|
Trifluperidol
Trifluperidol is a typical antipsychotic of the butyrophenone chemical class. It has general properties similar to those of haloperidol, but is considerably more potent by weight, and causes relatively more severe side effects, especially tardive dyskinesia and other extrapyramidal effects. It is used in the treatment of psychoses including mania and schizophrenia. It was discovered at Janssen Pharmaceutica in 1959. Synthesis The Grignard reaction between 1-benzyl-4-piperidone 612-20-2(1) and 3-bromobenzotrifluoride 01-78-5(2) gives 1-benzyl-4-(3-(trifluoromethyl)phenyl)piperidin-4-olCID:12718203(3). Catalytic hydrogenation Hydrogenation is a chemical reaction between molecular hydrogen (H2) and another compound or element, usually in the presence of a catalyst such as nickel, palladium or platinum. The process is commonly employed to reduce or saturate organic ... removes the benzyl protecting group to give 4- -(trifluoromethyl)phenyl4-piperidinol 249-28-7(4). Alkyl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trifluperidol Synthesis
Trifluperidol is a typical antipsychotic of the butyrophenone chemical class. It has general properties similar to those of haloperidol, but is considerably more potent by weight, and causes relatively more severe side effects, especially tardive dyskinesia and other extrapyramidal effects. It is used in the treatment of psychoses including mania and schizophrenia. It was discovered at Janssen Pharmaceutica in 1959. Synthesis The Grignard reaction between 1-benzyl-4-piperidone 612-20-2(1) and 3-bromobenzotrifluoride 01-78-5(2) gives 1-benzyl-4-(3-(trifluoromethyl)phenyl)piperidin-4-olCID:12718203(3). Catalytic hydrogenation removes the benzyl protecting group to give 4- -(trifluoromethyl)phenyl4-piperidinol 249-28-7(4). Alkylation with 4-Chloro-4'-fluorobutyrophenone 874-54-2(5) introduces the sidechain and hence completed the synthesis of Trifluperidol (6). See also * Ocaperidone Ocaperidone (R 79598) is a benzisoxazole antipsychotic. It was initially developed by Jan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ocaperidone
Ocaperidone (R 79598) is a benzisoxazole antipsychotic. It was initially developed by Janssen, later licensed to French laboratory Neuro3D and then acquired in 2007 by German company Evotec. It was found to be more potent than risperidone in animal studies, but its testing was abandoned in 2010 after unfavorable results in human Phase II trials, as while it was effective at controlling symptoms of schizophrenia, ocaperidone produced an unacceptable amount of extrapyramidal side effects.Geerts H, Spiros A, Roberts P, Twyman R, Alphs L, Grace AA. Blinded prospective evaluation of computer-based mechanistic schizophrenia disease model for predicting drug response. ''PLoS One''. 2012;7(12):e49732. Synthesis The last step requires attachment of the sidechain between 3-(2-bromoethyl)-2,9-dimethyl 4H-pyrido ,2-ayrimidin-4-oneCID:18995805(1) and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole 4163-77-9(2) completing the convergent synthesis of Ocaperidone (3).. See also * Benperidol * ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Grignard Reaction
The Grignard reaction () is an organometallic chemical reaction in which alkyl, allyl, vinyl, or aryl-magnesium halides (Grignard reagent) is added to a carbonyl group in an aldehyde or ketone. This reaction is important for the formation of carbon–carbon bonds. The reaction of an organic halide with magnesium is ''not'' a Grignard reaction, but provides a Grignard reagent. : Grignard reactions and reagents were discovered by and are named after the French chemist François Auguste Victor Grignard ( University of Nancy, France), who published it in 1900 and was awarded the 1912 Nobel Prize in Chemistry for this work. Reaction mechanism Because carbon is more electronegative than magnesium, the carbon attached to magnesium functions as a nucleophile and attacks the electrophilic carbon atom that is present within the polar bond of a carbonyl group. The addition of the Grignard reagent to the carbonyl typically proceeds through a six-membered ring transition state. Based ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Butyrophenone Antipsychotics
Butyrophenone is an organic compound with the formula C6H5C(O)C3H7. It is a colorless liquid. The butyrophenone structure—a ketone flanked by a phenyl ring and a butyl chain—forms the basis for many other chemicals containing various substituents. Some of these butyrophenones are used to treat various psychiatric disorders such as schizophrenia, as well as acting as antiemetics. Examples of butyrophenone-derived pharmaceuticals include: * Haloperidol, the most widely used classical antipsychotic drug in this class * Benperidol, the most potent commonly used antipsychotic (200 times more potent than chlorpromazine) * Droperidol, Antiemetic An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer. They may b ... for postoperative nausea and vomiting References Aromatic ketones Phenyl c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Belgian Inventions
Belgian may refer to: * Something of, or related to, Belgium * Belgians, people from Belgium or of Belgian descent * Languages of Belgium, languages spoken in Belgium, such as Dutch, French, and German *Ancient Belgian language, an extinct language formerly spoken in Gallia Belgica *Belgian Dutch or Flemish, a variant of Dutch *Belgian French, a variant of French *Belgian horse (other), various breeds of horse *Belgian waffle, in culinary contexts * SS ''Belgian'', a cargo ship in service with F Leyland & Co Ltd from 1919 to 1934 *''The Belgian'', a 1917 American silent film See also * *Belgica (other) Gallia Belgica was a province of the Roman Empire in present-day Belgium, Luxembourg, and the Netherlands. Belgica may also refer to: Places * Belgica Glacier, Antarctica * Belgica Guyot, an undersea tablemount off Antarctica * Belgica Mounta ... * Belgic (other) {{Disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aromatic Ketones
In chemistry, aromaticity is a chemical property of cyclic ( ring-shaped), ''typically'' planar (flat) molecular structures with pi bonds in resonance (those containing delocalized electrons) that gives increased stability compared to saturated compounds having single bonds, and other geometric or connective non-cyclic arrangements with the same set of atoms. Aromatic rings are very stable and do not break apart easily. Organic compounds that are not aromatic are classified as aliphatic compounds—they might be cyclic, but only aromatic rings have enhanced stability. The term ''aromaticity'' with this meaning is historically related to the concept of having an aroma, but is a distinct property from that meaning. Since the most common aromatic compounds are derivatives of benzene (an aromatic hydrocarbon common in petroleum and its distillates), the word ''aromatic'' occasionally refers informally to benzene derivatives, and so it was first defined. Nevertheless, many ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tertiary Alcohols
In chemistry, an alcohol is a type of organic compound that carries at least one hydroxyl () functional group bound to a saturated carbon atom. The term ''alcohol'' originally referred to the primary alcohol ethanol (ethyl alcohol), which is used as a drug and is the main alcohol present in alcoholic drinks. An important class of alcohols, of which methanol and ethanol are the simplest examples, includes all compounds which conform to the general formula . Simple monoalcohols that are the subject of this article include primary (), secondary () and tertiary () alcohols. The suffix ''-ol'' appears in the IUPAC chemical name of all substances where the hydroxyl group is the functional group with the highest priority. When a higher priority group is present in the compound, the prefix ''hydroxy-'' is used in its IUPAC name. The suffix ''-ol'' in non-IUPAC names (such as paracetamol or cholesterol) also typically indicates that the substance is an alcohol. However, some comp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Catalytic Hydrogenation
Hydrogenation is a chemical reaction between molecular hydrogen (H2) and another compound or element, usually in the presence of a catalyst such as nickel, palladium or platinum. The process is commonly employed to reduce or saturate organic compounds. Hydrogenation typically constitutes the addition of pairs of hydrogen atoms to a molecule, often an alkene. Catalysts are required for the reaction to be usable; non-catalytic hydrogenation takes place only at very high temperatures. Hydrogenation reduces double and triple bonds in hydrocarbons. Process Hydrogenation has three components, the unsaturated substrate, the hydrogen (or hydrogen source) and, invariably, a catalyst. The reduction reaction is carried out at different temperatures and pressures depending upon the substrate and the activity of the catalyst. Related or competing reactions The same catalysts and conditions that are used for hydrogenation reactions can also lead to isomerization of the alkenes from ci ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Typical Antipsychotic
Typical antipsychotics (also known as major tranquilizers, and first generation antipsychotics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia). Typical antipsychotics may also be used for the treatment of acute mania, agitation, and other conditions. The first typical antipsychotics to come into medical use were the phenothiazines, namely chlorpromazine which was discovered serendipitously. Another prominent grouping of antipsychotics are the butyrophenones, an example of which is haloperidol. The newer, second-generation antipsychotics, also known as atypical antipsychotics, have largely supplanted the use of typical antipsychotics as first-line agents due to the higher risk of movement disorders in the latter. Both generations of medication tend to block receptors in the brain's dopamine pathways, but atypicals at the time of marketing were claimed to differ from typical antipsychotics in that they ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Butyrophenone
Butyrophenone is an organic compound with the formula C6H5C(O)C3H7. It is a colorless liquid. The butyrophenone structure—a ketone flanked by a phenyl ring and a butyl chain—forms the basis for many other chemicals containing various substituents. Some of these butyrophenones are used to treat various psychiatric disorders such as schizophrenia, as well as acting as antiemetics. Examples of butyrophenone-derived pharmaceuticals include: * Haloperidol, the most widely used classical antipsychotic drug in this class * Benperidol, the most potent commonly used antipsychotic (200 times more potent than chlorpromazine) * Droperidol, Antiemetic An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer. They may b ... for postoperative nausea and vomiting References Aromatic ketones Phenyl c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Janssen Pharmaceutica
Janssen Pharmaceuticals is a pharmaceutical company headquartered in Beerse, Belgium, and wholly-owned by Johnson & Johnson. It was founded in 1953 by Paul Janssen. In 1961, Janssen Pharmaceuticals was purchased by New Jersey-based American corporation Johnson & Johnson, and became part of Johnson & Johnson Pharmaceutical Research and Development (J&J PRD), now renamed to Janssen Research and Development (JRD), which conducts research and development activities related to a wide range of human medical disorders, including mental illness, neurological disorders, anesthesia and analgesia, gastrointestinal disorders, fungal infection, HIV/AIDS, allergies and cancer. Janssen and Ortho-McNeil Pharmaceutical have been placed in the Ortho-McNeil-Janssen group within Johnson & Johnson Company. Subsidiaries * Actelion * Cilag AG * Janssen Biotech (formerly ''Centocor'') * Janssen Vaccines (formerly ''Crucell'') * Tibotec * Beijing Dabao Cosmetics Co., Ltd. History The early ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
.png "Click for more on -> Aromatic Ketones")
