147528-20-9Relevant articles and documents
Generalized dipeptidomimetic template: Solution phase parallel synthesis of combinatorial libraries
Boger, Dale L.,Tarby, Christine M.,Myers, Peter L.,Caporale, Lynn Helena
, p. 2109 - 2110 (1996)
-
Multigram Synthesis of Heterabicyclo[n.1.0]alkan-1-yl Trifluoroborates
Kleban, Ihor,Krokhmaliuk, Yevhen,Reut, Sofiia,Shuvakin, Serhii,Pendyukh, Vyacheslav V.,Khyzhan, Oleksandr I.,Yarmoliuk, Dmytro S.,Tymtsunik, Andriy V.,Rassukana, Yuliya V.,Grygorenko, Oleksandr O.
, p. 6551 - 6560 (2021)
An approach to the synthesis of oxa- and azabicyclo[n.1.0]alkan-1-yl trifluoroborates on a multigram scale was developed. Two synthetic strategies were evaluated: the first based on the lithiation–borylation of the corresponding 2-bromoallyl derivatives, and the other relying on regioselective hydroboration of the appropriate hetera-substituted enynes. The second method appeared to be more efficient in terms of scalability and substrate scope. Further steps included ring closing-metathesis, mild palladium-catalyzed cyclopropanation with diazomethane, and reaction with KHF2 and furnished the title compounds in up to 50 g scale in a single run (10–41 % overall yield, 4–5 steps).
Palladium-catalyzed intermolecular [4 + 2] formal cycloaddition with (Z)-3-iodo allylic nucleophiles and allenamides
Yan, Fachao,Liang, Hanbing,Ai, Bing,Liang, Wenjing,Jiao, Luyang,Yao, Shuzhi,Zhao, Pingping,Liu, Qing,Dong, Yunhui,Liu, Hui
supporting information, p. 2651 - 2656 (2019/03/12)
A highly chemo- and regioselective [4 + 2] formal cycloaddition of (Z)-3-iodo allylic nucleophiles and allenamides catalyzed by palladium is reported. The methodology proceeds under mild reaction conditions and is tolerant of alkyl and aryl functional groups. The SN2′ substitution at the proximal C═C bond performed against the Heck or SN2 pathway delivered a variety of 2-amino-dihydropyrans and 2-amino-tetrahydropiperidines in moderate to satisfactory yields. The [4 + 2] formal cycloaddition derivatives are convertible to interesting scaffolds 2,6,7,7a-tetrahydropyrano[2,3-b]pyrrole and 2,6,7,7a-tetrahydro-1H-pyrrolo[2,3-b]pyridine derivatives via ring-closing metathesis (RCM) with Grubbs catalyst II.
Three-membered fused ring substituted amino six-membered ring derivative and medicine applications thereof relates to a three-membered fused ring substituted amino six-membered ring derivative as shown in the general formula
-
Page/Page column 33; 34, (2017/08/02)
The present invention relates to a three-membered fused ring substituted amino six-membered ring derivative and medicine applications thereof, and more particularly to a three-membered fused ring substituted amino six-membered ring derivative as shown in the general formula (I) or a stereoisomer of the derivative, a pharmaceutically acceptable salt, a prodrug, a medicinal composition containing the derivative and an application of the derivative to preparation of the medicine, namely a dipeptidyl peptidase IV(DPP-IV) inhibitor, wherein the definitions of the various substituents in the general formula (I) are the same as those in the specification.