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HRID 390157作成日:2026年10月24日

Ethanaminium, N,N,N-triethyl-, fluoride (1:1) → HCID 58295714、化合物

https://huagongshe.com/ja/reaction/390157

反応式

関与物質

役割名称HCID仕込み量
反応物Ethanaminium, N,N,N-triethyl-, fluoride (1:1)HCID 69582—
反応物(+/-)-(E)-2-(trimethylsilyl)ethyl 7-bromo-1'-(3-(2-(trifluoromethyl)phenyl)acryloyl)-2,3-dihydrospiro[indene-1,4'-piperidine]-3-ylcarbamateHCID 67223014—
溶媒AcetonitrileHCID 6342—
生成物HCID 58295714HCID 5829571488.3%

反応条件

温度100 °C

反応手順

(±)-(E)-2-(trimethylsilyl)ethyl 7-bromo-1′-(3-(2-(trifluoromethyl)phenyl)acryloyl)-2,3-dihydrospiro[indene-1,4′-piperidine]-3-ylcarbamate (16.5 mg, 0.026 mmol) and Et4NF (30 mg) were dissolved in MeCN (3 mL). The solution was heated at 100° C. for 10 min in a microwave. The solution was concentrated and the residue was purified by preparative HPLC to give (±)-(E)-1-(3-amino-7-bromo-2,3-dihydrospiro[indene-1,4′-piperidine]-1′-yl)-3-(2-(trifluoromethyl)phenyl)prop-2-en-1-one (11 mg, 70%) as its TFA salt. LC-MS Method 1 tR=1.38, min, m/z=479, 481; 1H NMR (CD3OD) 1.53 (m, 1H), 1.67 (m, 1H), 2.08 (m, 1H), 2.55 (m, 1H), 2.9-3.5 (5H), 4.38 (d, 1H), 4.72 (d, 1H), 7.2-8.0 (9H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08383629B2
出典データセットuspto-grants-2013_02
ORD IDord-f91e544cfc5d460e8abc75187bb983f4
出典メモuspto-grants-2013_02