| 摘要 |
<p>The invention aims at providing a process for industrial production of novel estradiol derivatives useful as drugs; intermediates used in the process; and a process for production of the intermediates. The invention provides a process for production of compounds represented by the general formula (|): (|) (wherein m is an integer of 2 to 14; n is an integer of 2 to 7; and R4 is linear or branched halogenoalkyl having 1 to 7 carbon atoms), which comprises the step of introducing a side chain represented by the general formula: -(CH2)mCH(COOR3)-(CH2)n-R4 (wherein m, n, and R4 are each as defined above; and R3 is a carboxyl-protecting group) to the 7-position of a compound represented by the general formula (||): (||) (wherein R1 and R2 are each independently a hydroxyl-protecting group), and the step of conducting reduction of the carbonyl group at the 6-position and deblocking of the hydroxyl-protecting groups at the 3- and 17-positions and the carboxyl-protecting group.</p> |
