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Title:
5-METHYLCHROMONE, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/088583
Kind Code:
A1
Abstract:
The present invention provides 5-methylchromone, and a preparation method therefor and an application thereof. The 5-methylchromone has the following structure as shown in the formula, wherein R1 and R2 are alkyl. The substituted chromone has biological activity for inhibiting tyrosinase. The preparation method comprises: taking 3,5-dihydroxytoluene as a raw material, and performing acylation, esterification, rearrangement, a cyclization reaction and the like to synthesize chromone substituted by different groups at a 2-C site. In the present invention, R1 is -CH2CH2CH3, and R2 is -CH2CH3; R1 is -C(CH3)3, and R2 is H; the compounds are novel compounds. All the compounds have significant inhibitory activity on tyrosinase and can be applied to preparation of tyrosinase inhibitors or whitening agents.

Inventors:
LI YOUBIN (CN)
WANG XUESONG (CN)
WANG YAN (CN)
XU JUNYU (CN)
CHEN YU (CN)
ZENG TINGTING (CN)
CUI XUE (CN)
TAN YINFENG (CN)
GONG JINGWEN (CN)
Application Number:
PCT/CN2021/080485
Publication Date:
May 05, 2022
Filing Date:
March 12, 2021
Export Citation:
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Assignee:
HAINAN MEDICAL UNIV (CN)
International Classes:
C07D311/22; A61K8/49; A61Q19/02; C07C45/45; C07C45/64; C07C45/68; C07C49/825; C07C49/84; C07C67/08; C07C69/16
Domestic Patent References:
WO2017015221A12017-01-26
Foreign References:
CN112174922A2021-01-05
JPH05301813A1993-11-16
CN109912556A2019-06-21
JP2020066619A2020-04-30
Other References:
AHLUWALIA, V. K.; RANI, NIMMI: "Formation of 4-Propylcoumarins from β-Diketones & a Reinvestigation of Kostanecki-Robinson Butyrylation of β-Orcacetophenone", INDIAN JOURNAL OF CHEMISTRY, vol. 15B, no. 11, 30 November 1977 (1977-11-30), DE , pages 1003 - 1005, XP009536163, ISSN: 0376-4699
Attorney, Agent or Firm:
HAIKOU HEIP INTELLECTUAL PROPERTY AGENCY CO., LTD (CN)
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