公开(公告)号：US20110152544A1

公开(公告)日：2011-06-23

申请号：US13031975

申请日：2011-02-22

申请人： Johannes STOELWINDER ,  Nicolaas Elisabeth Cornelis MOERS

发明人： Johannes STOELWINDER ,  Nicolaas Elisabeth Cornelis MOERS

IPC分类号： C07D319/06 ,  C07J1/00 ,  C07C49/603

CPC分类号： C07J75/005

摘要： 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 R1 is a C1-C10 alkyl, alkenyl or aryl group; —Cl, —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 R1 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 R1 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.

摘要翻译： 本发明提供了一种制备雌酮和雌二醇的2-取代衍生物的方法，其包括：i）通过一种或多种步骤将通式（I）的化合物与一种或多种步骤反应制备通式（II）的化合物， 其中R 1是C 1 -C 10烷基，烯基或芳基; -Cl，-Br，-I，-F; -CN; -哦; 或-OR 2，-O（CO）R 2或-R 2 -OH基团，其中R 2是具有1-6个C原子的烷基或亚烷基; 并且原子9和10之间的键合是单键或双键。 ii）通式II化合物与通式Ⅲ化合物的芳构化，其中R1和R2具有上述定义; 和iii）任选地将通式III的化合物还原成通式IV的化合物，其中R 1和R 2具有上述定义。 此外，本发明提供了几种新颖的化合物，其可以是上述方法中的中间体，以及制备这些新化合物的方法。 本发明还提供基本上不含其它雌激素中间体的2-烷氧基 - 雌酮，2-烷氧基 - 雌二醇或其混合物。