发明名称 |
PROCESS FOR THE PREPARATION 2-SUBSTITUTED-DERIVATIVES OF ESTRONE AND ESTRADIOL |
摘要 |
<p>The invention provides a process for the preparation of 2- substituted-derivatives of estrone and estradiol comprising i) the preparation of a compound of general formula (II) by reacting a compound of general formula (I) in one or more steps to a compound of general formula II wherein Rl is a C1-C10 alkyl, alkenyl or aryl group; -C1, -Br, -I, -F; -CN; -OH; or a -OR2, -O(CO)R2 or -R2-OH group, wherein R2 is an alkyl or alkylene group having 1-6 C atoms; and the bonding between atoms 9 and 10 is a single or a double bond. ii) aromatization of the compound of general formula II to a compound of general formula III wherein Rl and R2 have the above defined meanings; and iii) optionally, reduction of the compound of general formula III to a compound of general formula IV wherein Rl and R2 have the above defined meanings . Furthermore the invention provides several novel compounds, which can be intermediates in the above process, and processes to prepare these novel compounds . The invention also provides 2-alkoxy-estrone, 2-alkoxy- estradiol or mixtures thereof essentially free from other estrogenic intermediates.</p> |
申请公布号 |
WO2006013196(A1) |
申请公布日期 |
2006.02.09 |
申请号 |
WO2005EP53732 |
申请日期 |
2005.08.01 |
申请人 |
AKZO NOBEL N.V.;STOELWINDER, JOHANNES;MOERS, NICOLAAS, ELISABETH, CORNELIS |
发明人 |
STOELWINDER, JOHANNES;MOERS, NICOLAAS, ELISABETH, CORNELIS |
分类号 |
C07J75/00;(IPC1-7):C07J75/00 |
主分类号 |
C07J75/00 |
代理机构 |
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