- Novel method of preparing Epinastine
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The present invention relates to a novel manufacturing method for synthesizing an anti-histamine pharmaceutical medicine, epinastine. The novel manufacturing method for synthesizing epinastine according to the present invention has fewer synthesizing steps than a conventional epinastine manufacturing method, and is a safe synthesis method, thereby being expected to be used for inexpensively synthesizing the anti-histamine pharmaceutical medicine, epinastine by the manufacturing method, and supplying the same to the market.COPYRIGHT KIPO 2020
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Paragraph 0076-0079
(2020/05/13)
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- A facile synthesis of epinastine HCl via dehydroepinastine intermediate
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Epinastine is a second generation histamine H1 receptor antagonist used as a non-sedative antiallergic drug. When given orally, epinastine poorly penetrates blood-brain barrier (BBB) and appears to be free of cardiac toxicity as compared to other antihistamine drugs. A couple of synthetic approaches for epinastine HCl have been reported so far. They hold several problems such as explosive, highly toxic or expensive reagents. Moreover, they usually do not offer concise synthetic steps. In our synthesis shown here, a commonly used starting material, 6-(chloromethyl)-11H-dibenzo[b,e]azepine is treated with cyanamide to afford dehydroepinastine (14) in significantly high yield, which is subsequently reduced in the presence of aqueous HCl to give epinastine HCl in only two steps (75% overall yield for two steps). The problems associated with the reported processes such as using toxic and dangerous chemicals, lengthy synthetic steps or low overall product yields can be overcome by utilizing this new route. We believe our synthetic scheme might provide a breakthrough to reduce the cost of the production of epinastine HCl.
- Park, Sang Won,Kang, Han Eol,Yun, Wheesahng,Lee, Sang Yeul,Nam, Tae-gyu
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supporting information
(2019/12/24)
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- Preparation method of 6-Chloromethylmorphanthridine
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The invention belongs to the technical field of medicinal chemistry and particularly relates to a preparation method of 6-Chloromethylmorphanthridine. The preparation method comprises the steps that under the action of concentrated sulfuric acid, N-[2-(phenyl methyl)phenyl]-2-chloroacetamide is taken as the raw material, a complex compound of a trifluoromethanesulfonic acid rare earth compound and dimethyl sulfoxide is taken as the catalyst, and dehydration cyclization is performed to prepare the 6-Chloromethylmorphanthridine. According to the preparation method of the 6-Chloromethylmorphanthridine, the complex compound of the trifluoromethanesulfonic acid rare earth compound and the dimethyl sulfoxide is taken as the catalyst, a better effect is realized, the pollution is small, the preparation method is environment-friendly, and recyclable production is realized.
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Paragraph 0031; 0034-0035; 0038; 0041; 0043; 0045; 0047
(2017/11/04)
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- A new process for the preparation of 3-amino-9,13b-dihydro-1H-dibenz [c,f] imidazo[1,5-a]azepine bromic acid salt
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The present invention relates to a novel method for preparing an enhanced 3-amino-9, 13b-dihydro-1H-dibenz [c,f] imidazo [1,5-a] azepine bromic acid salt. The compound is used as an intermediate in manufacturing the epinastine hydrochloride. The compound is represented by the structural formula (I).COPYRIGHT KIPO 2015
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Paragraph 0017; 0025-0029
(2016/12/07)
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- Stereoselective synthesis of (R)-(-)-mianserin
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(14bR)-2-Methyl-1,2,3,4,10,14b-hexahydrodibenzo[c,f]pyrazino[1,2-a]azepine, (R)-(-)-mianserin 1a was synthesised in several steps in good enantiomeric purity with the use of (S)-(-)-α-methylbenzylamine 5. The absolute configuration was assigned on the bas
- Pawlowska,Czarnocki,Wojtasiewicz,Maurin
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p. 3335 - 3342
(2007/10/03)
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