| 摘要 |
<p>There is described a process for preparing a dihydroxy compound of the formula <CHEM> or a physiologically acceptable ether or ester thereof, or a physiologically acceptable acid addition salt of the dihydroxy compound or of the ether or ester thereof; wherein R<1> and R<2> are independently C1-C4 alkyl, or combine to form C4-C6 polymethylene, -(CH2)2O(CH2)2-, or -CH2CH(CH3)CH2CH2-; which process comprises acylating a compound of the formula <CHEM> wherein R<3> is -COR<5> or -SO2R<5>, and R<5> is C1-C4 primary or secondary alkyl, trifluoromethyl, trichloromethyl, phenyl, p-tolyl, p-anisyl, or mono- or di(halo or nitro)phenyl; under Friedel-Crafts conditions with an acylating agent of the formula <CHEM> wherein R<7> is X or <CHEM> X is chloro, bromo or -SO2R<5>; and R<6> is chloro, bromo, iodo, or an activating ester group; when R<7> is X, displacing the X group with an amine of the formula <CHEM> when R<3> is -SO2R<5>, cleaving the R<3> groups to substitute hydrogen for -SO2R<5>; and when R<3> is -COR<5>, optionally cleaving none, one, or both R<3> groups to substitute hydrogen for -COR<5>. The use of particularly advantageous protecting groups for the hydroxy groups of 6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophenes provides a high-yielding process for the preparation of such compounds having a 4-(2-aminoethoxy)benzoyl 3-group.</p> |
