- Preparation method of 5-mercapto-1H-tetrazole compound
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The invention relates to a preparation method of a 5-mercapto-1H-tetrazole compound shown in a formula (III), which comprises the following steps of: (1) dissolving disulfide in halogenated alkane, dropwise adding a chlorinating reagent at -5 to 0 DEG C, carrying out heat preservation reaction for 2-5 hours, and carrying out reduced pressure distillation at 5-10 DEG C to obtain chlorinated disulfide; (2) dissolving the chlorinated disulfide prepared in the step (1) in lower saturated monohydric alcohol, dissolving sodium azide in water, dripping a sodium azide solution at 20-30 DEG C, heatingto 50-65 DEG C after dripping, and carrying out heat preservation reaction for 2-5 hours; (3) evaporating the solution obtained in the step (2) at 40-45 DEG C under reduced pressure to remove the lower saturated monohydric alcohol, and adding halogenated alkane for extraction for three times to obtain a halogenated alkane extraction liquid; (4) concentrating and crystallizing the halogenated alkane extraction liquid prepared in the step (3), and filtering to obtain the 5-mercapto-1H-tetrazole compound. The preparation method has high yield, good product quality, convenient solvent recycling and low production cost.
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Paragraph 0034; 0036-0043
(2019/11/04)
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- Synthesis and biological properties of new 1β-methylcarbapenems having tetrazolothioether moiety
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The synthesis and biological activities of a series of new 1β-methylcarbapenems 1a-1 having tetrazolothioether moiety at C-5 position of pyrrolidine were described. Among these compounds, 1c showed the most potent antibacterial activity and advanced pharmacokinetics compared with imipenem and meropenem. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Shin, Kye Jung,Koo, Ki Dong,Yoo, Kyung Ho,Kim, Dong Chan,Kim, Dong Jin,Park, Sang Woo
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p. 1421 - 1425
(2007/10/03)
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- Synthesis of hydroxyethyltetrazolethiol and etherified intermediates therefor
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By heating an N-(2-hydroxyethyl)dithiocarbamate ester protected at its hydroxy group as an ether in the presence of an azide, the corresponding 1-(protected hydroxyethyl)-1H-tetrazole-5-thiol is obtained, and then, if required, deprotecting the etheric protection to give an industrially useful chemical, 1-(2-hydroxyethyl)-1H-tetrazole-5-thiol.
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- 7-[2-(2-Imino-4-thiazolin-4-yl)-2-(syn)-hydroxy-iminoacetamido]-cephalosporins
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Disclosed are 2-(syn)-hydroxyimino-acetamide derivatives of the formula: STR1 wherein Y is hydrogen, hydroxyl, an acyloxy, carbamoyloxy, a quaternary ammonium or a nitrogen-containing heterocyclic ring-substituted thio group; or pharmaceutically acceptable salts or esters thereof are useful as antibacterial agents. Also disclosed are processes for producing them.
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- 7-Substituted-3-aminoalkyl-, acylaminoalkyl-, or hydroxyalkyl-substituted heterocyclic thiomethyl-3-cephem-4-carboxylic acid derivatives and preparation thereof
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Cephalosporanic acid derivatives and preparation thereof having the following formula STR1 wherein R1 is hydrogen or acyl, and R2 is aminoalkyl-, acylaminoalkyl-, sulfoalkylaminoalkyl-, or hydroxyalkyl-substituted, N- or N and S-containing heterocyclic groups.
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- A new cephalosporin. SCE-963: 7-[2-(2-aminothiazol-4-yl)-acetamido]-3- [[[1-(2-dimethylaminoethyl)-1h-tetrazol-5-yl]-thio]methyl]ceph-3-em-4-carboxylic acid. Chemistry and structure-activity relationships
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The synthesis and the in vitro and in vivo antimicrobial activities of a series of 7-[2-(2-aminothiazol-4-yl)acetamido]cephalosporins (1) having varied 3-substituents, such as methyl, hydroxymethyl, acetoxymethyl, pyridiniomethyl and heterocyclicthiomethyls, are described. The derivates having five membered heterocyclicthiomethyls exhibited strong inhibitory activities against Gram-negative organisms including some strains od Escherichia coli and Proteus morganii which are insensitive to cefazolin and cephaloridine. Pronounced activities were noted with 7-[2-(2-aminothiazol-4-yl)-acetamido]-3-[[[1-(2-dimethylaminoethyl)-1H-tetra zol-5-yl]thio]methyl]ceph-3-em-4-carboxylic acid (1y;SCE-963).
- Numata,Minamida,Yamaoka,Shiraishi,Miyawaki,Akimoto,Naito,Kida
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p. 1262 - 1271
(2007/10/09)
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