WestCHEM, School of Chemistry, The Joseph Black Building, University of Glasgow , Glasgow G12 8QQ, United Kingdom.
J Org Chem. 2016 Aug 5;81(15):6697-706. doi: 10.1021/acs.joc.6b01357. Epub 2016 Jul 21.
Rapid access to allylic trichloroacetimidates bearing a 2-allylaminoaryl group from readily available 2-iodoanilines combined with a one-pot multibond forming process has allowed the efficient synthesis of a series of 5-amino-2,5-dihydro-1H-benzo[b]azepines. The potential of these compounds as synthetic building blocks was demonstrated by the preparation of a late-stage intermediate of the hyponatremia agent, mozavaptan.
从易得的 2-碘苯胺出发，通过快速获得带有 2-烯丙基氨基芳基的烯丙基三氯乙酰亚胺，结合一锅多键形成过程，高效合成了一系列 5-氨基-2,5-二氢-1H-苯并[b]氮杂卓。这些化合物作为合成砌块的潜力通过制备低钠血症药物莫扎伐普坦的晚期中间体得到了证明。
