Ortho lithiation-in situ borylation of substituted morpholine benzamides
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
Morpholine amides are cheap and safe alternative to Weinreb amides as acylating agents of organometallic species. Herein, the in-situ lithiation/borylation of 18 ortho- meta- and para-substituted morpholine benzamides has been investigated. 10 of the 18 substrates provided the desired boronic esters as the major isomer (>90% regioselectivity) in crude isolated yields ranging from 68 to 93%. The synthetic usability of such building blocks was subsequently illustrated via the synthesis of a kinase inhibitor.
Originalsprog | Engelsk |
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Tidsskrift | Tetrahedron |
Vol/bind | 73 |
Udgave nummer | 12 |
Sider (fra-til) | 1576–1582 |
Antal sider | 7 |
ISSN | 0040-4020 |
DOI | |
Status | Udgivet - 23 mar. 2017 |
ID: 173700828