Chemistry:SB-245570

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SB-245570 is a serotonin 5-HT1B receptor antagonist which was under development for the treatment of major depressive disorder but was never marketed.[1][2][3][4] It was being developed by GlaxoSmithKline in the 1990s.[1][2][3] A chemical synthesis for SB-245570 has been published.[3][4] The drug reached the preclinical research stage of development prior to the discontinuation of its development.[1][2]

See also

References

  1. ↑ 1.0 1.1 1.2 "SB 245570". 12 January 2000. https://adisinsight.springer.com/drugs/800010350. 
  2. ↑ 2.0 2.1 2.2 "Delving into the Latest Updates on SB-245570 with Synapse". 23 January 2025. https://synapse.patsnap.com/drug/4d344c66398f4a27855c7b3eae916dba. 
  3. ↑ 3.0 3.1 3.2 "Selected Applications of Transition Metal-Catalyzed Carbon–Carbon Cross-Coupling Reactions in the Pharmaceutical Industry". Applications of Transition Metal Catalysis in Drug Discovery and Development: An Industrial Perspective. Wiley. 22 June 2012. p. 48. doi:10.1002/9781118309872. ISBN 978-0-470-63132-4. https://www.people.uniurb.it/GiovanniPiersanti/organica2/Lectures/10_Applications%20of%20transition%20metal%20catalysis%20in%20drug%20discovery%20and%20development%20-%20an%20industrial%20perspective.pdf#page=42. "Another example of biaryl Suzuki coupling was reported by GSK in the synthesis of SB-245570 (4), a compound in development for the treatment of depression (Scheme 2.3) [45]. [...] SCHEME 2.3 GSK’s synthesis of SB-245570 via a Suzuki coupling." 
  4. ↑ 4.0 4.1 "Development of a Catalytic Tributyltin Hydride Cyclisation Process". Organic Process Research & Development 4 (2): 98–101. 1 March 2000. doi:10.1021/op9900941. ISSN 1083-6160. "The spirocyclic indoline 21 is a key intermediate in the preparation of SB-245570 3, a 5HT1B autoreceptor antagonist, indicated for the treatment of depression. SB-245570 3 was prepared by the carbonyl diimidazole coupling of the spirocycle 2 with the biphenylcarboxylic acid 11 (Scheme 1).". 





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