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foerfarande foer uppbyggnad av hydroxiacetyl - sidokedjan i steroider av pregnantyp nya 21 - hydroxi - 20 - oxo - 17alfa - pregnanfoereningar samt farmaceutiska preparat som innehaoller saodana foereningar
foerfarande foer uppbyggnad av hydroxiacetyl - sidokedjan i steroider av pregnantyp nya 21 - hydroxi - 20 - oxo - 17alfa - pregnanfoereningar samt farmaceutiska preparat som innehaoller saodana foereningar
The present invention relates to a novel general process for synthesizing a alpha - or beta -oriented hydroxyacetyl side chain of steroids of the pregnane type, which comprises treating a corresponding steroid carbaldehyde in succession with formaldehyde dimethylmercaptal-S-oxide in the form of an alkali metal salt thereof, and with a strongly acid hydrolysing agent. Preferred final products are compounds of the formula IMAGE (IA) wherein n is 1 or 2, R2 represents methyl or difluoromethyl, and R1 represents hydroxymethyl, methoxymethyl, acetoxymethyl or hydrogen, and, if n is 2 and/or R2 is difluoromethyl, R1 also represents methyl. These compounds act as agonists or antagonists of natural steroid hormones. The antigestagenic 19,21-dihydroxy-17 alpha -pregn-4-ene-3,20-dione and its 6,7-dehydro derivatives and diacetates are of particular interest.
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机译:本发明涉及一种用于合成孕烷类固醇的α-或β-取向的羟乙酰基侧链的新颖的一般方法,该方法包括用碱形式的甲醛二甲基巯基-S-氧化物连续处理相应的类固醇甲醛。其金属盐,并与强酸水解剂。优选的最终产物是式(IA)的化合物,其中n为1或2,R 2代表甲基或二氟甲基,R 1代表羟甲基,甲氧基甲基,乙酰氧基甲基或氢,并且如果n为2和/或R 2为二氟甲基。 R 1也代表甲基。这些化合物充当天然类固醇激素的激动剂或拮抗剂。抗孕激素的19,21-二羟基-17α-孕-4-烯-3,20-二酮及其6,7-脱氢衍生物和二乙酸酯特别受关注。
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