| 摘要 |
The invention comprises (1) novel compounds of Formula I <FORM:1107138/C2/1> wherein R1, R2 and R3 represent alkyl groups, R4, R5 and R6 represent hydrogen atoms or alkyl groups, and n represents 0 or 1, (2) the preparation thereof (a) by reacting a benzhydrol derivative of Formula II <FORM:1107138/C2/2> with an acetamide of formula B-(CH2-CH2-O)n-CH2CONR1R2 wherein A and B are different and each represents a halogen atom or a group -OM where M is a hydrogen or alkali metal atom, or A and B both represent hydroxyl groups, (b) by reacting an ester of Formula IV <FORM:1107138/C2/3> wherein R7 is an alkyl group, with a dialkylamine, (c) by N-alkylating by methods known per se a compound of Formula I in which R1 is hydrogen and R2 is hydrogen or an alkyl group, or (d) when n represents 1, by reacting a benzhydrol derivative of Formula VII <FORM:1107138/C2/4> with an acetamide of formula B-CH2CONR1R2 and (3) the preparation of compounds of Formula IX <FORM:1107138/C2/5> by reducing a compound of Formula I by methods known per se. Methyl o-methyl-a -phenylbenzyloxyacetate is prepared by treating o-methylbenzhydrol with sodium in xylene, reacting the product with chloroacetic acid, and converting the o-methyl-a -phenylbenzyloxyacetic acid formed to its methyl ester. 2-(Di-2,6-xylyl-methoxy)ethanol is made by heating 2,6,21,61-tetramethylbenzhydrol and b -chloroethanol, treating the 2-(di-2,6-xylyl-methoxy)ethyl chloride formed with potassium acetate, dimethyl sulphoxide and xylene, and heating the 2-(di-2,6-xylyl-methoxy)ethyl acetate thus obtained with potassium hydroxide in ethanol. Therapeutic compositions having sedative and anti-convulsant activity, which may be administered orally or parenterally, contain as active ingredient at least one compound of Formula I above. |
