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HRID 61291作成日:2026年10月25日

Ether hydrochloride → (S)-2-amino-3-difluoromethoxypropionic acid benzyl ester hydrochloride salt

https://huagongshe.com/reaction/61291

反応式

関与物質

役割名称HCID仕込み量
反応物Ether hydrochlorideHCID 10953452—
反応物(S)-2-tert-butoxycarbonylamino-3-difluoromethoxy-propionic acid benzyl esterHCID 90041473—
溶媒Diethyl EtherHCID 3283—
生成物(S)-2-amino-3-difluoromethoxypropionic acid benzyl ester hydrochloride saltHCID 9004014069%

反応条件

温度0 °C

反応手順

A solution of the compound of Formula XIII(a), (S)-2-tert-butoxycarbonylamino-3-difluoromethoxy-propionic acid benzyl ester (2.11 g, 5.89 mmol) in ether (10 mL) was treated with 2M HCl/ether, and stirred at 0° C. for 2 hours. The reaction mixture was concentrated to dryness and triturated with hexane/ether to give the compound of Formula V(a) (S)-2-amino-3-difluoromethoxy-propionic acid benzyl ester hydrochloride salt (1.15 g, 69%) as a white powder. 1H NMR (300 MHz, CDCl3): δ (ppm) 7.40-7.33 (m, 5H), 6.53 (broad s, 1H), 6.18 (wt, 1H), 5.25 (dd, 1H), 5.21 (dd, 2H), 4.53 (dt, 1H) 4.18 (td, 1H), 4.16-4.13 (m, 2H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09441012B2
出典データセットuspto-grants-2016_09
ORD IDord-53d4b22b70ed40a481fbf2687825441d
出典メモuspto-grants-2016_09