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1. WO2022088583 - 5-METHYLCHROMONE, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF

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Publication Number WO/2022/088583
Publication Date 05.05.2022
International Application No. PCT/CN2021/080485
International Filing Date 12.03.2021
IPC
C07D 311/22 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo pyrans, not hydrogenated in the carbocyclic ring
22with oxygen or sulfur atoms directly attached in position 4
C07C 45/45 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
45Preparation of compounds having C=O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
45by condensation
C07C 49/825 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
49Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
76Ketones containing a keto group bound to a six-membered aromatic ring
82containing hydroxy groups
825all hydroxy groups bound to the ring
C07C 45/64 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
45Preparation of compounds having C=O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
61by reactions not involving the formation of C=O groups
64by introduction of functional groups containing oxygen only in singly bound form
C07C 45/68 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
45Preparation of compounds having C=O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
61by reactions not involving the formation of C=O groups
67by isomerisation; by change of size of the carbon skeleton
68by increase in the number of carbon atoms
C07C 49/84 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
49Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
76Ketones containing a keto group bound to a six-membered aromatic ring
84containing ether groups, groups, groups, or groups
CPC
A61K 2800/782
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
2800Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
74Biological properties of particular ingredients
78Enzyme modulators, e.g. Enzyme agonists
782Enzyme inhibitors; Enzyme antagonists
A61K 8/498
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
8Cosmetics or similar toilet preparations
18characterised by the composition
30containing organic compounds
49containing heterocyclic compounds
4973with oxygen as the only hetero atom
498having 6-membered rings or their condensed derivatives, e.g. coumarin
A61Q 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
QSPECIFIC USE OF COSMETICS OR SIMILAR TOILET PREPARATIONS
19Preparations for care of the skin
02for chemically bleaching or whitening the skin
C07C 45/455
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
45Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
45by condensation
455with carboxylic acids or their derivatives
C07C 45/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
45Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
61by reactions not involving the formation of >C = O groups
64by introduction of functional groups containing oxygen only in singly bound form
C07C 45/68
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
45Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
61by reactions not involving the formation of >C = O groups
67by isomerisation; by change of size of the carbon skeleton
68by increase in the number of carbon atoms
Applicants
  • 海南医学院 HAINAN MEDICAL UNIVERSITY [CN]/[CN]
Inventors
  • 李友宾 LI, Youbin
  • 王雪松 WANG, Xuesong
  • 王燕 WANG, Yan
  • 徐俊裕 XU, Junyu
  • 陈煜 CHEN, Yu
  • 曾婷婷 ZENG, Tingting
  • 崔雪 CUI, Xue
  • 谭银丰 TAN, Yinfeng
  • 龚晶雯 GONG, Jingwen
Agents
  • 海口汉普知识产权代理有限公司 HAIKOU HEIP INTELLECTUAL PROPERTY AGENCY CO., LTD
Priority Data
202011166791.727.10.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) 5-METHYLCHROMONE, AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
(FR) 5-MÉTHYLCHROMONE, ET PROCÉDÉ DE PRÉPARATION ASSOCIÉ ET SON APPLICATION
(ZH) 一种5-甲基色酮及其制备方法和应用
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Abstract
(EN) 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.
(FR) La présente invention concerne la 5-méthylchromone et un procédé de préparation associé et son application. La 5-méthylchromone a la structure suivante, telle que présentée dans la formule, dans laquelle R1 et R2 représentent un alkyle. La chromone substituée a une activité biologique visant à inhiber la tyrosinase. Le procédé de préparation comprend : la prise de 3,5-dihydroxytoluène en tant que matière première et la mise en œuvre d’une acylation, d’une estérification, d’un réarrangement, d’une réaction de cyclisation et analogues pour synthétiser une chromone substituée par différents groupes au niveau d’un site 2-C. Dans la présente invention, R1 représente -CH2CH2CH3 et R2 représente -CH2CH3 ; R1 représente -C(CH3)3 et R2 représente H ; les composés sont des composés nouveaux. Tous les composés présentent une importante activité inhibitrice de la tyrosinase et peuvent s’appliquer à la préparation d’inhibiteurs de la tyrosinase ou d’agents de blanchiment.
(ZH) 本发明提供一种5-甲基色酮及其制备方法和应用，所述5-甲基色酮具有下述结构：其中R1和R2为烷基。取代后的色酮具有抑制酪氨酸酶的生物活性。制备方法以3,5-二羟基甲苯为原料，经过酰基化、酯化、重排和环化反应等合成2-C位不同基团取代的色酮。本发明R1为-CH2CH2CH3，R2为-CH2CH3及R1为-C(CH3) 3，R2为H者为全新的化合物。所有化合物对酪氨酸酶具有明显的抑制活性，可应用于制备酪氨酸酶抑制剂或美白剂。
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