反応 #11900

反応方程式

toluene

trityl candesartan cilexetil

formic acid

→

candesartan cilexetil

溶媒

methanol

反応条件

後処理

1. 1
   温度Typically, the deprotection step comprises heating
2. 2
   温度to reflux until a clear solution
3. 3
   その他is obtained
4. 4
   その他is from about 30° C. to about 90° C., preferably from about 50° C. to about 90° C.
5. 5
   その他for about 5 to about 19 hours
6. 6
   workup.WAITpreferably for about 8 to about 12 hours
7. 7
   その他Thereafter, the solvents are removed by evaporation

実験手順

Typically, the deprotection step comprises heating to reflux trityl candesartan cilexetil in methanol. Optionally, the deprotection solvent mixture further comprises an organic solvent, such as toluene, and/or an acid, such as formic acid. The cilexetil trityl candesartan is heated to reflux until a clear solution is obtained. Typically, the reaction temperature is from about 30° C. to about 90° C., preferably from about 50° C. to about 90° C., and the heating takes place for about 5 to about 19 hours, preferably for about 8 to about 12 hours. Thereafter, the solvents are removed by evaporation to obtain crude deprotected candesartan cilexetil. The solvents may be removed at a temperature of about 30° C. to about 70° C., preferably at a temperature of about 50° C., and at a reduce pressure of about 30 mbar.

出典