Preparing tapinarof in treatment of plaque psoriasis, comprises dealkylating stilbene derivative, and using dealkylating agent in presence of metal catalyst to provide tapinarof
	SEERLA R; SOMISETTI N R; NANDEPU H; NANDEPU V R
	2023-07-27
专利权人	METROCHEM API PVT LTD (METR-Non-standard)
申请日期	2023-07-27
专利号	IN202341050582-A
成果简介	NOVELTY - Preparing tapinarof (I) comprises dealkylating stilbene derivative (II), and using a dealkylating agent in the presence of a metal catalyst to provide the tapinarof. USE - Method for preparing tapinarof in treatment of plaque psoriasis. No biological data given. ADVANTAGE - The method provides tapinarof crystalline Form IV, which has purity more than 99% by high-performance liquid chromatography, thus ensures tapinarof and its intermediates with high chemical purity and yields. DETAILED DESCRIPTION - Preparing tapinarof of formula (I) comprises dealkylating stilbene derivative of formula (II), and using a dealkylating agent in the presence of a metal catalyst to provide the tapinarof, where R1 is 1-6C alkyl; or reducing a benzyl carboxylic acid derivative of formula (III) in presence of boron trifluoride etherate and sodium borohydride to provide benzyl alcohol derivative of formula (IV), reacting with a halogenating agent to provide benzyl alcohol derivative intermediate of formula (V), reacting with triethyl phosphate to provide phosphate intermediate of formula (VI), reacting with benzaldehyde to provide stilbene, and dealkylating using a dealkylating agent in the presence of a metal catalyst to provide tapinarof. An INDEPENDENT CLAIM is included for a method for preparing the tapinarof crystalline Form IV, which comprises: (a) providing a solution of Tapinarof in alcoholic solvent selected from methanol or ethanol, (b) adding water to solution or vice versa; and (c) isolating the crystalline Form IV of tapinarof.
IPC 分类号	A61P-017/06 ; A61P-037/02 ; C07C-037/055 ; C07C-039/21 ; C07C-041/30 ; C07C-043/215 ; C07C-045/68 ; C07C-047/575
国家	印度
专业领域	医药卫生
语种	英语
成果类型	专利
文献类型	科技成果
条目标识符	http://119.78.100.226:8889/handle/3KE4DYBR/21085
专题	中国科学院新疆生态与地理研究所
作者单位	METROCHEM API PVT LTD (METR-Non-standard)
推荐引用方式 GB/T 7714	SEERLA R,SOMISETTI N R,NANDEPU H,et al. Preparing tapinarof in treatment of plaque psoriasis, comprises dealkylating stilbene derivative, and using dealkylating agent in presence of metal catalyst to provide tapinarof. IN202341050582-A[P]. 2023.

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