Crystalline forms of an androgen receptor modulator
US-2015133481-A1 · May 14, 2015 · US
US9926291B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9926291-B2 |
| Application number | US-201615370093-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 6, 2016 |
| Priority date | Mar 27, 2007 |
| Publication date | Mar 27, 2018 |
| Grant date | Mar 27, 2018 |
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A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.
Opening claim text (preview).
What is claimed is: 1. A method of synthesizing a compound of formula: the method comprising: reacting a compound of formula: wherein R 1 is or —CN, with in the presence of a source of cyanide to provide a compound of formula: 2. The method of claim 1 , wherein R 1 is 3. The method of claim 1 , wherein R 1 is —CN. 4. The method of claim 1 , wherein the source of cyanide is NaCN. 5. The method of claim 1 , wherein the source of cyanide is KCN. 6. The method of claim 1 further comprising purifying the product of the step of reacting by recrystallization. 7. The method of claim 1 further comprising purifying the product of the step of reacting by column chromatography. 8. The method of claim 1 further comprising purifying the product of the step of reacting by distillation.
Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals · CPC title
Halogen atoms or nitro radicals · CPC title
by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups · CPC title
2-Phenoxypyridines; Derivatives thereof · CPC title
Nitriles · CPC title
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