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    • 10. 发明公开
    • 신물질6-메틸-3-펜에틸-3,4-디히드로-1H-큐나졸린-2-티온,이의 제조방법 및 이를 유효성분으로 포함하는 미백 효능조성물
    • 具有白色活性和无皮肤毒性的6-甲基-3-苯基-3,4-二氢-1H-喹喔啉-2-酮的化合物,其制备方法和含有该化合物作为有效成分的衍生物组合物
    • KR1020050019401A
    • 2005-03-03
    • KR1020030057135
    • 2003-08-19
    • 충북대학교 산학협력단솔젠트 (주)
    • 김영수정상헌민경락박준규이지현
    • C07D239/78C07D239/80A61K31/495
    • A61K8/4953A61K31/495A61Q19/02C07D239/93
    • PURPOSE: A compound of 6-methyl-3-phenethyl-3,4-dihydro-1H-quinazoline-2-thione, a preparation method thereof and a depigmentation composition containing the same compound as an effective component are provided, which compound has improved whitening activity and no toxicity against skin. CONSTITUTION: The compound of 6-methyl-3-phenethyl-3,4-dihydro-1H-quinazoline-2-thione represented by formula (1) is provided. The method for preparing the compound of 6-methyl-3-phenethyl-3,4-dihydro-1H-quinazoline-2-thione of formula (1) comprises the steps of: reducing (5-methyl-2-nitrobenzyl) phenethylamine of formula (2) to prepare 4-methyl-2-(penethylaminomethyl) phenylamine of formula (3); reacting the 4-methyl-2-(penethylaminomethyl) phenylamine of formula (3) with 1,1'-carbonyldiimidazol to prepare 6-methyl-3-penethyl-3,4-dihydro-1H-quinazoline-2-one of formula (4); reacting the 6-methyl-3-penethyl-3,4-dihydro-1H-quinazoline-2-one of formula (4) with a Lawesson's reagent. The depigmentation composition contains 0.0001 to 1 wt.% of 6-methyl-3-phenethyl-3,4-dihydro-1H-quinazoline-2-thione of formula (1).
    • 目的:提供6-甲基-3-苯乙基-3,4-二氢-1H-喹唑啉-2-硫酮的化合物,其制备方法和含有与有效成分相同的化合物的脱色组合物,该化合物具有改善 美白活性,无皮肤毒性。 构成:提供由式(1)表示的6-甲基-3-苯乙基-3,4-二氢-1H-喹唑啉-2-硫酮的化合物。 制备式(1)的6-甲基-3-苯乙基-3,4-二氢-1H-喹唑啉-2-硫酮化合物的方法包括以下步骤:将(5-甲基-2-硝基苄基)苯乙胺还原为 式(2)制备式(3)的4-甲基-2-(penethylaminomethyl)phenylamine; 使式(3)的4-甲基-2-(辛基氨基甲基)苯胺与1,1'-羰基二咪唑反应,制备式(6)的6-甲基-3-苯乙基-3,4-二氢-1H-喹唑啉-2-酮 4); 使式(4)的6-甲基-3-苯乙基-3,4-二氢-1H-喹唑啉-2-酮与Lawesson试剂反应。 脱色组合物含有0.0001〜1重量%的式(1)的6-甲基-3-苯乙基-3,4-二氢-1H-喹唑啉-2-硫酮。