Large-scale synthesis of galeterone and lead next generation galeterone analog VNPP433-3β

Puranik Purushottamachar,Elizabeth Thomas,Retheesh S Thankan,Vladimir Rudchenko,Guangfei Huang,Vincent C O Njar

Steroids（2022）

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摘要

•We have developed an improved large-scale synthesis of Galeterone (1) from DHEA with an overall yield of 59%.•Developed large-scale synthesis of lead NGGA (VNPP433-3β) from DHEA with an overall yield of 26%.•The 8-steps synthetic process (DHEA to VNPP433-3β) require only two column chromatographic steps.•The use of inexpensive reagents and organic solvents was accomplished.

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关键词

Galeterone,VNPP433-3β,Large-scale synthesis

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