反应 #157341

反应方程式

HCl

1,4-dioxane

tert-butyl 4-(2,3-dihydro-1H-inden-5-ylcarbamoyl)-3-((pyridin-3-yloxy)methyl)piperazine-1-carboxylate TFA salt

→

title compound

收率 65.0%

N-(2,3-dihydro-1H-inden-5-yl)-2-((pyridin-3-yloxy)methyl)piperazine-1-carboxamide dihydrochloride

收率 65.0%

溶剂

MeOH

反应条件

后处理

1. 1
   浓缩the reaction mixture was concentrated under reduced pressure
2. 2
   其他purified by HPLC (5 to 50% MeCN/0.1% TFA in H2O/0.1% TFA gradient)
3. 3
   workup.ADDITIONThe fractions containing the desired product
4. 4
   浓缩were concentrated under reduced pressure
5. 5
   workup.DISSOLUTIONThe material was dissolved in MeOH (1 mL)
6. 6
   workup.ADDITIONtreated with 4 M HCl in 1,4-dioxane (6 mL)
7. 7
   浓缩The mixture was concentrated under reduced pressure

实验过程

4 M HCl in 1,4-dioxane (6 mL, 24 mmol) was added to a solution of tert-butyl 4-(2,3-dihydro-1H-inden-5-ylcarbamoyl)-3-((pyridin-3-yloxy)methyl)piperazine-1-carboxylate TFA salt (62.6 mg, 0.110 mmol) in MeOH (1 mL). After 1 h, the reaction mixture was concentrated under reduced pressure and purified by HPLC (5 to 50% MeCN/0.1% TFA in H2O/0.1% TFA gradient). The fractions containing the desired product were concentrated under reduced pressure. The material was dissolved in MeOH (1 mL) and treated with 4 M HCl in 1,4-dioxane (6 mL). The mixture was concentrated under reduced pressure to give 30.7 mg (65%) of the title compound. LC-MS: RT=4.79 min, [M+H]+=353.2.

来源