发明名称 |
SYNTHESIS OF TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY |
摘要 |
The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) with an oxidizing agent, thereby producing a compound of formula (IA). The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: (IB) or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: (HB) in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula: (IIIB). |
申请公布号 |
WO2007139952(A2) |
申请公布日期 |
2007.12.06 |
申请号 |
WO2007US12520 |
申请日期 |
2007.05.25 |
申请人 |
SYNTA PHARMACEUTICALS CORP.;LEE, CHI-WAN;JAMES, DAVID;ZHANG, SHIJIE;YING, WEIWEN;CHIMMANAMADA, DINESH, U.;CHAE, JUNGHYUN;PRZEWLOKA, TERESA |
发明人 |
LEE, CHI-WAN;JAMES, DAVID;ZHANG, SHIJIE;YING, WEIWEN;CHIMMANAMADA, DINESH, U.;CHAE, JUNGHYUN;PRZEWLOKA, TERESA |
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