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Osanetant Synthesis (Glaxo)
Osanetant (developmental code name SR-142,801) is a neurokinin 3 receptor antagonist which was developed by Sanofi-Synthélabo and was being researched for the treatment of schizophrenia but was discontinued. It was the first non-peptide NK3 antagonist developed in the mid-1990s. Professor David J. Anderson, Director and Leadership Chair of the Tianqiao and Chrissy Chen Institute for Neuroscience at California Institute of Technology, has advocated that osanetant be explored as a treatment for pain, anxiety, and aggression in humans and companion animals experiencing bereavement or social isolation, citing research suggesting that osanetant has an excellent safety profile and suppresses negative effects of social isolation in mice through an evolutionarily-conserved mechanism and without acting as a depressant. Another potential application for osanetant is in the treatment of drug addiction, as it has been found to block the effects of cocaine in animal models. Osanetant is ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tachykinin Receptor 3
Tachykinin receptor 3, also known as TACR3, is a protein which in humans is encoded by the ''TACR3'' gene. Function This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neurokinin 3, also referred to as neurokinin B. Selective ligands A number of selective ligands are available for NK3. NK3 receptor antagonists are being investigated as treatments for various indications. Agonists * Neurokinin B – endogenous peptide ligand, also interacts with other neurokinin receptors but has highest affinity for NK3 * Senktide – 7-amino acid polypeptide, NK3 selective, CAS# 106128-89-6 Antagonists * Elinzanetant (BAY-3427080 GSK-1144814, NT-814) * Fezolinetant (ESN-364) * Osanetant (SR-142, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trimethylsilyl Cyanide
Trimethylsilyl cyanide is the chemical compound with the formula (CH3)3SiCN. This volatile liquid consists of a cyanide group, that is CN, attached to a trimethylsilyl group. The molecule is used in organic synthesis as the equivalent of hydrogen cyanide. It is prepared by the reaction of lithium cyanide and trimethylsilyl chloride: :LiCN + (CH3)3SiCl → (CH3)3SiCN + LiCl Structure The molecule exhibits the expected structure of a nitrile-like compound. The compound exists in a facile equilibrium with a small amount of the isomeric isocyanide (CH3)3SiNC. By contrast, the nearly isostructural ''tert''-butyl nitrile does not readily isomerize to ''tert''-butyl isocyanide. Reactions Trimethylsilyl cyanide hydrolyzes to give hydrogen cyanide and trimethylsilanol: :(CH3)3SiCN + H2O → (CH3)3SiOH + HCN In its principal application, it adds across carbon-oxygen double bonds, for example in an aldehyde, to form a new carbon-carbon bond: : + (CH3)3SiC≡N → N≡C–Si(CH3)3 Th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chloroarenes
In organic chemistry, an aryl halide (also known as haloarene) is an aromatic compound in which one or more hydrogen atoms, directly bonded to an aromatic ring are replaced by a halide. The haloarene are different from haloalkanes because they exhibit many differences in methods of preparation and properties. The most important members are the aryl chlorides, but the class of compounds is so broad that there are many derivatives and applications. Preparation The two main preparatory routes to aryl halides are direct halogenation and via diazonium salts. Direct halogenation In the Friedel-Crafts halogenation, Lewis acids serve as catalysts. Many metal chlorides are used, examples include iron(III) chloride or aluminium chloride. The most important aryl halide, chlorobenzene is produced by this route. Monochlorination of benzene is always accompanied by formation of the dichlorobenzene derivatives. Arenes with electron donating groups react with halogens even in the absence of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzamides
Benzamide is a organic compound with the chemical formula of C6H5C(O)NH2. It is the simplest amide derivative of benzoic acid Benzoic acid is a white (or colorless) solid organic compound with the formula , whose structure consists of a benzene ring () with a carboxyl () substituent. It is the simplest aromatic carboxylic acid. The name is derived from gum benzoin, wh .... In powdered form, it appears as a white solid, while in crystalline form, it appears as colourless crystals. It is slightly soluble in water, and soluble in many organic solvents. It is a natural alkaloid found in the herbs of Berberis pruinosa. Chemical derivatives A number of substituted benzamides are commercial drugs, including: See also * References External links Physical characteristics {{Authority control Phenyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antipsychotics
Antipsychotics, also known as neuroleptics, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder. Prior research has shown that use of any antipsychotic is associated with smaller brain tissue volumes, including white matter reduction and that this brain shrinkage is dose dependent and time dependent. A more recent controlled trial suggests that second generation antipsychotics combined with intensive psychosocial therapy may potentially prevent pallidal brain volume loss in first episode psychosis. The use of antipsychotics may result in many unwanted side effects such as Extrapyramidal symptoms, involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acetamides
Acetamide (systematic name: ethanamide) is an organic compound with the formula CH3CONH2. It is the simplest amide derived from acetic acid. It finds some use as a plasticizer and as an industrial solvent. The related compound ''N'',''N''-dimethylacetamide (DMA) is more widely used, but it is not prepared from acetamide. Acetamide can be considered an intermediate between acetone, which has two methyl (CH3) groups either side of the carbonyl (CO), and urea which has two amide (NH2) groups in those locations. Acetamide is also a naturally occurring mineral with the IMA symbol: Ace. Production Laboratory scale Acetamide can be produced in the laboratory from ammonium acetate by dehydration: : H4CH3CO2] → CH3C(O)NH2 + H2O Alternatively acetamide can be obtained in excellent yield via ammonolysis of acetylacetone under conditions commonly used in reductive amination. It can also be made from anhydrous acetic acid, acetonitrile and very well dried hydrogen chloride gas, using a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Convergent Synthesis
In chemistry a convergent synthesis is a strategy that aims to improve the efficiency of multistep synthesis, most often in organic synthesis. In this type of synthesis several individual pieces of a complex molecule are synthesized in stage one, and then in stage two these pieces are combined to form the final product. In linear synthesis the overall yield quickly drops with each reaction step: :A → B → C → D Suppose the yield is 50% for each reaction; the overall yield of D is only 12.5% from A. In a convergent synthesis :A → B (50%) :C → D (50%) :B + D → E (25%) the overall yield of E (25%) looks much better. Convergent synthesis is applied in the synthesis of complex molecules and involves fragment coupling and independent synthesis. This technique is more useful if the compound is large and symmetric, where at least two aspects of the molecule can be formed separately and still come together. Examples: * Convergent synthesis is encountered in dendrimer s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ritter Reaction
The Ritter reaction is a chemical reaction that transforms a nitrile into an ''N''-alkyl amide using various electrophilic alkylating reagents. The original reaction formed the alkylating agent using an alkene in the presence of a strong acid. Mechanism and scope The Ritter reaction proceeds by the electrophilic addition of either a carbenium ion or covalent species to the nitrile. The resulting nitrilium ion is hydrolyzed by water to the desired amide. Primary, secondary, tertiary, and benzylic alcohols, as well as ''tert''-butyl acetate, also successfully react with nitriles in the presence of strong acids to form amides via the Ritter reaction. A wide range of nitriles can be used. In particular, formonitrile (hydrogen cyanide) can be used to prepare formamides, which are useful precursors to isocyanides. Applications The large scale application of the Ritter reaction is in the synthesis of tert-octylamine. An estimated 10,000 tons/y (year: 2000) of this and related li ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Osanetant Synthesis (Warner Lambert)
Osanetant (developmental code name SR-142,801) is a Tachykinin receptor 3, neurokinin 3 receptor receptor antagonist, antagonist which was developed by Sanofi-Synthélabo and was being researched for the treatment of schizophrenia but was discontinued. It was the first non-peptide NK3 antagonist developed in the mid-1990s. Professor David J. Anderson, Director and Leadership Chair of the Tianqiao and Chrissy Chen Institute for Neuroscience at California Institute of Technology, has advocated that osanetant be explored as a treatment for pain, anxiety, and aggression in humans and companion animals experiencing bereavement or social isolation, citing research suggesting that osanetant has an excellent safety profile and suppresses negative effects of social isolation in mice through an evolutionarily-conserved mechanism and without acting as a depressant. Another potential application for osanetant is in the treatment of drug addiction, as it has been found to block the effects o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves " '' GlaxoWellcome.'' Retrieved on December 6, 2007. They are sometimes called blockers; examples include alpha blockers, |
Borane Dimethylsulfide
Borane dimethylsulfide (BMS) is a complexed borane reagent that is used for hydroborations and reductions. The advantages of BMS over other borane reagents, such as borane-tetrahydrofuran, are its increased stability and higher solubility. BMS is commercially available at much higher concentrations than its tetrahydrofuran counterpart (10 M) and does not require sodium borohydride as a stabilizer, which could result in undesired side reactions. In contrast, borane·THF requires sodium borohydride to inhibit reduction of THF to tributyl borate. BMS is soluble in most aprotic solvents. Preparation and structure Although usually purchased, BMS can be prepared by absorbing diborane into dimethyl sulfide: :B2H6 + 2 SMe2 → 2 Me2SBH3 It can be purified by bulb to bulb vacuum transfer. Although a structure of BMS has not been determined crystallographically, (pentafluorophenyl)-borane dimethylsulfide (C6F5BH2SMe2), has been examined by X-ray crystallography. The boron center ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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