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HRID 857019作成日:2026年10月27日

Potassium Phosphate, Tribasic → {1-[3-(3-Dimethylamino-pyrrolidin-1-yl)-phenyl]-ethyl}-carbamic acid tert-butyl ester

https://huagongshe.com/reaction/857019

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium Phosphate, TribasicHCID 62657—
反応物(3R)-(+)-3-(Dimethylamino)pyrrolidineHCID 2758521—
反応物(S)-N-Boc-1-(3-bromophenyl)ethylamineHCID 56971804—
触媒Bis(dibenzylideneacetone)palladiumHCID 9811564—
溶媒DichloromethaneHCID 6344—
溶媒1,2-DimethoxyethaneHCID 8071—
生成物{1-[3-(3-Dimethylamino-pyrrolidin-1-yl)-phenyl]-ethyl}-carbamic acid tert-butyl esterHCID 6958872627%

反応手順

A mixture of (S )[1-(3-bromo-phenyl)-ethyl]-carbamic acid tert-butyl ester (6 g), (3R)-3-(dimethylamino)-pyrrolidine (4.56 g), Pd2(dba)3 (1.83 g), di-t-butyl-biphenylphosphine (600 mg), K3PO4 (8.48 g) in DME (40 mL) was stirred at reflux for 16 h. The reaction mixture was cooled down to room temperature, diluted with methylene chloride, and filtered. The filtrated was evaporated in vacuo, and the crude product was purified by Flash Chromatography using Biotage eluting with 20% MeOH in ethyl acetate to give the title compound (1.8 g) as an oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07144881B2
出典データセットuspto-grants-2006_12
ORD IDord-25c8f9ac53e244bba0ba6badd5929881
出典メモuspto-grants-2006_12