| 摘要 |
Novel spiro-(4,5)-decanes have the general formula <FORM:1100281/C2/1> where R is hydrogen, C1- 4 lower alkyl, or an Ar-A-grouping, where Ar is phenyl optionally substituted by one or two of halogen, CF3, C1-C5 alkyl and alkoxy, methylene dioxy, hydroxyl or carbomethoxy, or is pyrimidyl or tetrahydrofuryl, and A represents a straight chain -(CH2)nwhere n is 1 to 4, or a branched chain methylene arrangement of up to 4 carbon atoms, or a methylene arrangement substituted by an aryl group, or containing a double bond, a secondary alcohol group, an ether group, or an amide group. The compounds are prepared, when R is other than hydrogen, by reacting an amino alcohol of the formula <FORM:1100281/C2/2> with phosgene, urea or an alkyl ester of carbonic acid in the presence of an alcoholate, or by reacting a compound of the first general formula above, where R is hydrogen, with a derivative R-hal where R is other than hydrogen and hal is Cl, Br or I. The compounds in which R is hydrogen are prepared by debenzylating 1 - oxa - 2 - oxo - 3,8 - diaza - 8 - benzylspiro - (4,5) - decane by catalytic hydrogenolysis. 1 - Benzyl - 4 - hydroxy - 4 - aminomethylpiperidine is prepared by reduction of the corresponding cyanohydrin in tetrahydrofuran with aluminium alanate: 1-phenethyl-, 1-g -phenyl-propyl-, 1-phenylisopropyl-, and 1-methyl-4 - hydroxy - 4 - aminomethyl - piperidine are prepared in a similar manner. Therapeutic compositions useful as bronchodilators, analgesics, and anti-inflammatory agents contain a compound of the first general formula above or a physiologically tolerable addition salt thereof together with a pharmaceutically acceptable carrier. They may be administered orally, rectally, or parenterally. |
| 申请人 |
SCIENCE UNION ET CIE. (SOCIETE FRANCAISE DE RECHERCHE MEDICALE), SURESNES, HAUTS-DE-SEINE (FRANKREICH) |
发明人 |
REGNIER, GILBERT, SCEAUX;CANEVARI, ROGER, LA HAYE LES ROSES;DOUAREC, JEAN- CLAUDE LE, SURESNES |
