反応 #514356

反応方程式

tert-butyl N-(3-((2-methoxyacetimidoyl) aminomethyl)benzyl)carbamate

3-(aminomethyl)benzyl carbamate

→

N-(3-(Aminomethyl)benzyl)-2-methoxyacetamidine

収率 61.8%

溶媒

trifluoroacetic acid

反応条件

後処理

1. 1
   その他The crude product was purified by C18 reverse phase chromatography
2. 2
   洗浄eluting with water (0.1% trifluoroacetic acid)

実験手順

The intermediate tert-butyl N-(3-((2-methoxyacetimidoyl) aminomethyl)benzyl)carbamate (360 mg) prepared from tert-butyl N-(3-(aminomethyl)benzyl carbamate and intermediate G analogous to example 1 was deprotected in trifluoroacetic acid at 20° C. for 16 h. The crude product was purified by C18 reverse phase chromatography eluting with water (0.1% trifluoroacetic acid) to yield 150 mg of N-(3-(Aminomethyl)benzyl)-2-methoxyacetamidine as a yellowed, viscous oil (freeze-dried). Mass spectrum (CI) 208.0 (MH+, 100%). 1H NMR (200 MHz, D2O) δ 7.5-7.3 (m, 4H), 4.57 (s, 2H), 4.37 (s, 2H), 4.15 (s, 2H), 3.44 (s, 3H).

出典