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HRID 11804作成日:2026年10月26日

Formic Acid → Candesartan Cilexetil

https://huagongshe.com/reaction/11804

反応式

関与物質

役割名称HCID仕込み量
反応物Formic AcidHCID 284—
反応物TolueneHCID 1140—
反応物Trityl candesartan cilexetilHCID 11029254—
溶媒MethanolHCID 887—
生成物Candesartan CilexetilHCID 2540—

反応手順

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.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07098342B2
出典データセットuspto-grants-2006_08
ORD IDord-9ddc7e8714f848aa8be681a6021447c6
出典メモuspto-grants-2006_08