HRID1669420

反应详情

EQUATION

反应方程式

HRID 1669420 的结构方程式

AUXILIARIES

试剂、催化剂与溶剂

2

CONDITIONS

反应条件

温度
40 °C

PROCEDURE

实验过程

(7R)-7-[{2-[(tert-butoxycarbonyl)(methyl)amino]ethyl}(methyl)amino]-14-cyclohexyl-3-(pyridin-2-ylmethoxy)-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid, N-(2,2-dimethoxyethyl)-N-methylsulfamide (2 eq, see Example 1, Step 1) and DMAP (5 eq) were dissolved in DCM (24 mM) and EDC (3 eq) was added. The mixture was warmed to 40° C. After 2 h the mixture was diluted with DCM and extracted twice with H2O, sat. aq. NH4Cl and brine. The organic phase was dried over Na2SO4 and evaporated in vacuo. The product was obtained as a yellowish sticky solid and used without further purification (91%). (ES+) m/z 849 (M+H)+.

WORKUP

后处理

  1. extractionextracted twice with H2O, sat. aq. NH4Cl and brine
  2. dry with materialThe organic phase was dried over Na2SO4
  3. customevaporated in vacuo
  4. customThe product was obtained as a yellowish sticky solid
  5. customused without further purification (91%)