反应 #167769

反应方程式

compound 77a

tert-butyl 2-amino-4-[(1R)-1-({[(6R)-6-(5-chloro-2-methoxybenzyl)-7-oxo-3-(phenoxyimino)-1,4-diazepan-1-yl]carbonyl}amino)propyl]benzoate

hydrochloric acid

→

title compound

收率 161.7%

2-amino-4-[(1R)-1-({[(6R)-6-(5-chloro-2-methoxybenzyl)-7-oxo-3-(phenoxyimino)-1,4-diazepan-1-yl]carbonyl}amino)propyl]benzoic acid hydrochloride

收率 161.7%

溶剂

acetic acid

反应条件

后处理

1. 1
   workup.ADDITIONwas added
2. 2
   浓缩The reaction solution was concentrated
3. 3
   workup.ADDITIONthe residue was diluted with ethyl acetate
4. 4
   workup.ADDITIONTo this solution, a 1M hydrochloric acid in acetic acid solution was added
5. 5
   workup.STIRRINGthe mixture was stirred
6. 6
   workup.ADDITIONFurther, diethyl ether was added
7. 7
   过滤the precipitated solid was collected by filtration

实验过程

To the compound 77a (523 mg) obtained at Step (1), 1M hydrochloric acid in acetic acid solution (18 ml) was added, and the mixture was stirred at room temperature for 2.5 hours. The reaction solution was concentrated, then the residue was diluted with ethyl acetate. To this solution, a 1M hydrochloric acid in acetic acid solution was added and the mixture was stirred. Further, diethyl ether was added, and the precipitated solid was collected by filtration to obtain the title compound (410 mg).

来源