Synthesizing carbamazepine used for treating neural disorders, involves preparing oxacarbazepine from diphenylamine and chloroacetyl chloride, adding reducing agent to oxacarbazepine in organic solvent, refluxing (Z)-10-hydroxy-10,11-dihydro-5H-dibenzo[b, f]azepine-5-carboxamide with Lewis acid
	SINGH D; GILL M S
	2023-10-13
专利权人	NAT INST PHARM EDUCATION & RES (NAPH-Non-standard)
申请日期	2023-10-13
专利号	IN202311069022-A
成果简介	NOVELTY - Synthesizing carbamazepine of (II), involves: (A) preparing oxacarbazepine of (I), from diphenylamine and chloroacetyl chloride; (B) adding a reducing agent to the oxacarbazepine, in a mole ratio of 1:1-1:15, in presence of an organic solvent at a predetermined temperature for a predetermined time period to yield (Z)-10-hydroxy-10,11-dihydro-5H-dibenzo[b, f]azepine-5-carboxamide; and (C) refluxing (Z)-10-hydroxy-10,11-dihydro-5H-dibenzo[b, f]azepine-5-carboxamide with a Lewis acid, in a mole ratio of 1:1-1:15, in presence of an organic solvent, at a predetermined temperature for a predetermined time period, to yield carbamazepine. USE - Process for synthesizing carbamazepine used as anti-epileptical agent for treatment of neural disorders, or Parkinson's disease or Parkinsonian syndromes. No biological data given. ADVANTAGE - The process is cost-effective, efficient, environmentally benign, non-toxic, non-hazardous and economical; and utilizes water assisted solvent, with less reaction time and good yield. DETAILED DESCRIPTION - Synthesizing carbamazepine of formula (II), involves: (A) preparing oxacarbazepine of formula (I), from diphenylamine and chloroacetyl chloride; (B) adding a reducing agent to the oxacarbazepine, in a mole ratio of 1:1-1:15, in presence of an organic solvent at a predetermined temperature for a predetermined time period to yield (Z)-10-hydroxy-10,11-dihydro-5H-dibenzo[b, f]azepine-5-carboxamide; and (C) refluxing (Z)-10-hydroxy-10,11-dihydro-5H-dibenzo[b, f]azepine-5-carboxamide with a Lewis acid, in a mole ratio of 1:1-1:15, in presence of an organic solvent, at a predetermined temperature for a predetermined time period, to yield carbamazepine. An INDEPENDENT CLAIM is included for a process for synthesizing oxcarbazepine of (I), which involves: (i) reacting diphenyl amine and chloroacetyl chloride in a mole ratio of 1:1-1:5, in presence of an organic solvent at a predetermined temperature for a predetermined time period to obtain 2-chloro-N, N-diphenylacetamide; (ii) adding a Lewis acid at a predetermined concentration to a solution of 2-chloro-N,N-diphenylacetamide in a mole ratio of 1:1-1:7, in presence of the organic solvent at a predetermined temperature for a predetermined time to yield 1-phenylindolin-2-one; (iii) treating 1-phenylindolin-2-one with a base in a mole ratio of 1:1-1:10 in presence of an organic solvent at a predetermined temperature for a predetermined time period to yield 2-(2-(phenylamino)phenyl)acetic acid; (iv) treating 2-(2-(phenylamino)phenyl)acetic acid with a Lewis acid in a mole ratio of 1:1-1:10, in presence of an organic solvent at a predetermined temperature for a predetermined time period to yield 5,11-dihydro-10H-dibenzo[b, f]azepin-10-one; (v) reacting 5,11-dihydro-10H-dibenzo[b, f]azepin-10-one, and O-phenyl carbamate in a mole ratio of 1:1-1:6, in presence of a base and an organic solvent at a predetermined temperature for a predetermined time period to yield 10-oxo-10,11-dihydro-5H-dibenzo[b, f]azepine-5-carboxamide (oxcarbazepine).
IPC 分类号	A61K-031/55 ; C07C-259/06 ; C07D-223/18 ; C07D-223/22 ; C07D-223/28 ; C07D-223/30
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/19966
专题	中国科学院新疆生态与地理研究所
作者单位	NAT INST PHARM EDUCATION & RES (NAPH-Non-standard)
推荐引用方式 GB/T 7714	SINGH D,GILL M S. Synthesizing carbamazepine used for treating neural disorders, involves preparing oxacarbazepine from diphenylamine and chloroacetyl chloride, adding reducing agent to oxacarbazepine in organic solvent, refluxing (Z)-10-hydroxy-10,11-dihydro-5H-dibenzo[b, f]azepine-5-carboxamide with Lewis acid. IN202311069022-A[P]. 2023.

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