endowed with high affinity, selectivity, and increased lipophilicity have been developed.The affinity and selectivity of these compounds have been cheracterized in vitro and in vivo using guinea pig, rat, and mouse.Most of these compounds proved to be selective for the CCK-B receptor, the most potent analog, N--D-α-methyltryptophanyl>-N-i value of 6.1 nM for guinea pig cortex membranes in vitro and a good selectivity ratio (Ki CCK-A/Ki CCK-B = 174).Furthermore, the in vivo affinity of 26A for mouse brain CCK-B receptors, following intracerebroventricular injection at different concentrations, was found to be 10 nmol.Using competition experiments with the specific CCK-B ligand pBC 264, compound 26A was shown to cross the blood-brain barrier (0.2percent) after intraperitoneal administration in mice.This compound is therefore an interesting pharmacological tool to further elucidate the physicopathological role of endogenous CCK.
- Blommaert, Armand G.S.,Weng Jian-Hui,Dorville, Agnes,McCort, Isabelle,Ducos, Bertrand,et al.
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p. 2868 - 2877
(2007/10/02)
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