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【结 构 式】 
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【分子编号】15136 【品名】rac-(2-fluorocyclopropanecarboxylic acid) 【CA登记号】 |
【 分 子 式 】C4H5FO2 【 分 子 量 】104.0809032 【元素组成】C 46.16% H 4.84% F 18.25% O 30.74% |
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：(XII)The chiral intermediate (1R,2S)-N-(tert-butoxycarbonyl)-2-fluorocyclopropylamine (III) can also be obtained as follows: 4) The cyclopropanation of 1-chloro-1-fluoroethylene (XXVIII) with diazoacetic esters (XXIX) catalyzed by rhodium catalysts, especially dirhodium (II) tetrakistriphenylacetate, gives preferentially the corresponding 2t-chloro-2c-fluorocyclopropane-1r-carboxylic esters (XXX), which are easily dechlorinated to the cis-racemic-2-fluorocyclopropanecarboxylic acid (XII), already obtained as intermediate in the synthesis shown in Scheme 2.
| 【1】 Castaner, J.; Graul, A.; Prous, J.; DU-6859. Drugs Fut 1994, 19, 9, 827. |
| 【2】 Kohda, H.; Takahashi, H.; Ishida, Y.; et al.; Practical synthesis of DU-6859a: Novel synthesis of cis-2-fluorocyclopropanecarboxylic acid, the key intermediate of 1-substituent. 33rd Intersci Conf Antimicrob Agents Chemother (Oct 17-20, New Orleans) 1993, Abst 975. |
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