- Ampicillin sodium and sulbactam sodium pharmaceutical composition
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The present invention discloses an ampicillin sodium and sulbactam sodium pharmaceutical composition comprising sulbactam sodium and ampicillin sodium with the specific optical rotation of + 264 degrees to + 269 degrees, and the mass ratio of ampicillin sodium to sulbactam sodium is 2: 1. The ampicillin sodium and sulbactam sodium pharmaceutical composition is prepared from the sulbactam sodium and the ampicillin sodium with the particular specific optical rotation, the drug stability is improved, and drug safety is improved.
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Paragraph 0049; 0050
(2016/11/17)
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- A solvent crystallization method for preparing sodium ampicillin
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The invention discloses a method for preparing ampicillin sodium by a menstruum crystallization method. The method comprises the following steps: firstly, dissolving sodium 2-ethylhexanoate into methanol, controlling the temperature to 15 DEG C, adding ampicillin acid into dichloromethane, and dripping diisopropylamine for a dissolution reaction; adding a sodium 2-ethylhexanoate solution into a crystallization tank, then adding a dichloromethane liquation agent in a flowing manner, and adding a seed crystal for growing crystals in a standing manner; then adding the dichloromethane liquation agent for crystallization; controlling the crystallization temperature to 20-25 DEG C; controlling the flowing acceleration of the liquation agent to 100 ml/h; after the crystallization reaction is completed, discharging materials, filtering the discharged materials, and drying the filtered materials to obtain the ampicillin sodium. According to the method, the methanol solvent, in which the ampicillin sodium is easy to dissolve, is selected for use, and then the dichloromethane solvent is used for dissolving out products, so that the crystallization speed of the product can be controlled; in addition, measures of adding the seed crystal for growing the crystal, controlling the dissolving temperature and the crystallization temperature, controlling the flowing acceleration of the liquation agent and the like are taken, so that the crystallization speed can be controlled, the crystal nucleus of the product are enlarged and uniform, the product purity is high, the dissolving residue is low, and the quality is stable.
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Paragraph 0005; 0029-0033
(2017/05/04)
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- Protection of functional groups during reaction and their subsequent restoration
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In the process for preparing an organic compound of the formula in which X is an amino group, a hydroxyl group or a carboxyl group, and A' is the remainder of the molecule, from an organic compound of the formula in which A is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formula in which Z is --NH--, --O-- or a direct C--C bond, and R is a radical of the formula STR1 IN WHICH Y is a direct C--C single bond, the --CH=CH-- group or an arylene group, R1 to R4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, or R1 + r2 and R3 + R4 each independently completes a 5- or 6-membered carbocyclic ring, or R1 and R3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen, Thereby to protect X, then converting A -- Z -- COOR into a compound of the formula and then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporins.
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