- New adaptation diseases of cefoperazone medicinal preparation for treating endometritis and other gynecological genital tract infections
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The invention discloses new adaptation diseases of cefoperazone medicinal preparation for treating gynecological genital tract infections of gynecology department. The cefoperazone sodium provided bya specific raw material production process is extremely low in impurity content and remarkable in medicine effect, so that the quality of a preparation product is improved, the safety and effectiveness of the preparation product are guaranteed, and the invention provides the application of preparing the medicine for treating endometritis and other gynecological genital tract infections.
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Paragraph 0108; 0109; 0115-0126; 0141-0142
(2020/08/22)
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- 1/4 head spore Meng Duozhi sodium compound (by machine translation)
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The invention discloses 1/4 head spore Meng Duozhi sodium compound and its preparation method, each of the plurality of containing sodium molar spore Meng 1/4 mole water. The method of the invention for preparing the compounds of the spore Meng Duozhi sodium, low impurity content, good stability, and good fluidity, the moisture and small, with more extensive application prospects. (by machine translation)
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Paragraph 0025; 0026; 0029; 0030; 0033; 0034; 0037-0039
(2017/07/20)
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- 1/5 water cefamandole sodium compound
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The invention discloses a 1/5 water cefamandole sodium compound and a preparation method thereof. Each mol of cefamandole sodium compound contains 1/5 mol of water. The cefamandole sodium compound prepared by the method disclosed by the invention has low impurity content and good stability and has a wider application prospect.
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Paragraph 0029; 0030
(2017/07/20)
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- Preparation method of cefmetazole
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The invention relates to a preparation method of cefmetazole. The preparation method comprises the steps of adopting a one-pot method containing 7-ACA, 1-methyl-5-tetrazole-thione and chloroacetyl chloride, obtaining 7-DCT, then using seven-position methoxy groups of sodium methylate and tert-butyl hypochlorite, and obtaining methoxy cephalosporin mother nuclei which are shared mother nuclei. The cefmetazole can serve as four methoxy cephalosporin products, namely cefminox, cefmetazole, cephalosporin and cefotetan disodium, three steps are omitted, the processing steps are greatly shortened, cost is lowered, and the overall yield is raised to 70%.
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Paragraph 0024
(2016/10/10)
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- A novel synthetic route to 7-MAC from 7-ACA
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An efficient and practical seven-step procedure is described for the synthesis of (6R,7S)-benzhydryl-7-amino-7-methoxy-3-((1-methyl-1H-tetrazol-5-ylthio)methyl)-8-oxo-5-thia-1-aza-bicyclo [4.2.0]oct-2-ene-2-carboxylate (7-MAC, 3) with overall yield of 49?%. This synthesis features a convenient and highly selective method for the introduction of 7α-methoxy group to cephalosporin nucleus in 10 using MeOLi/t-BuOCl in THF.
- Xiong, Fei,Li, Gen,Song, Bo,Chen, Fen-Er,Zeng, Zhao-Sen
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p. 1019 - 1025
(2016/05/02)
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- Synthesis method of methoxy cephalosporin drug intermediate 7-MAC
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The invention provides a synthesis method of a methoxy cephalosporin drug intermediate 7alpha-methoxy-7beta-amino-3-(1-methyl-1H-tetrazole-5-methylthio)-3-cephem-4-diphenylmethyl carboxylate (7-MAC). The synthesis method comprises steps as follows: 7-aminocephalosporanic acid (7-ACA) is taken as a raw material, a side chain at a C-3 site and amino at a C-7beta site are modified firstly, oxidative rearrangement and reduction are performed after protection of diphenylmethyl at a C-4 site, a methoxy group is selectively introduced to a C-7alpha site, an amino protecting group is removed finally, and 7-MAC is obtained through 7-step reaction. According to the synthesis method of the methoxy cephalosporin drug intermediate 7-MAC, the defects that byproducts such as methyl mercaptan and the like are required to be removed while the methoxy group is introduced in the existing synthesis technology are overcome. Meanwhile, the synthesis method of the methoxy cephalosporin drug intermediate7-MAC does not adopt diazo compounds, and accordingly, danger such as explosion possibly caused by the diazo compounds is eliminated.
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Paragraph 0007; 0031; 0032; 0033
(2016/10/09)
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- Preparation method for sodium cefamandole
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The invention relates to a preparation method for sodium cefamandole. The preparation method comprises mixing 7-aminocephalosporanic acid, 5-mercapto-1-methyltetrazole and a catalyst boron trifluoride acetonitrile complex, heating and stirring for reacting, cooling and processing to obtain a compound 1; performing heating refluxing reaction on the compound 1 and a silanization agent until the solution is clear, adding N,N-dimethylaniline under protection of inert gas, and dropwise adding (D)-(-)-O-formylmandeloyl chloride for chloroformylation reaction, after the reaction is finished, adding water for hydrolysis, adjusting the pH value to 5.0-7.5 by using a sodium bicarbonate or sodium carbonate solution, separating out the organic layer, adding ethyl acetate into the water layer, and adjusting the pH value to 0.5-1.5, so as to obtain a cephamandole solution, performing decoloring and dewatering, then adding an organic solution of sodium isooctanoate or sodium acetate, and crystallizing to obtain sodium cefamandole. The preparation technology is simple and easy to realize, the obtained product is shallow in color grade, impurity is less, yield is high, and the solvent is easy to recover and reuse, and thus production cost is reduced.
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Paragraph 0024
(2017/02/23)
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- Cycloaddition reactions of cephalosporin compounds. XI [1]. 1,3-dipolar cycloaddition reaction of an exo-2-methylenecephem with diphenyldiazomethane
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In the 1,3-dipolar cycloaddition reaction of the exo-2-methylenecephem 6 with diphenyldiazomethane the initially formed pyrazolines decompose and spirocyclopropylcephalosporin formation takes place. The structure elucidation with 1H, 13C, ASIS and NOE nmr methods is also described.
- Pitlik,Jaszberenyi
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p. 461 - 464
(2007/10/02)
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- Process for preparing cephalosporin intermediates
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Processes for the preparation of stable, crystalline cephalosporin intermediates of the formula STR1 wherein X is HI or HCl, and Nu and Nu≈ are certain N-containing heterocyclic rings attached via a sulfur atom or a ring nitrogen atom, respectively, which are substantially free of the Δ2 isomer; processes for intermediates in the preparation of the above compounds; and processes for the preparation of broad-spectrum cephalosporin antibiotics.
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- Use of Bistrimethylsilylated Intermediates in the Preparation of Semisynthetic 7-Amino-3-substituted-cephems. Expedient Syntheses of a New 3-cephalosporin
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Several "one-pot" methods for conversion of 7-ACA (6) to a variety of 7-amino-3-(ammoniomethyl)- or 7-amino-3-methyl>cephalosporin derivatives via bistrimethylsilylated intermediates are presented.For example, bistrimethylsilylation of 7-ACA (6) in 1,1,2-trichlorotrifluoroethane (Freon TF) using HMDS and 3 mol percent TMSI, followed by treatment with 1.15 equiv of TMSI and subsequent reactions with tertiary alicyclic or heteroaromatic amines or heteroaromatic thiols, led to the desired products in good yields.Alternatively, novel reaction of the bistrimethylsilylated derivative 15 with amine/TMSI adducts in Freon TF at 35 deg C provided an alternative approach to some 7-amino-3-(ammoniomethyl)cephalosporins.The solvent dependence of Δ3/Δ2 isomer ratios in quaternization reactions of 11 with N-methylpyrrolidine is presented.Hypotheses for the explanation of experimental results observed on reaction of 15 in Freon TF with amine/TMSI adducts are presented.Acylation of 17 (X = Cl, I) with 8 in aqueous THF provided 18 (BMY-28142) as its sulfate salt in overall yields of 18percent and 43percent, respectively, from 7-ACA (6).
- Walker, Donald G.,Brodfuehrer, Paul R.,Brundidge, Steven P.,Shih, Kun Mao,Sapino, Chester
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p. 983 - 991
(2007/10/02)
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- Cephalosporin intermediates
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Stable, crystalline cephalosporin intermediates of the formula STR1 wherein X is HI or HCl and Nu and Nu≈ are certain N-containing heterocyclic rings attached via a sulfur atom or a ring nitrogen atom, respectively, which are substantially free of the Δ2 isomer; processes for, and intermediates in, the preparation of the above compounds; and processes for the preparation of broad-spectrum cephalosporin antibiotics.
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- Cephalosporin antibiotics
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Novel cephalosporin antibiotic derivatives.
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- Cephalosporin antibiotics
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Novel cephalosporin antibiotic derivatives.
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- Cephalosporin antibiotics
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Novel cephalosporin antibiotic derivatives.
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- Cephalosporin derivatives
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New cephalosporin derivatives of the formula: STR1 wherein one of A and A1 represents oxygen or sulphur and the other represents sulphur, R1 represents hydrogen, acetoxy, (5-methyl-1,3,4-thiadiazol-2-yl)thio or (1-methyl-1,2,3,4-tetrazol-5-yl)thio and R2 represents carboxy, or R1 represents a pyridinio radical and R2 represents the carboxylate ion, are therapeutically useful compounds possessing antibacterial properties.
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- 3-Heterothio derivatives of (carbamoylthioacetyl)cephalosporins
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3-Heterothio(carbamoylthioacetyl)cephalosporin derivatives of the general formula EQU1 wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, a salt forming ion or the group EQU2 R1 is hydrogen, lower alkyl, phenyl, thienyl, or pyridyl; R2 is lower alkyl or phenyl-lower alkyl; R3 is a five or six membered nitrogen, sulfur and/or oxygen containing ring system; and R4 is lower alkyl, phenyl or phenyl-lower alkyl; are useful as antibacterial agents.
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- 3-Heterothio derivatives of [(alkoxycarbonyl)oxyacetyl]cephalosporins
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3-Heterothio derivatives of [(alkoxycarbonyl)oxyacetyl]cephalosporins which have the formula SPC1 tri(lower Wherein R1 is hydrogen, lower alkyl, phenyl, phenyl-lower alkyl or certain heterocyclic groups; R2 is lower alkyl; R3 is hydrogen, lower alkyl, tri(lower alkyl)silyl, tri(lowe alkyl)stannyl, a salt forming ion, or EQU1 R is lower alkyl, phenyl, or phenyl-lower alkyl; R4 is a five-membered nitrogen and sulfur or oxygen-containing ring system; are useful as antibacterial agents.
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- Isothiourea substituted cephalosporin derivatives
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Novel cephalosporin and penicillin antibiotic derivatives.
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- 3-Heterothio[(oxyalkyl)thioacetyl]cephalosporin derivatives
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3-Heterothio[(oxyalkyl)thioacetyl] cephalosporin derivatives which have the formula EQU1 wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri (lower alkyl) silyl, a salt forming ion, or the group EQU2 R1 is hydrogen, lower alkyl, phenyl, thienyl or furyl; R2 and R6 each is hydrogen or lower alkyl; R3 and R5 is lower alkyl, phenyl or phenyl-lower alkyl; and R4 is a five- or six-member nitrogen and/or sulfur or oxygen-containing ring system; are useful as antibacterial agents.
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- 3-Heterothio derivatives of (α-thiocarbonylamino) cephalosporins
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3-Heterothio(α-thiocarbonylamino)cephalosporin derivatives of the general formula STR1 wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, tri(lower alkyl)silyl, trihaloethyl, a salt forming ion or the group STR2 R1 is hydrogen, lower alkyl, cyclo-lower alkyl, unsaturated cyclo-lower alkyl, phenyl, substituted phenyl or thienyl; R2 and R5 each is hydrogen or lower alkyl; R3 is a five or six membered nitrogen, sulfur and/or oxygen containing ring system; and R4 is lower alkyl, phenyl or phenyl-lower alkyl; are useful as antibacterial agents.
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