Preparing Deucravacitinib used as selective tyrosine kinase inhibitor for treatment of psoriasis, involves reacting ester compound with Methan-d3-amine or its hydrochloride in presence of base and solvent to produce amide compound, further reacted with amine compound to produce Deucravacitinib
	HIRATOT S N; GANTA S; KOYYADI S; KUMAR C R P; SAMANTA P K; SEKHAR N M; BUDHDEV R R
	2023-07-19
专利权人	REDDYS LAB LTD (REDY-C)
申请日期	2023-07-19
专利号	IN202341048682-A
成果简介	NOVELTY - Preparing Deucravacitinib (I), involves (a) reacting pyridazine-2,4-diol (II) with phosphoryl chloride (POCl3) in presence base and solvent to produce 2, 4-chloro pyridazine (III), (b) reacting a compound (III) with 3-phenyl-1H-1,2,4-triazole compound (IV) in presence of base and solvent to produce ester compound (V), (c) reacting a compound (V) with Methan-d3-amine or its hydrochloride in presence of base and solvent to produce amide compound (VI), (d) reacting a compound (VI) with amine compound (VII) in presence of catalyst, ligand and base to produce Deucravacitinib formula (VIII). USE - Method for preparing Deucravacitinib, i.e., 6-(cyclopropanecarbonylamido)-4-[2- methoxy-3-(1-methyl-1,2,4-triazol-3-yl)anilino]-N-(trideuteriomethyl)pyridazine-3- carboxamide, used as selective tyrosine kinase 2 (TYK2) inhibitor for the treatment of psoriasis. ADVANTAGE - The method provides a simple and cost-efficient process for preparation of a Deucravacitinib. DETAILED DESCRIPTION - Preparing Deucravacitinib of formula (I), involves (a) reacting pyridazine-2,4-diol of formula (II) with phosphoryl chloride (POCl3) in presence base and solvent to produce 2, 4-chloro pyridazine of formula (III), (b) reacting a compound of formula (III) with 3-phenyl-1H-1,2,4-triazole compound of formula (IV) in presence of base and solvent to produce ester compound of formula (V), (c) reacting a compound of formula (V) with Methan-d3-amine or its hydrochloride in presence of base and solvent to produce amide compound of Formula (VI), (d) reacting a compound of Formula (VI) with amine compound of formula (VII) in presence of catalyst, ligand and base to produce Deucravacitinib formula (VIII). An INDEPENDENT CLAIM is included for a process for the preparation of crystalline Deucravacitinib, which involves: (a) providing a solution of Deucravacitinib in a solvent, (b) optionally seeding with crystalline Deucravacitinib, and (c) removing the solvent to obtain crystalline Deucravacitinib.
IPC 分类号	C07D-403/12
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/21249
专题	中国科学院新疆生态与地理研究所
作者单位	REDDYS LAB LTD (REDY-C)
推荐引用方式 GB/T 7714	HIRATOT S N,GANTA S,KOYYADI S,et al. Preparing Deucravacitinib used as selective tyrosine kinase inhibitor for treatment of psoriasis, involves reacting ester compound with Methan-d3-amine or its hydrochloride in presence of base and solvent to produce amide compound, further reacted with amine compound to produce Deucravacitinib. IN202341048682-A[P]. 2023.

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