| 发明名称 | Synthesis of thiohydantoins | ||
| 摘要 | 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. | ||
| 申请公布号 | US8987452(B2) | 申请公布日期 | 2015.03.24 |
| 申请号 | US201313848477 | 申请日期 | 2013.03.21 |
| 申请人 | Sloan-Kettering Institute for Cancer Research | 发明人 | Ouerfelli Ouathek;Dilhas Anna;Yang Guangbin;Zhao Hong |
| 分类号 | C07D401/14;C07D401/04;C07C209/36;C07C213/08;C07C253/00;C07C253/30;C07D213/61;C07D213/64;C07D213/72;C07D213/74;C07D213/84 | 主分类号 | C07D401/14 |
| 代理机构 | Wolf, Greenfield & Sacks, P.C. | 代理人 | Wolf, Greenfield & Sacks, P.C. ;Baker C. Hunter;Zhang Wei |
| 主权项 | 1. A method of synthesizing a compound of formula: the method comprising: coupling a substituted pyridine of formula: with a compound of formula: in the presence of thiophosgene to provide an imidohydantoin intermediate; and hydrolyzing the imidohydantoin intermediate under suitable acidic conditions to form a product of formula: | ||
| 地址 | New York NY US | ||