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A versatile synthesis of 2-substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepine-3-ones
Tetrahedron ( IF 2.1 ) Pub Date : 9 June 2003 , DOI: 10.1016/s0040-4020(03)00583-0
Karolien Van Rompaey , Isabelle Van den Eynde , Norbert De Kimpe , Dirk Tourwé

A mild and general strategy for the synthesis of 2-substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepine-3-ones is described. The seven-membered lactam is prepared by intramolecular amide bond formation from the intermediate amino acid, which is obtained either by reductive alkylation of a variety of amines with N-Boc,N-Me-ortho-formyl-Phe and Phth-ortho-formyl-Phe, or by reductive amination of a variety of aldehydes with N-Boc-ortho-aminomethyl-Phe.

中文翻译:

2-取代的4-氨基-1,2,4,5-四氢-2-苯并ze庚因-3-酮的通用合成

描述了合成2-取代的4-氨基-1,2,4,5-四氢-2-苯并ze庚因-3-酮的温和且通用的策略。七元内酰胺是通过从中间氨基酸,它是由各种与胺的还原性烷基化得到的任一分子内形成酰胺键制备Ñ -Boc,Ñ -Me--甲酰基Phe和Phth--甲酰基-Phe,或通过将各种醛与N -Boc-邻-氨基甲基-Phe还原胺化而制得。
更新日期:2017-01-31
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