2133-07-5Relevant academic research and scientific papers
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.
Practical asymmetric synthesis of an edivoxetine·HCl intermediate via an efficient diazotization process
Kopach, Michael E.,Heath, Perry C.,Scherer, Roger B.,Pietz, Mark A.,Astleford, Bret A.,McCauley, Mary Kay,Singh, Utpal K,Wong, Sze Wing,Coppert, David M.,Kerr, Mark S.,Houghton, Peter G.,Rhodes, Gary A.,Tharp, Gregg A.
, p. 543 - 550 (2015/04/27)
A convergent synthesis of (S)-(4-benzylmorpholin-2-yl)(morpholino)methanone methanesulfonate (1), a key regulatory starting material for edivoxetine·HCl, was developed at Eli Lilly & Company. This novel synthesis utilizes d-serine as the source of chirali
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.
A PROCESS FOR THE PREPARATION OF MORPHOLINO SULFONYL INDOLE DERIVATIVES
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Page/Page column 35, (2012/11/07)
The present invention relates to a process for the preparation of the compounds of formula (I) which are morpholino sulphonyl indole derivatives. The compounds of formula (I) are capable of inhibiting, modulating or regulating Insulin-Like-Growth Factor I
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.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 49, (2008/06/13)
Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
