RYU, JAE WOOK,류재욱,KO, YOUNG KWAN,고영관,KIM, JONG GEUN,김종근,SEO, JI SU,서지수,KOO, DONG WAN,구동완,KIM, KYOUNG SUNG,김경성,CHOI, IN YOUNG,최인영,HONG, MI SOOK,홍미숙,KIM, TAE JOON,김태준,AHN, HEE GEUN,안희근,KIM, SI YONG,김시용
申请号:
KR1020110143415
公开号:
KR1020130075163A
申请日:
2011.12.27
申请国别(地区):
KR
年份:
2013
代理人:
摘要:
PURPOSE: A method for preparing 4,5-dihydrooxazol-2-ylbenzene derivatives is provided to have a relatively mild reaction condition, to easily handle a reagent, and to synthesize the 4,5-dihydrooxazol-2-ylbenzene derivatives with high yield.CONSTITUTION: A method for preparing 4,5-dihydrooxazole-2-ylbenzene compound of chemical formula 1 or a salt thereof comprises the step of cyclizing a hydroxyalkyl benzamide of chemical formula 2 under the presence of (diethylamino)sulfur trifluoride (DAST) or para-toluene sulfonate (TsOH). The cyclization is performed under the presence of a base selected from the group consisting of tray (C_1-C_6) alkyl amine, alkali metal or hydroxide of the alkali earth metal, hydroxide, and C_1-C_6 alkoxide. The base is selected from the group consisting of trimethyl amine, triethyl amine, diethyl isopropyl amine, lithium hydroxide, sodium hydroxide, calcium hydroxide, sodium hydroxide, potassium hydroxide, sodium methoxide, and potassium methoxide.COPYRIGHT KIPO 2013본 발명은 하이드록시알킬 벤즈아마이드 화합물을 고리화 반응시켜 4,5-디히드로옥사졸-2-일벤젠 화합물 또는 이의 염을 제조하는 방법에 관한 것이다.