| 摘要 |
<p>1,140,399. Benzhydrol/glycerol ethers; cyclic arylboronates. KONINKLIJKE PHARMACEUTISCHE FABRIEKEN V/H BROCADES - STHEEMAN & PHARMACIA. 15 Sept., 1967 [16 Sept., 1966], No. 41540/66. Heading C2C. The invention comprises compounds (I) of formula wherein each R is H, halogen, alkyl or CF 3 , or R 1 R 1 , is a 2,2<SP>1</SP>-CH 2 -CH 2 - or -CH= CH- bridge, and their cyclic esters (II) with ArB(OH) 2 where Ar is Ph or naphthyl, possibly substituted by halogen, alkyl, nitro, amino or carboxy. (I) which are prepared by reacting a reactive ester of the corresponding benzhydrol with glycerol; (II) which are prepared by reacting (I) with ArB(OH) 2 , may be hydrolysed back to (I). (I) may also be made by reacting a benzhydrol-reactive ester with 2,2-dimethyl- 4-hydroxymethyl-1,3-dioxolan to give the 2,2- dimethyl - 4 - benzhydryloxymethyl - 1,3- dioxolan, and reacting this with H 3 BO 3 to give the cyclic (diester) borate of (I), which is then hydrolysed. Therapeutic compositions containing the above compounds (I) have muscle-relaxant, anticonvulsive, sedative and analgesic activity, and may be administered orally or parenterally. The arylboronates (II) have similar activity, and may also be used as neutron capturing agents in tumour treatment, e.g. in the brain.</p> |
