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The Total Synthesis of Spermine Alkaloid Kukoamine Bimesylate
Synlett ( IF 1.7 ) Pub Date : 2018-11-14 , DOI: 10.1055/s-0037-1610326
Kai Dong 1
Affiliation  

The first total synthesis of kukoamine B bimesylate was completed from 1,4-diaminobutane dihydrochloride in 12 steps with a 11.4% overall yield, and all the steps could be carried out at a kilogram scale. The cyano groups were used as the precursor of amino groups to avoid the competitive reaction delicately. The aza-Michael addition reaction, amidation and hydrogenation of the cyano group sequence was streamlined as a general approach towards the synthesis of polyamine structures.

中文翻译:

精胺生物碱库克胺双甲磺酸盐的全合成

首次以1,4-二氨基丁烷二盐酸盐为原料合成kukoamine B二甲磺酸盐,共分12步,总收率11.4%,所有步骤均可在公斤级规模进行。氰基被用作氨基的前体,以避免微妙的竞争反应。氮杂-迈克尔加成反应、氰基序列的酰胺化和氢化被简化为合成多胺结构的一般方法。
更新日期:2018-11-14
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