Preparation of 1,1,2,2-tetramethyl-1,2-bis(2-fluoro-4-hydroxyphenyl)ethane derivatives and antitumor pharmaceuticals containing them

Abstract

The title compds. [I; R1, R2 = H, (di)(alkyl)aminocarbonyl, PO(OH)2, (halo)alkanoyl, alkenoyl] are prepd. as antiestrogens, and are useful for the treatment of estrogen receptor-pos. tumors (no data). Thus, 2-(2-fluoro-4-methoxyphenyl)-2-propanol (II; prepn. given) was stirred with TiCl3 in dry dimethoxyethane, followed by the addn. of LiAlH4 and more II, to give I (R1 = R2 = OMe), which was treated sequentially with BBr3 in CH2Cl2 at -60 Deg and NaOH-MeOH, to give I (R1 = R2 = OH)(III). A mixt. of 10 g III, 106.7 g CaHPO4, 2.3 g gelatin, 1 g Polysorbate, and 20.7 g water was granulated. The granules were mixed with 20 g corn starch and encapsulated.