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HRID 2038656作成日:2026年10月26日

Triethylamine → 3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-(2-oxo-tetrahydro-pyrimidin-1-ylmethyl)-benzamide

https://huagongshe.com/reaction/2038656

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Di(succinimido) carbonateHCID 676246—
反応物5-[(3-amino-propylamino)-methyl]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-benzamideHCID 59347991—
溶媒Acetonitrile tetrahydrofuranHCID 22177404—
生成物3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-(2-oxo-tetrahydro-pyrimidin-1-ylmethyl)-benzamideHCID 1157042461.2%

反応手順

The amine synthesized in Step A (66.4 mg, 0.1233 mmol) was dissolved in THF:CH3CN (1:1 v/v, 3.0 ml). N,N-disuccinimidyl carbonate (47.4 mg, 1.5 eq., 0.1849 mmol) and triethylamine (103.1 μl, 6.0 eq., 0.7398 mmol) were added sequentially to this solution, and the mixture was stirred at room temperature for 20 hours. The solvent was removed under reduced pressure, and the residue was purified by LC/MS to give white crystals (42.6 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08575391B2
出典データセットuspto-grants-2013_11
ORD IDord-cb017b8eb39d4e5ca03e452baacee576
出典メモuspto-grants-2013_11