Luo Lingyan, S. Dongsheng, Zhou Zongzhou
2011
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Journal
Chinese Journal of Pharmaceuticals
Abstract
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%.