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ChemicalBook CAS DataBase List 2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate
89604-92-2

2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate synthesis

2synthesis methods
-

Yield:89604-92-2 92.6%

Reaction Conditions:

Stage #1:di(benzothiazol-2-yl)disulfide;(Z)-2-(2-aminothiazol-4-yl)-2-(1-tert-butoxycarbonyl-1-methylethoxy)iminoacetic acid with pyridine;triethylamine in acetonitrile at 21 - 30; for 0.833333 h;
Stage #2: with triethyl phosphite in acetonitrile at 21; for 5.5 h;Temperature;

Steps:

2 Example 2
At 21 ° C,35g cefotaxime side chain acid and 48gDMWas added to a mixture of dichloro and acetonitrile (the mass of the mixture was 250 g and the density was 1.0 g / cm 3)After stirring for 10 min,1.0 mL of pyridine was added,At 22 ° C, triethylamine (8.0 mL)After the addition was completed, the temperature was raised to 30 ° C., the reaction was incubated for 50 minutes, cooled,28 ml of triethyl phosphite was added dropwise at 21 ° C,Drop when the process of sharing 2.5h,After the addition was completed, the reaction was incubated at 21 ± 1 ° C for 3.0 h,Then cooled to 3 incubated reaction 30min, suction filtration,And dried at 60 to ceftazidime side chain acid active ester, the yield was 92.6%The content is 99.3%.

References:

Zibo Xinquan Pharmaceutical Services Co., Ltd.;Zhang Yanhong;Liu Chengxue;Zhang Liming CN106699683, 2017, A Location in patent:Paragraph 0028-0033

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2-Mercaptobenzothiazolyl-(Z)-(2-aminothiazol-4-yl)-2-(tert-butoxycarbonyl) isopropoxyiminoacetate Related Search: