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【结 构 式】 
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【分子编号】14654 【品名】2-(cyclopropylmethoxy)benzoyl isocyanate 【CA登记号】 |
【 分 子 式 】C12H11NO3 【 分 子 量 】217.22428 【元素组成】C 66.35% H 5.1% N 6.45% O 22.1% |
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：(III)The reaction of salicylamide (I) with cyclopropylmethyl bromide in the presence of potassium hydroxide gives the ether (II). This intermediate is converted to the benzoyl isocyanate (III) by refluxing with oxalyl chloride in 1,2-dichloroethane. The isocyanate is converted without further purification to endo-2-(cyclopropylmethoxy)-N-[[(8-methyl-8-azabicyclo[3.2.1]oct-3-yl) amino]-carbonyl]benzamide (WAY100289) by reaction with endo-3-aminotropane.
| 【1】 Ward, T.J.; White, J.C.; Bradley, G. (John Wyeth & Brother Ltd.); Aroyl-ureas. AU 9163749; EP 0422846; GB 2236528; JP 1991133986 . |
| 【2】 Ward, T.J.; Taylor, A.; White, J.C.; Coleman, J.; Bradley, G.; Rhodes, K.F.; Novel antagonists of the 5-HT3 receptor. Synthesis and structure activity relationships of (2-alkoxybenzoyl)ureas. J Med Chem 1992, 35, 9, 1515-9. |
| 【3】 Ward, T.J.; WAY 100289. Drugs Fut 1993, 18, 1, 23. |
Extended Information