Title of article
Synthesis and antibacterial activity of 2α-functionalized 1β-methylcarbapenems related to KR-21012
Author/Authors
Hyun J. Kwak، نويسنده , , Do K. Pyun، نويسنده , , Jae H. Kim، نويسنده , , Eun J. Kim and Michael Abberton، نويسنده , , Hee J. Jeong، نويسنده , , Bong J. Kim، نويسنده , , Cheol H. Lee، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
4
From page
333
To page
336
Abstract
The 2α-functionalized 1β-methylcarbapenems 3 were synthesized from the 2-formyl 1β-methylcarbapenem intermediate 5. The best compound in the series of 2α-(hydroxy)alkylcarbapenems, KR-21012, displayed well balanced in vitro and in vivo activity as a parent compound of oral carbapenem.
Scheme 1. Reagents and reaction conditions; (i) MnO2, CH2Cl2, reflux (70%); (ii) RMgX or RLi, THF or Et2O (50–75%); (iii) KF, n-Bu4NBr, →KF, n-Bu4NBr, AcOH, THF (80%); (iv) Pd(PPh3)4, SHE, THF (62%).
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790635
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