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Detour of prenostodione synthesis towards pyrazolones for antibacterial activity.

Abstract：

:Our attempts to prepare indolyl acid (3), enroute to prenostodione (2), from phenyl-hydrazine following a reported procedure of Fischer-Indole synthesis rather lead to ethyl 2-(5-oxo-1-phenyl-2,5-dihydro-1H-pyrazol-3-yl)acetate as a major product, which underwent facile condensation with aldehydes to provide the pyrazolones. Intrigued by the opportunity for the diversity oriented synthesis of substituted pyrazolones, we have developed a facile one pot approach for pyrazolones and screened for antibacterial activity and, herein, results are reported.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Rasapalli S,Fan Y,Yu M,Rees C,Harris JT,Golen JA,Jasinski JP,Rheingold AL,Kwasny SM,Opperman TJ

doi

10.1016/j.bmcl.2013.03.123

subject

Has Abstract

pub_date

2013-06-01 00:00:00

pages

3235-8

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00451-4

journal_volume

23

pub_type

杂志文章

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