반응 #1115256

반응 방정식

tert-butyl (3S,5R)-5-methylpiperidin-3-ylcarbamate

6-(6-(thiazol-2-yl)pyridin-2-yl)quinolin-4-yl trifluoromethanesulfonate

DIEA

→

(3S,5R)-5-methyl-1-(6-(6-(thiazol-2-yl)pyridin-2-yl)quinolin-4-yl)piperidin-3-amine

수율 51.0%

용매

i-PrOH

반응 조건

후처리

1. 1
   온도Upon cooling the material
2. 2
   기타was purified directly by RP-HPLC
3. 3
   농축concentrated
4. 4
   기타purified by RP-HPLC

실험 절차

A solution of tert-butyl (3S,5R)-5-methylpiperidin-3-ylcarbamate (1.5 equiv.) and 6-(6-(thiazol-2-yl)pyridin-2-yl)quinolin-4-yl trifluoromethanesulfonate (1.0 equiv.) and DIEA (2.0 equiv.) in i-PrOH was heated in a microwave at 150° C. (5×20 min). Upon cooling the material was purified directly by RP-HPLC. Upon lyophilization, the Boc group was deprotected by treatment with 25% TFA/CH2Cl2, concentrated, purified by RP-HPLC and lyophilized to yield (3S,5R)-5-methyl-1-(6-(6-(thiazol-2-yl)pyridin-2-yl)quinolin-4-yl)piperidin-3-amine (51%). LC/MS=402.0 (M+H), LC=2.16 min.

출처