A new, easy access to the 6-aminoperhydro-1,4-diazepine scaffold under ultrasound and microwave irradiation.

[摘要]：A novel, efficient, and rapid synthesis of the 6-aminoperhydro-1,4-diazepine scaffold is reported. It was promoted by microwave or sequential ultrasound/microwave irradn. under solvent-free conditions or in soln. Protected ethylenediamine derivs. and N-Boc-serinol dimesylate underwent rapid cyclization to give 6-aminoperhydro-1,4-diazepines in excellent yields and with high selectivity, whereas the same reaction failed or gave negligible yields under conventional heating. Cs or K ions catalyzed the ring closure by coordinating the sulfonamide groups. All relevant work reported to date in the literature mostly concern about the syntheses of either 1H-tetrahydro-1,4-diazepine-2,5-dione or substituted 1,4-benzodiazepines, while the few published procedures for the prepn. of 6-aminoperhydro-1,4-diazepines involved several steps, required long reaction times and afforded low yields. By the present method, access to 6-aminoperhydro-1,4-diazepines becomes much easier and faster.

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