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HRID 886700作成日:2026年10月27日

5-Amino-1-(4-fluorophenyl)-N-(3,3,3-trifluoro-2-hydroxy-2-{[(phenylmethyl)amino]methyl}propyl)-1H-pyrazole-4-carboxamide → 5-amino-N-[2-(aminomethyl)-3,3,3-trifluoro-2-hydroxypropyl]-1-(4-fluorophenyl)-1H-pyrazole-4-carboxamide

https://huagongshe.com/reaction/886700

反応式

関与物質

役割名称HCID仕込み量
反応物5-Amino-1-(4-fluorophenyl)-N-(3,3,3-trifluoro-2-hydroxy-2-{[(phenylmethyl)amino]methyl}propyl)-1H-pyrazole-4-carboxamideHCID 59487497—
触媒PalladiumHCID 23938—
溶媒EthanolHCID 702—
生成物5-amino-N-[2-(aminomethyl)-3,3,3-trifluoro-2-hydroxypropyl]-1-(4-fluorophenyl)-1H-pyrazole-4-carboxamideHCID 5948749489.4%

反応手順

5-amino-1-(4-fluorophenyl)-N-(3,3,3-trifluoro-2-hydroxy-2-{[(phenylmethyl)amino]methyl}propyl)-1H-pyrazole-4-carboxamide (20.47 g) was dissolved in ethanol (100 ml) and hydrogenated over 10% palladium on carbon (2 g). A small portion was filtered using celite to give an orange yellow solution and LC/MS analysis indicated complete reaction. Therefore the remainder of the suspension was then filtered and the orange yellow solution concentrated in vacuo to give a pale yellow solid. This was dried on the vacuum line overnight to give the title compound (14.64 g) as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08247377B2
出典データセットuspto-grants-2012_08
ORD IDord-7156466eb3734303aaefd568e298b614
出典メモuspto-grants-2012_08