摘要
用两种方法制得抗凝剂利伐沙班的中间体4-(4-氨基苯基)-3-吗啉酮(1):①溴苯相继与乙醇胺、氯乙酰氯反应得4-苯基吗啉酮,再经硝化、还原生成1,总收率约32%;②溴苯先硝化,再与乙醇胺反应得到2-(4-硝基苯胺基)乙醇,再经氯乙酰氯闭环、还原反应制得1,总收率约47%。
4-（4-Aminophenyl）-3-morpholinone is the key intermediate of anticoagulant rivaroxaban.Two synthetic routes were achieved from bromobenzene.One is that bromobenzene reacted with 2-aminoethanol to give 2-anilinoethanol,which was subjected to cyclization with chloroacetyl chloride,followed by nitration and reduction with an overall yield of about 32%.The other is that bromobenzene underwent a sequence of reactions of nitration, N-arylation,acylation,cyclization and reduction with an overall yield of about 47%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2011年第2期93-95,共3页
Chinese Journal of Pharmaceuticals
