| 摘要 |
Novel 14 - hydroxydihydronormorphines of the general formula <FORM:1119270/C2/1> wherein R is allyl, dimethylallyl, methylallyl, propargyl, methylpropargyl, cyclopropylmethyl, cyclopropylbutyl or propyl and pharmaceutically acceptable salts thereof are prepared by reacting a compound of the formula wherein Z is <FORM:1119270/C2/2> (in which case Z may be protected) with a substituting agent (a) of the formula R-CH2-X wherein X is a halogen or an R-CH2-sulphate residue or the residue of an aryl or alkyl sulphonate group, or (b) of the formula R-CO-X wherein X is halogen or the remainder of an ester or anhydride group, and wherein R in each of formulae (a) and (b) is vinyl, 1-propenyl, 2-methyl-1-propenyl, ethynyl, 2-methylethynyl, cyclopropyl, cyclobutyl or ethyl and then, if required reducing. Examples are given of the preparation of the N - hydrocarbyl substituted - 14 - hydroxydihydronormorphinones by the process described above without the final reduction. Pharmaceutical compositions comprise a novel compound as above defined and an acceptable vehicle. The compounds may be administered from ampoules or vials or in the form of tablets (hypodermic, sublingual or oral), liquids or rectal suppositories. The compounds are stated to have narcotic antagonism and analgetic properties.
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