Title compds. [I; R1 = H, alkyl, dialkylaminoalkylene; X = alkylene, alkylenecarbonyl, 5-6 membered N-contg. heterocycle; R2 = aminocarbonyl, amino, (substituted) 5-6 membered N-contg. heterocycle; R1R2 = atoms to complete a (substituted) 5-6 membered heterocycle; W1 = Ph; W2 = OH; or both W1, W2 = Me; X1 = H, Me; X2 = H, Me, MeOCH2; when both W1, W2 = Me, then X1 = Me and X2 = H], were prepd. Thus, GE2270 factor A3 in DMF was treated with Et3N, DPPA, and serine (4-dimethylpiperidino)amide to give a condensation product which in THF was treated with Burgess reagent in CH2Cl2 followed by treatment with Me2CHOH and reflux to give I (NR1XR2 = 4-dimethylaminopiperidin-1-yl; W1 = Ph; W2 = OH; X1 = Me; X2 = MeOCH2). The latter had a min. inhibitory concn. of 0.5 μg/mL against Streptococcus pneumoniae L44.
Preparation of basic oxazolineamide derivatives of GE2270 and GE2270-like antibiotics / S. Lociuro, P. Seneci, R. Ciabatti.
Preparation of basic oxazolineamide derivatives of GE2270 and GE2270-like antibiotics
P. SeneciSecondo
;
1996
Abstract
Title compds. [I; R1 = H, alkyl, dialkylaminoalkylene; X = alkylene, alkylenecarbonyl, 5-6 membered N-contg. heterocycle; R2 = aminocarbonyl, amino, (substituted) 5-6 membered N-contg. heterocycle; R1R2 = atoms to complete a (substituted) 5-6 membered heterocycle; W1 = Ph; W2 = OH; or both W1, W2 = Me; X1 = H, Me; X2 = H, Me, MeOCH2; when both W1, W2 = Me, then X1 = Me and X2 = H], were prepd. Thus, GE2270 factor A3 in DMF was treated with Et3N, DPPA, and serine (4-dimethylpiperidino)amide to give a condensation product which in THF was treated with Burgess reagent in CH2Cl2 followed by treatment with Me2CHOH and reflux to give I (NR1XR2 = 4-dimethylaminopiperidin-1-yl; W1 = Ph; W2 = OH; X1 = Me; X2 = MeOCH2). The latter had a min. inhibitory concn. of 0.5 μg/mL against Streptococcus pneumoniae L44.
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