Clinical data | |
---|---|
ATC code |
|
Identifiers | |
IUPAC name
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
ChEMBL | |
CompTox Dashboard (EPA) | |
Chemical and physical data | |
Formula | C18H25N3O3 |
Molar mass | 331.416 g·mol |
3D model (JSmol) | |
SMILES
| |
InChI
| |
(what is this?) (verify) |
Azaloxan (CGS-7135A) is a drug which was patented as an antidepressant by Ciba-Geigy in the early 1980s, but was never marketed.
Synthesis
Thymoleptic described as a “psychostimulant” according to patent title.
The halogenation of allyl cyanide (1) with bromine gives 3,4-dibromobutyronitrile (2). This is further reacted with catechol (3) to give the 1,4-benzodioxan-2-yl-acetonitrile (4). Acid catalyzed hydrolysis of the nitrile to the acid gives 1,4-benzodioxan-2-yl-acetic acid (5). The reduction of this to alcohol with sodium bis(2-methoxyethoxy)aluminium hydride gives 2-(1,4-benzodioxan-2-yl)ethanol (6). The tosylation of this intermediate gives CID:12850582 (7). The synthesis concludes with an SN-2 displacement reaction with 1-(4-piperidinyl)-2-imidazolidinone (8) completing the synthesis of Azaloxan (9).
See also
References
- Triggle DJ (1997). Dictionary of pharmacological agents. London: Chapman & Hall. ISBN 0-412-46630-9.
- Charles F. Huebner, U.S. patent 4,329,348 (1982 to Ciba-Geigy Corporation).