Total synthesis of an enantiomeric pair of FR900482 .1. Synthetic and end-game strategies
Total synthesis of an enantiomeric pair of FR900482 .1. Synthetic and end-game strategies
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DOI：
10.1016/s0040-4020(97)00650-9
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发表时间：
1997-07-28
期刊：
影响因子：
2.1
通讯作者：
Terashima, S
中科院分区：
文献类型：
--
作者：
Katoh, T;Itoh, E;Terashima, S
开发了FR 900482（1）对映体对的合成策略，其特征在于从5-羟基戊酸（16）和酒石酸二乙酯（17和ent-17）的各对映体开始的收敛和对映体选择性序列。以1的三乙酰基衍生物FK 973（3）为原料合成了关键中间体10，并成功地将10转化为1。这些初步研究明确表明，10适合作为1的潜在高级关键中间体，其中可以实现涉及精细脱保护和氧化步骤的关键最终反应序列（10->1）。(C)1997年爱思唯尔科学有限公司
A synthetic strategy for an enantiomeric pair of FR900482 (1) was developed, which features a convergent and enantioselective sequence starling from 5-hydroxyisophthalic acid (16) and each enantiomer of diethyl tartrate (17 and ent-17). The proposed key intermediate 10 was synthesized from FK973 (3), the triacetyl derivative of 1, and successful reconversion of 10 into 1 was also achieved. These preliminary studies definitely demonstrated that 10 is suitable as a potential advanced key intermediate for 1 mid that the crucial final sequence of reactions (10-->1) involving delicate deprotection and oxidation steps can be realised. (C) 1997 Elsevier Science Ltd.