반응 #61533

반응 방정식

1-[5-(5-Chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-5-furan-2-yl-1H -pyrazole-3-carboxylic acid

4-(4-Amino-phenyl)-morpholin-3-one

BOP-Cl

→

1-[5-(5-Chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-5-furan-2-yl-1H-pyrazole-3-carboxylic acid [4-(3-oxo-morpholin-4-yl)-phenyl]-amide

용매

DCM

NEt3

반응 조건

후처리

1. 1
   농축The mixture was was concentrated under reduced pressure
2. 2
   기타the residue was purified by preparative HPLC (
3. 3
   세척C18 reverse phase column, elution with a H2O/MeCN gradient with 0.1% TFA)
4. 4
   workup.ADDITIONThe fractions containing the product
5. 5
   기타were evaporated
6. 6
   기타to yield a white solid

실험 절차

To 100 mg 1-[5-(5-Chloro-thiophen-2-yl)-isoxazol-3-ylmethyl]-5-furan-2-yl-1H -pyrazole-3-carboxylic acid in 2 ml DCM and 0.1 ml NEt3, 62 mg 4-(4-Amino-phenyl)-morpholin-3-one and 67 mg BOP-Cl were added at RT and the mixture was stirred for 16 h. The mixture was was concentrated under reduced pressure and the residue was purified by preparative HPLC (C18 reverse phase column, elution with a H2O/MeCN gradient with 0.1% TFA). The fractions containing the product were evaporated and lyophilized to yield a white solid.

출처