[3α-(3)H]17α-羟基孕烯醇酮和[3α-(3)H]孕烯醇酮的合成
Synthesis of [3α-(3) H] 17α-hydroxy pregnenolone and [3α-(3) H] pregnenolone.
作者信息
Tian Yuan, Hong Yang, Bonacorsi Samuel J, Balog Aaron, Gong Sharon
机构信息
Radiochemical Synthesis Group, Bristol-Myers Squibb Company, Route 206 and Province Line Road, Princeton, NJ, 08543, USA.
出版信息
J Labelled Comp Radiopharm. 2014 Jan;57(1):1-11. doi: 10.1002/jlcr.3114. Epub 2013 Oct 24.
For the first time, [3α-(3) H] 17α-hydroxy pregnenolone (1) was synthesized through a multiple step sequence. The presence of [3β-(3) H] isomer in RP-HPLC purified product was identified by tritium NMR. The [3β-(3) H] isomer was then separated from [3α-(3) H] 17α-hydroxy pregnenolone with chiralPAK AD-H column. [3α-(3) H] pregnenolone (2) was synthesized from commercial available 5-pregnen-3,20-dione in one step with an improved procedure.
首次通过多步合成序列合成了[3α-(3)H]17α-羟基孕烯醇酮(1)。通过氚核磁共振鉴定了反相高效液相色谱纯化产物中[3β-(3)H]异构体的存在。然后用手性PAK AD-H柱从[3α-(3)H]17α-羟基孕烯醇酮中分离出[3β-(3)H]异构体。[3α-(3)H]孕烯醇酮(2)由市售的5-孕烯-3,20-二酮通过改进的方法一步合成。
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