Synthesis of Bis-heteroaryls Using Grignard Reagents and Pyridylsulfonium Salts
作者:Alexandra M. Horan、Vincent K. Duong、Eoghan M. McGarrigle
DOI:10.1021/acs.orglett.1c03379
日期:2021.12.3
reported ligand-coupling reactions of Grignardreagents with pyridylsulfonium salts. The method has wide functional group tolerance and enables the formation of bis-heterocycle linkages, including 2,4′-, 2,3′-, and 2,2′-bipyridines, as well as pyridines linked to pyrimidines, pyrazines, isoxazoles, and benzothiophenes. The methodology was successfully applied to the synthesis of the natural products caerulomycin
本文报道了格氏试剂与吡啶基锍盐的配体偶联反应。该方法具有广泛的官能团耐受性,能够形成双杂环键,包括 2,4'-、2,3'-和 2,2'-联吡啶,以及与嘧啶、吡嗪、异恶唑连接的吡啶,和苯并噻吩。该方法成功地应用于天然产物 caerulomycin A 和 E 的合成。
nitrogenous heteroarenes remain a challenging undertaking - coordination of Lewis basic atoms into metal centers often necessitate elevated temperature, high catalyst loading, etc. Herein, we report a sulfur (IV) mediated cross-coupling amendable for the efficient synthesis of heteroaromatic substrates. Addition of heteroaryl nucleophiles to a simple, readily-accessible alkyl sulfinyl (IV) chloride allows
Pyrimidine derivatives as modulators of insulin-like growth factor-1 receptor (igf-i)
申请人:Barlaam Bernard
公开号:US20050054638A1
公开(公告)日:2005-03-10
The invention provides compounds of formula
in which R
1
, R
2
, R
3
and R
4
have the meanings defined in the specification; processes for the preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
Pyrimidine derivatives as modulators of insulin-like growth factor-1 receptor (IGF-I)
申请人:AstraZeneca AB
公开号:US07521453B2
公开(公告)日:2009-04-21
The invention provides compounds of formula
in which R1, R2, R3 and R4 have the meanings defined in the specification; processes for the preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
The invention provides compounds of formula
in which R
1
, R
2
, R
3
and R
4
have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.