69651-48-5Relevant articles and documents
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
-
Paragraph 00539, (2018/09/12)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
-
Paragraph 00254, (2017/06/12)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
Synthesis method of hydroxylamine imidazole cephalosporin propylene glycol drug intermediate D-alpha-tert-butoxy carbonyl amino-alpha-(4-hydroxyphenyl)-acetic acid
-
Paragraph 0014; 0015; 0006, (2016/12/01)
The invention provides a synthesis method of a hydroxylamine imidazole cephalosporin propylene glycol drug intermediate D-alpha-tert-butoxy carbonyl amino-alpha-(4-hydroxyphenyl)-acetic acid. The method comprises the following steps that (i), 200 ml of a propionitrile solution, 0.06 mol of D-(-)-hydroxy phenylglycine and 0.08 mol of sodium bromide are added into a reactor provided with a stirrer, a condensation backflow device and a thermometer, stirring speed is controlled to range from 160 rpm to 190 rpm, stirring time is controlled to range from 90 min to 120 min, 0.081-0.085 mol of tert-butoxycarbonylation bromine is added slowly in batches, solution temperature is controlled to range from 60 DEG C to 65 DEG C, reaction time ranges from 19 h to 20 h, 500 ml of a potassium bromide solution is added for dilution, ethidene diamine is used for carrying out extraction 6-8 times, extract is dehydrated with calcium chloride, pressure reduction distillation is carried out to steam solvent out, residues are added into a butanol solution, a solid is smashed and filtered to obtain D-alpha-tert-butoxy carbonyl amino-alpha-(4-hydroxyphenyl)-acetic acid. The mass fraction of the propionitrile solution in the step (i) is 55-65%, and the mass fraction of the potassium bromide solution in the step (i) is 35-40%.