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2-芳基烷酸类抗炎药物中,如萘普生(Naproxen),为(S)-异构体,较(R)-体的活性强28倍。可用以下通法分别合成二个光学异构体。例如萘普生,可将(1)与甲醇钠甲醇溶液作用,定量地得到(2),再与l-10-樟脑磺酰氯反应,得到1:1的二个非对映体(3),拆分后(理论收率为66%),将(S)-异构体在H_2O-DMF中与碳酸钙作用,经芳基1,2-重排,β-
Among the 2-arylalkanoic anti-inflammatory drugs, such as Naproxen, are the (S) -isomers, which are 28 times more potent than (R) -. Two optical isomers can be synthesized separately by the following general method. For example, naproxen can be (1) and sodium methoxide methanol solution obtained quantitatively (2), and l-10-camphorsulfonyl chloride reaction to give a 1: 1 two diastereomers (3) After resolution (theoretical yield 66%), the (S) -isomer interacts with calcium carbonate in H 2 O-DMF,