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参考文献:Synthesis And Sar Study Of Novel Pseudo-Steroids As Potent And Selective Progesterone Receptor Antagonists
标题:Synthesis And Sar Study Of Novel Pseudo-Steroids As Potent And Selective Progesterone Receptor Antagonists
摘要:Synthesis Of Novel 7-Pseudo-Steroids 1C Has Been Achieved From Trenbolone 3 Via An Efficient 14 Step Sequence With Overall Yields Of 10-15%. Various Substitutions Were Incorporated At Both The Aromatic Side Chain As Well As The D Ring. The Orientation Of Aromatic Side Chain At C10 Plays A Crucial Role For Progesterone Receptor (Pr) Activity. Compound 2A (T47D = 1 Nm) With-Nme2 Para To The Aromatic Group Along With Spirofurane Groups In The D Ring Was The Optimal Substitution. All Compounds Were Also Evaluated For Glucocorticoid Receptor (Gr) Antagonist Activities In Vivo In A Rat And Found Efficacious In Uterine Complement C3 Assay Via The Oral Route Of Administrations. (C) 2009 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2009.01.095