发明名称 Process for the preparation of 20-keto-21 alpha-01-steroids
摘要 A process for the preparation of a compound of the formula <IMAGE> I wherein R1 is alkyl of 1 to 3 carbon atoms, R2 is alkyl of 1 to 12 carbon atoms, R3 is alkyl of 1 to 4 carbon atoms comprising reacting a compound of the formula <IMAGE> II wherein R4 is a remainder of an easily cleavable ether, K is a protected ketone function in the form of ketal, thioketal or mixed ketal and R1 has the above definition with a magnesium organic compound reagent of the formula HalMg-CH2-R2A wherein Hal is a halogen and R2 is defined as above to obtain a compound of the formula <IMAGE> III wherein R1, R2 and K are defined as above, reacting the latter with an acylation agent to obtain a compound of the formula <IMAGE> IV wherein R5 is alkyl of 1 to 6 carbon atoms or aryl of 6 to 10 carbon atoms and R1, R2 and K are defined as above, reacting the latter with an appropriate alkylation agent to obtain a compound of the formula <IMAGE> V wherein R1, R2, R3 and K are defined as above, subjecting the latter to autoxidation to obtain a compound of the formula <IMAGE> VI wherein R1, R2, R3 and K are defined as above, reacting the latter with an acid to obtain a reconjugated 3-keto compound of the formula <IMAGE> VII wherein R1, R2 and R3 are defined as above and reacting the latter with a regio- and enantioselective reducing agent to obtain a compound of formula I and intermediates formed therein.
申请公布号 US5399685(A) 申请公布日期 1995.03.21
申请号 US19930075822 申请日期 1993.06.11
申请人 ROUSSEL-UCLAF 发明人 BUENDIA, JEAN;CROCQ, VERONIQUE;MASSON, CHRISTIAN;PRAT, DENIS;VIVAT, MICHEL
分类号 C07J9/00;C07J21/00;C07J33/00;C07J41/00;C07J75/00;C12P33/00;C12R1/865;(IPC1-7):C07J9/00 主分类号 C07J9/00
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