奥沙米特合成工艺的研究Studies on synthesis of oxatomide
刘翔,刘庭辉,刘百里
LIU Xiang 1; LIU Ting hui 2; LIU Bai li 3 (1 No.6 Hospital of Shenyang;
摘要(Abstract)：
以邻苯二胺为起始原料 ,经 4步反应合成了H1 组胺受体拮抗剂奥沙米特。作者研究了 4步反应的工艺条件 ,如合成化合物 5时 ,改变二苯甲醇与无水哌嗪的投料比 ;合成化合物 4时 ,文献缩合剂为氢氧化钾和相转移催化 ,改为乙醇钠为缩合剂 ;合成化合物 1时 ,溶剂由甲苯改为DMF ,使每步反应的收率都有所提高
Oxatomide was synthesized from o phenylenediamine with four improved steps. Compound 5 was synthesized in an improved ratio of diphenylmethanol and anhydrous piperazine. Compound 4 was synthesized with an improved condensing agent. Compound 1 was synthesized with an improved solvent. The yield of every step was increased.
关键词(KeyWords)：
奥沙米特;H1-组胺受体拮抗剂;合成
oxatomide; H 1 antagonist; synthesis
基金项目(Foundation):
作者(Authors):
刘翔,刘庭辉,刘百里
LIU Xiang 1; LIU Ting hui 2; LIU Bai li 3 (1 No.6 Hospital of Shenyang;
参考文献(References)：
- [1]RichardsDM ,BrogdenRN ,HeelRC ,etal.OratomideAreviewofitspharmacodynamicpropertiesandtherapeuticefficacy[J].Drugs,1984,27(3):210-231.
- [2]姚凤鸣,刘素梅.脑益嗪合成方法的改进[J].医药工业,1984,(4):41-42.
- [3]陈夏英.脑益嗪的合成[J].医药工业,1982,(10):4-5.
- [4]VerninG ,DomlogH ,SivC ,etal.Synthesisof1 alkyland1,3 dialkyl2 benzimidazolonesfrom1 alkyl2 ben zimidazolonesusingphase transfercatalgsistechnique[J].JHeterocyclChem,1981,18:85-87.
- [5]GomezParraV ,GimerezM ,SanchezF ,etal.PotentialH1 antihistaminicdrugs:synthesisof4[(2,3 dihydro2 oxo1H benzimidzol1 yl)alkoxycarbonyl]1(diphenylmethyl) pipeazinesbyselectivemonoalkoxy carbonylationofα,ω dichloroalkanesbyphase transfercatalysis[J].LiebigsAnnChem,1989,(6):539-544.
- [6]JilekJ,HolubekJ,SvatekE ,etal.Tricyclicanaloguesoftheantiallergicagentoxatomide:10(3(4(10,11 dihy dro5H dibenzo[a,d] cycloheptene5 yl)1 piperazinyl)propyl)1,3 dihydro2H benzimidazol2 oneandthere lated6,11 dihydrodibenzo[b,e]thiepin,4,9 dihydroth ieno[2,3 c]2 benzothiepin,and10,11 dihydrodibenzo[b,f]thiepinderivatives[J].CollectCzechChemCom mun,1988,53:870-883.
- [7]王立升,王国满,刘百里,等.奥沙米特的合成[J].中国医药工业杂志,1994,25(5):196-197.