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Benzisoxazole
1,2-Benzisoxazole is an aromatic organic compound with a molecular formula C7H5NO containing a benzene-fused isoxazole ring structure. The compound itself has no common applications; however, functionalized benzisoxazoles and benzisoxazoyls have a variety of uses, including pharmaceutical drugs such as some antipsychotics (including risperidone, paliperidone, ocaperidone, and iloperidone) and the anticonvulsant zonisamide. Its aromaticity makes it relatively stable; however, it is only weakly basic. Synthesis Benzisoxazole may be prepared from inexpensive salicylaldehyde, via a base catalyzed room temperature reaction with hydroxylamine-''O''-sulfonic acid. : Reactions Kemp elimination First reported by Daniel S. Kemp, the relatively weak N-O bond can be cleaved by a strong base to yield a 2-hydroxybenzonitrile species. See also ;Structural isomers *Benzoxazole *Anthranil Anthranil (2,1-benzisoxazole) is an organic compound with a molecular formula C7H5NO, which feature ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydroxylamine-O-sulfonic Acid
Hydroxylamine-''O''-sulfonic acid (HOSA) is the inorganic compound with molecular formula H3NO4S that is formed by the sulfonation of hydroxylamine with oleum. It is a white, water-soluble and hygroscopic, solid, commonly represented by the condensed structural formula H2NOSO3H, though it actually exists as a zwitterion and thus is more accurately represented as +H3NOSO3−. It is used as a reagent for the introduction of amine groups (–NH2), for the conversion of aldehydes into nitriles and alicyclic compound, alicyclic ketones into lactams (cyclic amides), and for the synthesis of variety of nitrogen-containing heterocycles. Preparation According to a laboratory procedure hydroxylamine-''O''-sulfonic acid can be prepared by treating hydroxylamine sulfate with fuming sulfuric acid (oleum). The industrial process is similar. :(NH3OH)2SO4 + 2SO3 → 2H2NOSO3H + H2SO4 The sulfonation of hydroxylamine can also be effected with chlorosulfonic acid by a method first pub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anthranil
Anthranil (2,1-benzisoxazole) is an organic compound with a molecular formula C7H5NO, which features a fused benzene-isoxazole bicyclic ring structure. It is an isomer of the more common compounds benzoxazole and benzisoxazole, which have their oxygen atoms located in the 1-position. The locations of the heteroatoms in anthranil results in disrupted aromaticity 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 satur ..., making it by far the least stable of the 3 structural isomers. References Aromatic bases Simple aromatic rings {{heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Risperidone
Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder. It is taken either by mouth or by injection (subcutaneous or intramuscular). The injectable versions are long-acting and last for 2–4 weeks. Common side effects include extrapyramidal symptoms, movement problems, sedation, sleepiness, dizziness, trouble seeing, constipation, and increased weight. Serious side effects may include the potentially permanent movement disorder tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, and hyperglycemia, high blood sugar levels. In older people with psychosis as a result of dementia, it may increase the risk of death. It is unknown if it is safe for use in pregnancy. Its mechanism of action is not entirely clear, but is believed to be related to its action as a dopamine antagonist, dopamine and serotonin antagonist. Study of risperidone began in the late 1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Paliperidone
Paliperidone, sold under the trade name Invega among others, is an atypical antipsychotic. It is mainly used to treat schizophrenia and schizoaffective disorder. It is marketed by Janssen Pharmaceuticals. An extended release formulation is available that uses the OROS extended release system to allow for once-daily dosing. Paliperidone palmitate is a long-acting injectable formulation of paliperidone palmitoyl ester. It is on the World Health Organization's List of Essential Medicines. Medical use It is used for the treatment of schizophrenia and schizoaffective disorder. Adverse effects Sources:Joint Formulary Committee. British National Formulary (BNF) 65. Pharmaceutical Pr; 2013. ;Very Common (>10% incidence) * Headache * Tachycardia * Somnolence (causes less sedation than most atypical antipsychotics) * Insomnia * Hyperprolactinaemia (seems to cause comparable prolactin elevation to its parent drug, risperidone) * Sexual Dysfunction ;Common (1–10% incidence) * Cou ... [...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] |
Iloperidone
Iloperidone, commonly known as Fanapt and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia. Medical uses Iloperidone is indicated for the treatment of schizophrenia. In a 2013 study in a comparison of 15 antipsychotic drugs in effectivity in treating schizophrenic symptoms, iloperidone demonstrated mild effectiveness. As effective as lurasidone, and 13 to 15% less effective than ziprasidone, chlorpromazine, and asenapine. It generally appears to work better than placebo. Side effects Examination of the safety and tolerability of iloperidone have shown that at a 5 mg/day dose in healthy male volunteers, the drug was fairly well tolerated, although hypotension, dizziness, and somnolence were very common side effects ranging from mild to moderate in severity. A second study showed that co administration of food decreased the severity of these effects. This study also indicated that repeat administration of iloperidone could decr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zonisamide
Zonisamide, sold under the brand name Zonegran among others, is a medication used to treat the symptoms of epilepsy and Parkinson's disease. Chemically it is a sulfonamide. It serves as an anticonvulsant used primarily as an adjunctive therapy in adults with Parkinson's disease, partial-onset seizures; infantile spasm, mixed seizure types of Lennox–Gastaut syndrome, myoclonic and generalized tonic clonic seizure. Despite this it is also sometimes used as a monotherapy for partial-onset seizures. In 2020, it was the 276th most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses Epilepsy Zonisamide is approved in the United States, and United Kingdom for adjunctive treatment of partial seizures in adults and Japan for both adjunctive and monotherapy for partial seizures (simple, complex, secondarily generalized), generalized (tonic, tonic-clonic (grand mal), and atypical absence) and combined seizures. In Australia it is ma ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzoxazole
Benzoxazole is an aromatic organic compound with a molecular formula C7H5NO, a benzene-fused oxazole ring structure, and an odor similar to pyridine. Although benzoxazole itself is of little practical value, many derivatives of benzoxazoles are commercially important. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. Its aromaticity makes it relatively stable, although as a heterocycle, it has reactive sites which allow for functionalization. Occurrence and applications It is found within the chemical structures of pharmaceutical drugs such as flunoxaprofen and tafamidis. Benzoxazole derivatives are also of interest for optical brighteners in laundry detergents.E. Smulders, E. Sung "Laundry Detergents, 2. Ingredients and Products" in ''Ullmann's Encyclopedia of Industrial Chemistry'', Wiley-VCH, Weinheim, 2012. Benzoxazoles belong to the group of well-known antifungal agents with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aromatic
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] |
Daniel S
Daniel is a masculine given name and a surname of Hebrew origin. It means "God is my judge"Hanks, Hardcastle and Hodges, ''Oxford Dictionary of First Names'', Oxford University Press, 2nd edition, , p. 68. (cf. Gabriel—"God is my strength"), and derives from two early biblical figures, primary among them Daniel from the Book of Daniel. It is a common given name for males, and is also used as a surname. It is also the basis for various derived given names and surnames. Background The name evolved into over 100 different spellings in countries around the world. Nicknames (Dan, Danny) are common in both English and Hebrew; "Dan" may also be a complete given name rather than a nickname. The name "Daniil" (Даниил) is common in Russia. Feminine versions (Danielle, Danièle, Daniela, Daniella, Dani, Danitza) are prevalent as well. It has been particularly well-used in Ireland. The Dutch names "Daan" and "Daniël" are also variations of Daniel. A related surname developed ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aromatic Bases
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 non-benz ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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