期刊
TETRAHEDRON
卷 68, 期 27-28, 页码 5606-5611出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2012.04.068
关键词
Benzodiazepines; Benzodiazepinones; Tetrazoles; Ugi reaction; TMS-N-3
资金
- National Institute of Health (NIH) [P41GM086190]
A two-step strategy for the synthesis of arrays of tricyclic tetrazolo-fused benzodiazepines and benzodiazepinones has been investigated. The protocol uses ortho-N-Boc phenylisocyanides and phenylglyoxaldehydes or ethyl glyoxylate in the four-component Ugi-azide reaction to afford MCR (MultiComponent Reactions) derived adducts equipped with the desired diversity inputs. A subsequent acidic treatment (TFA/DCE) allows a simultaneous deprotection-cyclization leading to the final products. (c) 2012 Elsevier Ltd. All rights reserved.
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