78663-07-7Relevant articles and documents
Preparation method of ceftobiprole intermediate (R)-1-benzyl-3-aminopyrrolidine
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Paragraph 0022; 0035-0037; 0048-0050; 0061-0063, (2020/09/16)
The invention discloses a preparation method of a ceftobiprole intermediate, namely (R)-1-benzyl-3-aminopyrrolidine. The preparation method specifically comprises the following steps: with D-asparticacid as an initial raw material, carrying out amino protection, esterification, reduction, bromination cyclization and 3-amino protection removal successively to obtain (R)-1-benzyl-3-aminopyrrolidine. According to the method, the defects that raw materials for preparing (R)-1-benzyl-3-aminopyrrolidine are expensive, high temperature and high pressure are needed, precious metal is used for catalysis and the like in the prior art are overcome. All the materials used in the invention are cheap and easily available, so cost is low; and reactions can be carried out at normal temperature, so energyconsumption is low, industrial production is facilitated, and pollution is small.
Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents
Eswaran, Sumesh,Adhikari, Airody Vasudeva,Pal, Nishith K.,Chowdhury, Imran H.
supporting information; experimental part, p. 1040 - 1044 (2010/06/14)
A series of 26 new quinoline derivatives carrying active pharmacophores has been synthesized and evaluated for their in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv (MTB), Mycobacterium smegmatis (MC2), and Mycobacterium fortuitum following the broth micro dilution assay method. Compounds 13e, 13i, 13k, 14a, 14c, 14i, and 14k exhibited significant minimum inhibition concentrations, when compared with first line drugs isoniazid (INH) and rifampicin (RIF) and could be ideally suited for further modifications to obtain more efficacious compounds in the fight against multi-drug resistant tuberculosis.
Aqueous phosphoric acid as a mild reagent for deprotection of tert-butyl carbamates, esters, and ethers
Li, Bryan,Berliner, Martin,Buzon, Richard,Chiu, Charles K.-F.,Colgan, Stephen T.,Kaneko, Takushi,Keene, Nandell,Kissel, William,Le, Tung,Leeman, Kyle R.,Marquez, Brian,Morris, Ronald,Newell, Lisa,Wunderwald, Silke,Witt, Michael,Weaver, John,Zhang, Zhijun,Zhang, Zhongli
, p. 9045 - 9050 (2007/10/03)
(Chemical Equation Presented) Aqueous phosphoric acid (85 wt %) is an effective, environmentally benign reagent for the deprotection of tert-butyl carbamates, tert-butyl esters, and tert-butyl ethers. The reaction conditions are mild and offer good selectivity in the presence of other acid-sensitive groups, including CBZ carbamates, azetidine, benzyl and methyl esters, TBDMS, and methyl phenyl ethers. The mildness of the reaction is further demonstrated in the synthesis of clarithromycin derivative 4, in which a tert-butyl ester is removed in the presence of cyclic carbamate, lactone, ketal, acetate ester, and epimerizable methyl ketone functionalities. The reaction preserves the stereochemical integrity of the substrates. The reactions are high yielding, and the workup is convenient.
