80082-65-1Relevant articles and documents
Synthesis method of aztreonam monocyclic mother nucleus
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Paragraph 0046; 0050; 0051, (2019/06/13)
The invention discloses a synthesis method of an aztreonam monocyclic mother nucleus, and mainly relates to the technical field of pharmaceutical and chemical industry. The method comprises the stepsthat L-threonine is subjected to methyl esterification; terbutyloxycarbonyl anhydride is used for performing amino BOC protection; ammonia water is subjected to ammonolysis; under the catalysis of a solid basic catalyst, methyl-sulfuric-acyl reaction and sulfonation are performed; cyclization, deprotection and acidification are performed to obtain the aztreonam monocyclic mother nucleus. The raw materials are cheap and can be easily obtained; the yield is high; the cost is low; the synthesis method belongs to a green, energy-saving and environment-friendly practical technology.
Aztreonam primary ring synthesis method
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Paragraph 0019; 0040; 0041, (2017/08/25)
The invention discloses a synthesis method of an aztreonam main ring, which comprises the following steps: by using L-threonine as a raw material, carrying out amino protection, converting carboxyl group into amido sulfonic acid, carrying out cyclization reaction, and finally deprotecting to obtain the aztreonam main ring. The method is simple to operate and lower in cost, and the total yield is 48.7%. The produced aztreonam main ring is white solid powder, the specific rotatory power is -45 degrees, and the HPLC (high performance liquid chromatography) purity is 98.5% above. The quality of the product is high, and thus, the method is suitable for industrial production.
USEFUL COMBINATIONS OF MONOBACTAM ANTIBIOTICS WITH BETA-LACTAMASE INHIBITORS
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Page/Page column 98-99; 101-104, (2010/11/27)
A pharmaceutical composition, comprising a combination of an antibiotically active compound of the formula (I): with a ?-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another ?-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).