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HRID 237869作成日:2026年10月25日

Ethyl 3-cyclopropylprop-2-ynoate → (S)-2-(4-Bicyclo[3.3.1]non-9-yl-phenoxymethyl)-5-cyclopropyl-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-one

https://huagongshe.com/reaction/237869

反応式

関与物質

役割名称HCID仕込み量
反応物Ethyl 3-cyclopropylprop-2-ynoateHCID 639964—
反応物(S)-5-(4-bicyclo[3.3.1]non-9-yl-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamineHCID 68527534—
溶媒EthanolHCID 702—
生成物(S)-2-(4-Bicyclo[3.3.1]non-9-yl-phenoxymethyl)-5-cyclopropyl-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-oneHCID 2507014916%

反応条件

温度82 °C

反応手順

To a solution of (S)-5-(4-bicyclo[3.3.1]non-9-yl-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine (0.7 g, 2.23 mmol) (Example 20) in ethanol (40 mL) was added 0.462 g (3.35 mmol) of cyclopropyl-propynoic acid ethyl ester (Example 99). The reaction mixture was stirred at 82° C. for 30 minutes. The reaction mixture was concentrated and purified by chromatography on silica gel, eluting with MeOH/CH2Cl2 to afford 0.145 g of the title compound. [α]D25 −10.51 (c 0.5, CHCl3).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08642603B2
出典データセットuspto-grants-2014_02
ORD IDord-494112d35e844939b647719951059f8e
出典メモuspto-grants-2014_02