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【结 构 式】 
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【分子编号】14120 【品名】1-Pyrrolidinyl(4,5,6,7-tetrahydro-1H-benzimidazol-5-yl)methanone 【CA登记号】 |
【 分 子 式 】C12H17N3O 【 分 子 量 】219.2866 【元素组成】C 65.73% H 7.81% N 19.16% O 7.3% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(II)The Vilsmeier-type reaction of 1-methylindole (I) with 5-(1-pyrrolidinocarbonyl)-4,5,6,7-1H-tetrahydrobenzimidazole hydrochloride (II) and phosphorous oxychloride in 1,2-dichloroethane gives (±)-5-[(1-methyl-3-indolyl)carbonyl]-4,5,6,7-tetrahydro-1H-benzimidazol e (III). Optical resolution of (III) with (+)-dibenzoyltartaric acid (DIBTA) in DMF-H2O, followed by exchange of the salt affords YM060.
| 【1】 Ohta, M.; Koide, T.; Suzuki, T.; Matsuhisa, A.; Miyata, K.; Ohmori, J.-Y.; Yanagisawa, I. (Yamanouchi Pharmaceutical Co., Ltd.); Tetrahydrobenzimidazole derivs. AU 9048890; EP 0381422; JP 1991223278; US 5344927 . |
| 【2】 Ohmori, J.; Yanagisawa, I.; Matsuhisa, A.; Suzuki, T.; Furuya, T.; Ohta, M.; Miyata, K.; Koide, T.; Synthesis and 5-HT3 antagonistic activities of 4,5,6,7-tetrahydrobenzimidazole derivatives. 200th ACS Natl Meet (Aug 26-31, Washington DC) 1990, Abst MEDI 39.. |
| 【3】 Miyata, K.; Ohta, M.; YM060. Drugs Fut 1992, 17, 1, 28. |
Extended Information