Comment
Author: Admin | 2025-04-28
Tandospirone.[55]A number of analogues are recorded.[56]A number of methods of synthesis have also been reported.[57][58][59] One method begins with alkylation of 1-(2-pyrimidyl)piperazine (1) with 3-chloro-1-cyanopropane (4-chlorobutyronitrile) (2) to give (3). Next, reduction of the nitrile group is performed either by catalytic hydrogenation or with lithium aluminium hydride (LAH) giving (4). The primary amine is then reacted with 3,3-tetramethyleneglutaric anhydride (5) in order to yield buspirone (6).[60][61][62][63][64]Synthesis of buspirone Buspirone was first synthesized by a team at Mead Johnson in 1968[22] but was not patented until 1980.[65][60][66] It was initially developed as an antipsychotic acting on the D2 receptor but was found to be ineffective in the treatment of psychosis; it was then used as an anxiolytic instead.[3] In 1986, Bristol-Myers Squibb gained FDA approval for buspirone in the treatment of GAD.[22][67] The patent expired in 2001, and buspirone is now available as a generic drug.Society and culture[edit]Buspar (buspirone) 10-mg tabletsBuspirone is the INNTooltip International Nonproprietary Name, BANTooltip British Approved Name, DCFTooltip Dénomination Commune Française, and DCITTooltip Denominazione Comune Italiana of buspirone, while buspirone hydrochloride is its USANTooltip United States Adopted Name, BANMTooltip British Approved Name, and JANTooltip Japanese Accepted Name.[1][68][69][70]Buspirone was primarily sold under the brand name Buspar.[68][70] Buspar is currently listed as discontinued by the U.S. Food and Drug Administration (FDA).[71] In 2010, in response to a citizen petition, the FDA determined that Buspar was not withdrawn from sale for reasons of safety or effectiveness.[72]^ a b Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 192–. ISBN 978-1-4757-2085-3.^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.^ a b c d e f g h i j k l m n o p Loane C, Politis M (June 2012). "Buspirone: what is it all about?". Brain Research. 1461: 111–118. doi:10.1016/j.brainres.2012.04.032. PMID 22608068. S2CID 11734819.^ a b c "buspirone (Rx) - BuSpar, Buspirex, more." Medscape Reference. WebMD. Retrieved 14 November 2013.^ a b c Gammans RE, Mayol RF, LaBudde JA (March 1986). "Metabolism and disposition of buspirone". The American Journal of Medicine. 80 (3B): 41–51. doi:10.1016/0002-9343(86)90331-1. PMID 3515929.^ a b
Add Comment