首页> 外国专利> Method for preparing Ester 17 OL 17 Alpha ethinyl - 4 - 3 - World Premiere - OR 17 beta - acetyl - - 3 - 4 - pregnen onas

Method for preparing Ester 17 OL 17 Alpha ethinyl - 4 - 3 - World Premiere - OR 17 beta - acetyl - - 3 - 4 - pregnen onas

机译:制备酯17 OL 17α-乙炔基-4-3-世界首演-OR 17 beta-乙酰基--3-4-怀孕的方法

摘要

Steroid esters of the Formula I IMAGE I wherein the A, B, C, and D rings can be substituted in the usual manner, R10 is hydrogen or methyl; R13 is alkyl of 1-3 carbon atoms; R17 is 17 alpha -alkynyl or alkadiinyl of up to 4 carbon atoms or 17 beta -acetyl, Z is X-OH, Y-CO-OH, X-O-CO-Y-CO-OH, X-O-CO-R, Y-CO-OR, X-O-CO-Y-CO-OR, or X-O-SO2-R; X is a straight-chain or branched alkylene of 1-6 carbon atoms, optionally interrupted by O or S atoms, wherein the chain or branches can be substituted by -OH, -O-CO-R, or -O-SO2-R; Y is a direct bond, a straight-chain or branched carbon chain of 1-3 atoms, optionally interrupted by an O or S atom if Y is linked to the steroid residue via -O-CO-; of 1-16 atoms if Y is linked to X via -O-CO; or 1,4-phenylene, 1,4-cyclohexylene, or 1,3-cyclopentylene optionally substituted by alkyl of 1-2 carbon atoms, or groups analogously 1,2- and 1,3-disubstituted, respectively; and R is an optionally substituted alkyl of up to 22 carbon atoms, have longer acting activity than the corresponding unesterified steroids and higher activity than the corresponding long chain esters.
机译:式I I的类固醇酯,其中A,B,C和D环可按常规方式取代,R 10为氢或甲基; R13是1-3个碳原子的烷基; R17为至多4个碳原子的17个α-炔基或炔二基或17个β-乙酰基,Z为X-OH,Y-CO-OH,XO-CO-Y-CO-OH,XO-CO-R,Y- CO-OR,XO-CO-Y-CO-OR或XO-SO2-R; X是1-6个碳原子的直链或支链亚烷基,任选地被O或S原子中断,其中该链或支链可以被-OH,-O-CO-R或-O-SO 2 -R取代。 ; Y是1-3个原子的直键,直链或支链碳链,如果Y通过-O-CO-与甾族残基连接,则任选被O或S原子中断;如果Y通过-O-CO与X连接,则为1-16个原子;或者1,4-亚苯基,1,4-亚环己基或1,3-亚环戊基任选地被1-2个碳原子的烷基或分别类似地被1,2-和1,3-二取代的基团取代; R是最多22个碳原子的任选取代的烷基,具有比相应的未酯化的类固醇更长的作用活性和比相应的长链酯更高的活性。

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