2133-07-5Relevant articles and documents
Modular One-Step Three-Component Synthesis of Tetrahydroisoquinolines Using a Catellani Strategy
Qian, Guangyin,Bai, Miao,Gao, Shijun,Chen, Han,Zhou, Siwei,Cheng, Hong-Gang,Yan, Wei,Zhou, Qianghui
supporting information, p. 10980 - 10984 (2018/07/30)
Reported is a modular one-step three-component synthesis of tetrahydroisoquinolines using a Catellani strategy. This process exploits aziridines as the alkylating reagents, through palladium/norbornene cooperative catalysis, to enable a Catellani/Heck/aza-Michael addition cascade. This mild, chemoselective, and scalable protocol has broad substrate scope (43 examples, up to 90 % yield). The most striking feature of this protocol is the excellent regioselectivity and diastereoselectivity observed for 2-alkyl- and 2-aryl-substituted aziridines to access 1,3-cis-substituted and 1,4-cis-substituted tetrahydroisoquinolines, respectively. Moreover, this is a versatile process with high step and atom economy.
Observations on the modified wenker synthesis of aziridines and the development of a biphasic system
Buckley, Benjamin R.,Patel, Anish P.,Wijayantha
, p. 1289 - 1292 (2013/04/10)
A cheap and reliable process for the modified Wenker cyclization to afford aziridines has been achieved using biphasic conditions for a range of amino alcohol starting materials. A 100 mmol "one-pot" process has also been devised, and the enantiopurity of the starting amino alcohol is retained in the aziridine product.
METHODS OF USE FOR INHIBITORS OF AKT ACTIVITY
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Page/Page column 43, (2008/12/04)
Invented is the use of 1 H-imidazo[4,5-c]pyridin-2-yl compounds in the treatment of specified cancers.