Preparing triazine and triazin-yl-acetate, for preparing isopropyl benzamide, for treating cancer involves reacting substituted hydrazinecarbothioamide with diethyl oxalate, then reacting triazine-diol with catalyst, reacting diol with phosphorous oxychloride, reacting triazine with acetic anhydride
2023-08-30
专利权人ALMELO PRIVATE LTD (ALME-Non-standard)
申请日期2023-08-30
专利号IN202341058035-A
成果简介NOVELTY - Preparing 5,6-dichloro-2,4-triazine (I) and 6-chloro-1,2, 4- triazin-yl-acetate (II) involves (a) reacting substituted hydrazinecarbothioamide with diethyl oxalate in presence of solvent to give 3-mercapto-1,2,4-triazine-5,6-diol; (b) reacting 3-mercapto-1,2,4-triazine-5,6-diol with catalyst to provide (1,2,4-triazine-5,6-diol); (c) reacting(1,2,4-triazine-5,6-diol) with phosphorous oxychloride to get 5,6-dichloro-1,2,4- triazine; (d) reacting 5,6-dichloro-1,2,4-triazine with acetic anhydride in presence of solvent and base to get 6-chloro-1,2,4-triazin-5-y1 acetate (II). USE - Process for preparing of 5,6-dichloro-2,4-triazine (I) and 6-chloro-1,2, 4- triazin-yl-acetate (II), used for preparing (2-((5-chloro-1,2,4-triazin-6-ypoxy)-N-(3,3- difluorocyclobuty1)-5-fluoro-N-isopropylbenzamide), for treating cancer and having antibacterial, antifungal, anti-cancer, antiviral, antimalarial, anti inflammatory, antiulcer, anticonvulsant, antimicrobial, insecticidal and herbicidal activity. No biological data given. ADVANTAGE - The process is robust, safe and industrially feasible. The (I) has high yield. DETAILED DESCRIPTION - Preparing of 5,6-dichloro-2,4-triazine of formula (I) and 6-chloro-1,2, 4- triazin-yl-acetate of formula (II) involves (a) reacting substituted hydrazinecarbothioamide with diethyl oxalate in presence of solvent to give 3-mercapto-1,2,4-triazine-5,6-diol; (b) reacting 3-mercapto-1,2,4-triazine-5,6-diol with catalyst to provide (1,2,4-triazine-5,6-diol); (c) reacting(1,2,4-triazine-5,6-diol) with phosphorous oxychloride to get 5,6-dichloro-1,2,4- triazine; (d) reacting 5,6-dichloro-1,2,4-triazine with acetic anhydride in presence of solvent and base to get 6-chloro-1,2,4-triazin-5-y1 acetate (II). INDEPENDENT CLAIMS are included for: 1. a process for preparing of 2-((5-chloro-1, 2,4-triazin-6-yl)oxy)-5- fluorobenzoic acid of formula (III) which involves (a) reacting 5-fluoro-2-hydroxybenzoic acid with sulfuric acid in presence of solvent to get methyl 5-fluoro-2-hydroxy benzoate; (b) reacting methyl 5-fluoro-2-hydroxy benzoate with 5,6-dichloro-1,2,4-triazine (I) in presence of base, solvent to get methyl 24(5-chloro-1,2,4-triazin-6-y0oxy)-5- fluorobenzoate (I); (c) basify methyl 2((5-chloro-1,2,4-triazin-6-yl)oxy)-5-fluorobenzoate to get 2-((5-chloro1,2,4-triazin-6-yl)oxy)-5-fluorobenzoic acid (III); 2. a process for preparing of intermediate 5-fluoro-2-((5-hydroxy-1,2,4-triazin- 6- yI)oxy)benzoic acid of formula (IV) which involves; (a) reacting 5-fluoro-2-hydroxybenzoic acid with sulfuric acid in presence of solvent to get methyl 5-fluoro-2-hydroxy benzoate; (b) reacting methyl 5-fluoro-2-hydroxy benzoate with 6-chloro-1,2,4-triazin-5-y1 acetate (II) in presence of base, solvent to get methyl 24(5-acetoxy-1,2,4-triazin-6-yl)oxy)-5- fluorobenzoate; (c) basify methyl 2((5-acetoxy-1,2,4-triazin-6-yl)oxy)-5-fluorobenzoate to get 5-fluoro-24(5- LL C5 I hydroxy-1,2,4-triazin- 6-yl)oxy)benzoic acid.
IPC 分类号A61K-031/53 ; A61P-035/00 ; C07D-253/06 ; C07D-403/12 ; C07D-413/10 ; C07D-487/04
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/20604
专题中国科学院新疆生态与地理研究所
作者单位
ALMELO PRIVATE LTD (ALME-Non-standard)
推荐引用方式
GB/T 7714
RAO C C,KRISHNA A T P,DCO K. Preparing triazine and triazin-yl-acetate, for preparing isopropyl benzamide, for treating cancer involves reacting substituted hydrazinecarbothioamide with diethyl oxalate, then reacting triazine-diol with catalyst, reacting diol with phosphorous oxychloride, reacting triazine with acetic anhydride. IN202341058035-A[P]. 2023.
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