药物详细合成路线
| Name | Croconazole hydrochloride;Cloconazole hydrochloride;710674S;Pilzcin | | Chemical Name | 1-[1-[2-(3-Chlorophenyl)methoxy]phenyl]vinyl]-1H-imidazole monohydrochloride | | CAS | 77174-66-4 | | Related CAS | 77175-51-0 (free base) | | Formula | C18H16Cl2N2O | | Structure |  | | Formula Weight | 347.24702 | | Stage | 上市-1986 | | Company | Shionogi (Originator), Merz (Licensee) | | Activity/Mechanism | Antifungal Agents, ANTIINFECTIVE THERAPY | | Syn. Route | 1 | | Route 1 | | this 1-vinyl derivative (ii) is obtained by reaction of n,n-thionyldiimidazole (a) with o-hydroxyacetophenone (i) in dichloromethane at room temperature. treatment of (ii) with m-chlorobenzyl chloride (b) in the presence of koh in dmf gives the m-chlorobenzyl ether (iii). the hydrochloride can be prepared by treatment of (iii) with hcl in acoet. | | |  | | List of intermediates | No. | | (2r,3s)-2-(azidomethyl)tetrahydro-3-furanol | (iv) | | (3s)-3-[(4-methoxybenzyl)oxy]-4,4-dimethyl-6,6-diphenyl-5-hexen-1-ol | (ii) | | (3s)-3-[(4-methoxybenzyl)oxy]-4,4-dimethyl-6,6-diphenyl-5-hexenal | (iii) | | 1h-imidazol-5-ylmethanol | (i) | | hexahydropyrrolo[1,2-a]pyrazin-6(2h)-one | (v) | | | Reference 1: ogata, m.; hamada, y.; takehara, m.; tawara, k.; matsumoto, h.; 1-[1-[2-[(3-chlorobenzyl)oxy]phenyl]vinyl]-1h-imidazole hydrochloride, a new potent antifungal agent. j med chem 1983, 26, 5, 768-770. Reference 2: ogata, m.; tawara, k.; cloconazole hydrochloride. drugs fut 1985, 10, 6, 451. |
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来源:药化网
作者:药化小编
摘要:本文合成路线介绍的是药物中文名盐酸氯康唑；英文名Croconazole hydrochloride;Cloconazole hydrochloride;710674S;Pilzcin；CAS[77174-66-4]
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