A practical synthesis of 1, 3, 4, 14b??tetrahydro??2??methyl??10H??pyrazino??[1, 2??a] pyrrolo [2, 1??c][1, 4] benzodiazepine (1: 1) maleate

…, G Fitchett, JWF Wasley, G Zaunius

Index: Boyer; Fitchett; Wasley; Zaunius Journal of Heterocyclic Chemistry, 1984 , vol. 21, # 3 p. 833 - 835

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Citation Number: 12

Abstract

Abstract A practical synthesis of the anti-depressant, 1, 3, 4, 14b-tetrahydro-2-methyl-10H- pyrazino [1, 2-a] pyrrolo-[2, 1-c][1, 4] benzodiazepine (1: 1) maleate (Aptazapine 10) is reported in seven steps and approximately 20% overall yield. The key step of the synthesis was the formation of the tricyclic intermediate methyl 10, 11-dihydro-5H-pyrrolo [2, 1-c][1, 4] benzodiazepine-11-carboxylate (7) via a “Pictet-Spengler” type condensation of o- ...

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