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E2 receptor agonists prostaglandin which comprises, as an active ingredient, they -PGE1 compound 6-oxo, and methods for their preparation
E2 receptor agonists prostaglandin which comprises, as an active ingredient, they -PGE1 compound 6-oxo, and methods for their preparation
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机译:包含作为活性成分的-PGE1化合物6-oxo的E2受体激动剂前列腺素及其制备方法
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摘要
PROBLEM TO BE SOLVED: To obtain a new compound scarcely binding to other subtype receptors, selectively and strongly binding to an EP1 receptor and useful as an antidepressant, an antiulcer agent, etc. ;SOLUTION: This compound is represented by formula I [A is a 4- to a 7-membered carbocyclic ring; R1 is hydroxyl group, a 1-4C alkoxy or the like; R2 is a (substituted) 1-8C alkylene, a (substituted) 3-8C alkenylene or the like; R3 is H, a 1-4C alkyl, a (substituted)phenyl or the like], preferably 2,5-ethano-6- oxo-17,20-dimethyl-PGE), etc. The compound is preferably obtained by eliminating a protecting group of hydroxyl group in a compound represented by formula II [Y is the protecting group of the hydroxyl group eliminable under acidic conditions; R2a is a (substituted) 1-8C alkylene or a 3-8C alkenylene] under the acidic conditions.;COPYRIGHT: (C)1999,JPO
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机译:解决的问题:要获得一种新化合物,该化合物几乎不与其他亚型受体结合,可以选择性且牢固地与EP1受体结合,并可用作抗抑郁药,抗溃疡药等;解决方案:该化合物由式I表示[A为4至7元碳环; R 1 Sup>是羟基,1-4C烷氧基等。 R 2 Sup>是(取代的)1-8C亚烷基,(取代的)3-8C亚烯基等。 R 3 Sup>为H,1-4C烷基,(取代的)苯基等],优选为2,5-乙基-6-氧代-17,20-二甲基-PGE)等。该化合物优选通过消除式II表示的化合物中的羟基的保护基来获得[Y是在酸性条件下可消除的羟基的保护基; R 2a Sup>是在酸性条件下的(取代的)1-8C亚烷基或3-8C亚烯基。; COPYRIGHT:(C)1999,JPO
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