Chemistry:Dibenzosuberenone

From HandWiki
Dibenzosuberenone
Names
Other names
5H-Dibenzo[a,d]cyclohepten-5-one
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
EC Number
  • 218-737-3
UNII
Properties
C15H10O
Molar mass 206.24 g/mol
Density g/cm3 (20°C)
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
Infobox references
Tracking categories (test):

5-Dibenzosuberenone is an organic chemical with use in drug synthesis. Chemically speaking, the structure can be described as a benzophenone moiety bonded through an ethylene bridge into a seven membered ring.[1] In contrast to dibenzosuberone, dibenzosuberenone does not contain any sp3 hybridized bonds.

Applications

Dibenzosuberenone predominantly has uses in the synthesis of tricyclic antidepressants.

Synthesis

Dibenzosuberenone is made from dibenzosuberone by dehydrogenation.[16]

In an alternative method dibenzosuberone is halogenated with NBS; dehydrohalogenation then also furnishes the target molecule.[1] In an older document molecular bromine was used under irradiation. This gave a 70-90% yield of product.[17][18]

2-Carboxybenzaldehyde [119-67-5] and hydroxyphthalide [16859-59-9] exist together in a tautomeric equilibrium. Wittig reaction to this forms predominantly (Z)-2-stilbenecarboxylic acid [66374-10-5]. It is important to mention that the Z-isomer is indeed the favored product of this step and not the trans-isomer. Cyclization of the carboxylic acid in polyphosphoric acid then also forms dibenzosuberenone.[19]

References

  1. 1.0 1.1 Dastan, A., Kilic, H., Saracoglu, N. (February 2018). "The Dibenzosuberenone Scaffold as a Privileged Substructure: From Synthesis to Application". Synthesis. 50 (03): 391–439. doi:10.1055/s-0036-1589518.
  2. Jr Robert D Hoffsommer, Taub David, Norman L Wendler, US3272864 and US3442949 (1966 to Merck and Co Inc).
  3. Chang, Meng-Yang; Huang, Yu-Ping; Lee, Tein-Wei; Chen, Yeh-Long (2012). "Synthesis of dizocilpine". Tetrahedron 68 (16): 3283–3287. doi:10.1016/j.tet.2012.03.007. 
  4. Mahesh Kandula, et al. WO2013168004 (2016 to Cellix Bio Pvt Ld).
  5. Ciganek, Engelbert; Uyeda, Roy T.; Cohen, Marvin; Smith, Dewey H. (1981). "Imine analogs of tricyclic antidepressants". Journal of Medicinal Chemistry 24 (3): 336–341. doi:10.1021/jm00135a018. PMID 7265119. 
  6. Roy Teruyuki Uyeda, US3901945 (1975 to EIDP Inc).
  7. CID 44342445 from PubChem
  8. CID 9804490 from PubChem
  9. Takahara, A.; Hirasawa, A.; Dohmoto, H.; Shoji, M.; Yoshimoto, R.; Sugiyama, A.; Hashimoto, K. (2001). "In vivo antiarrhythmic profile of AP-792 assessed in different canine arrhythmia models". Japanese Journal of Pharmacology 87 (1): 21–26. doi:10.1254/jjp.87.21. PMID 11676194. 
  10. CID 9955277 from PubChem
  11. Bernt Sigfrid Emanuel Carnmalm, et al. US3904691 (1975 to Astra Lakemedel AB).
  12. Bernt Sigfrid Emanuel Carnmalm, et al. US4053632 (1977 to Astra Lakemedel AB).
  13. CID 165241 from PubChem
  14. CID 9805663 from PubChem
  15. E Christy Marcia, GB1074081 (1967 to Merck and Co Inc).
  16. Stefan Lambrecht & Horst Surburg, WO2001016065 (to SYMRIS & Co KG GmbH, Symrise AG).
  17. Treibs, W.; Klinkhammer, H. (6 September 1951). "Über das 2.3;6.7-Dibenz-suberon-(1), II. Mitteil.Synthese des 2.3;6.7-Dibenz-suberen-(4)-ons-(1) und des 2.3;6.7-Dibenz-suberens-(4)". Chemische Berichte 84 (8): 671–679. doi:10.1002/cber.19510840804. 
  18. Hellwinkel, D.; Becker, T. (August 1989). "Transannulare Hydridverschiebung versus Cyclokondensation bei 5-(2-Biphenylyl)-10,11-dihydro-5 H -dibenzo[ a , d ]cyclohepten-5-ol-Derivaten". Chemische Berichte 122 (8): 1595–1597. doi:10.1002/cber.19891220832. 
  19. Marco Thyes & Gerd Steiner, US4857658 (1989 to BASF SE).