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The compound of formlua I in which R represents the--CH2CHOHCH2OH group (compound II)has been found posses (1)an intravenous toxicity (LD50 i.v.)in the mouse of 23400mg I/Kg and an intracerebral toxicity (LD50 i.c.) in the mouse of greater than 1500mg I/Kg (2) nephrotoxicity in the rabbit greater than 10500 mgI/Kg (3) the ability to form solution of high concentration ,i.e. at least 400-500 mg I/ml(4)low viscosity of 6.2cP at 37oC.and12.6cPa20oC.,the concentration in each case being 300mg I/ml;and (4) low osmolailty (cryoscopic) 0.65 Os/Kg at a concentration of 300 mg I/ml The radiological compositions of the present invention are conveniently presented in a form suitable for administration by injection,for example,in ampoules or vials. The capacity of the ampoule or vial may be,for example ,from 5 to 300 ml and the concentration may,for example ,be from 20 to 500 mg I/ml The compounds of the present invention may be prepared in any convenient manner,but the following process is of particular interest and constitutes a further feature of the present invention Thus there is provided a process for the preparation of compounds of formula I as hereinbefore defined which comprises reacting a compound of the formula :II or an O-acetyl derivative thereof,which an appropriate hydroxyalkylating agent,for example,a compound of the formula :R-X (wherein R is as hereinbefore defined and X represents an atom or group removable an anion) followed,where necessary,by hydrolysis of any unwanted O-acetyl groups whereby a compound of formula I as hereinbefore defined is obtained Thus,for example the compound of formula I in which R represent a 2-hydroxyethyl group may be prepared by reaction of the compound of forumla II with 2-chloroethanol preferably in the presence of propylene glycol with,for example,sodium methoxide as base Similarly the compound of formular I in which R represent a 2,3-dihydroxypropyl group may,for example,be prepared by reaction of a compound of formular II with 3-chloropropan-1,2-diol preferably in the presence of propylene glycol with,for example,sodium methoxide as base the compound of II may be prepared in any convenient manner ,for example,by reaction of 5-acetamido-2,4,6-triiodoisophthaloyl chloride and/or 5-diacetylamino-2,4,6-triiodoisophthaloyl chloride with 2,3-dihydroxypropylamine followed,where 5-diacetyl is used by removal of one N acetyl group,e.g.by alkaline hydrolysis at slightly elevated temperature.The reaction may ,for example,be effected in the presence of dimethylformamide or dioxan as solvent,conveninetly in the additional presence of an alkali metal or alkaline earth metal carbonate or bicarbonate such as potassium bicarbonate |
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xiaohanhan2007 
捐助贵宾 (小有名气)
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【答案】应助回帖
szf19900508(金币+60, 翻译EPI+1): 十分感谢 2011-11-27 16:33:13
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化学式I中化合物的R代表CH2CHOHCH2OH基团，（1）在鼠中的静脉毒性为23400mg I/Kg，而脑毒性大于1500mg I/Kg （2）在兔中的肾毒性大于10500 mgI/Kg （3）可形成至少400-500 mg I/ml的高浓度溶液 （4）具有低粘度，在浓度均为为300mg I/ml的情况下，37oC.时的粘度为6.2cP，而20oC时的粘度为12.6cPa；（4）在浓度为为300mg I/ml时，具有低渗透压，通过冰点法测定为0.65Os/Kg。 此发明的放射性成分可通过一个公式简单表达，适合在诸如安瓶和小药水瓶内的注射管理。例如，安瓶和小药水瓶的容量为5至300 ml，则化合物浓度为20至500 mg I/ml。 此发明中的化合物可通过简单的方法制备，但以下的方法会特别令人感兴趣并进一步形成了此发明的特色所在。 因此，制备化学式I中化合物的过程包括与化学式II中的化合物进行反应，或者与乙酰衍生物反应，该衍生物是合适的羟烷基化试剂，例如，可在必要时水解R-X型（R已在此前定义过，而X代表一个可离去一个原子或基团的阴离子）化合物中任何不需要的乙酰基，从而得到化学式I中的化合物。 因此，例如，化学式I中以R代表2-羟乙基的化合物可通过将化学式II中的化合物与2-氯乙醇反应，最好是有丙二醇和甲醇钠存在时制备而得。 相似地，以R代表2,3-二羟丙基的化学式I中的化合物可通过将化学式II中的化合物与3-氯丙烷-1,2-二醇反应，最好是有丙二醇和甲醇钠存在时制备而得。 化学式II中的化合物可通过将5-乙酰氨基-2,4,6-三碘异酞酰氯与/或5-二乙酰氨基-2,4,6-三碘异酞酰氯与2,3-二异丙醇胺而简便制得，其中5-二乙酰基被用于N乙酰基的解离，例如可在略高的温度下进行碱解。此反应在试剂如二甲基甲酰胺或二氧六环，尤其是碱金属或碱土金属的碳酸盐或碳酸氢盐如碳酸氢钾存在时会受到影响。 |
2楼2011-11-27 14:48:59
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