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R-(-)- AND S-(+)-4-(3-AMINO-2-HYDROXYPROPOXY)-CARBAZOLES, STEREOSPECIFIC PREPARATIONS THEREFOR, AND PHARMACEUTICAL COMPOSITIONS
R-(-)- AND S-(+)-4-(3-AMINO-2-HYDROXYPROPOXY)-CARBAZOLES, STEREOSPECIFIC PREPARATIONS THEREFOR, AND PHARMACEUTICAL COMPOSITIONS
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机译:R-(-)-和S-(+)-4-(3-氨基-2-羟基),咔唑,立体异构体制备和药物组合物
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摘要
A process for the preparation of S- or R-carbazole derivatives of the general formula: IMAGE in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: IMAGE in which R1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt. The new R-(+)- and S-(-)-carbozole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.
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