Simon L, Fülöp F, Bernáth G, Argay G, Kálmán A, Sohár P
Szent-Gyorgyi Albert Orvostudomanyi Egyeten, Gyogyszerkemiai Intezet, Szeged.
Acta Pharm Hung. 1996 May;66(3):111-8.
trans-Perhydro-1,4-benzoxazepin-3-ones 2a-e were synthesized and transformed to condensed-skeleton perhydro-trans-1,4-benzoxazepines 3a,b, the thiones 4a,b, the urea derivatives 5a,b, and N-acylated compounds 6a-e. Compounds 6b,d were ring-opened by hydrochloride acid in ethanol to yield trans-2 (1-carbethoxyethoxy)-1-(acylaminomethyl)-cyclohexane derivatives 7b,d. The 1H- and 13C-nmr investigation and X-ray analysis of 5b and 6c,d proved that the expected N-acylated derivatives were formed and that both rings of the annolated compounds have a chair conformation.
合成了反式全氢-1,4-苯并恶唑-3-酮2a - e，并将其转化为稠合骨架的全氢反式-1,4-苯并恶唑3a、b、硫酮4a、b、脲衍生物5a、b和N-酰化化合物6a - e。化合物6b、d在乙醇中被盐酸开环，生成反式-2-(1-乙氧羰基乙氧基)-1-(酰氨基甲基)-环己烷衍生物7b、d。对5b和6c、d进行的1H-和13C-核磁共振研究以及X射线分析证明，形成了预期的N-酰化衍生物，并且稠合化合物的两个环均具有椅式构象。
