113359-04-9
113359-04-9 結(jié)構(gòu)式
基本信息
1-[[(6R,7R)-7-[(Z)-2-(5-氨基-1,2,4-噻二唑-3-基)-2-甲氧亞氨基乙酰胺基]-2-羧基-8-氧代-5-硫雜-1-氮雜雙環(huán)[4.2.0]辛-2-烯-3-基]甲基]咪唑并[1,2-b]噠嗪鎓氫氧化物內(nèi)鹽
1-[[(6R,7R)-7-[(Z)-2-(5-氨基-1,2,4-噻二唑-3-基)-2-甲氧亞氨基乙酰胺基]-2-羧基-8-氧代-5-硫雜-1-氮雜雙環(huán)[4.2.0]辛-2-烯-3-基]甲基]咪唑并[1,2-B]噠嗪氫氧化物內(nèi)鹽
sce2787
Cefozopran hydrochloride
1-[[(6R,7R)-7-[[2Z)-(5-Amino-1,2,4-thiadiazol-3-yl)(methoxyimino)acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]imidazo[1,2-b]pyridazinium Inner Salt
Firstci
SCE-1787
1-[[(6R,7R)-7-[[(2Z)-(5-Amino-1,2,4-thiadiazol-3-yl)(methoxyimino)acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-imidazo[1,2-b]pyridazinium hydroxide inner salt
Firstcin)
SCE-2787：Fastocin
制備方法
13g化合物(Ⅳ)和50ml三氟乙酸，在冰浴冷卻下攪拌，再在室溫下攪拌30min。濃縮，加入乙酸乙酯，再濃縮。往殘液中加入100ml乙醚，過濾收集產(chǎn)生的粉末，干燥，得10g化合物(V)，收率92%。
1.1g化合物(V)、1.0g咪唑并[1，2-b]噠嗪和1.1g碘化鉀溶于50%乙腈水溶液，在60--70℃下攪拌2h。冷卻，經(jīng)硅膠層析，以丙酮和80%丙酮水溶液洗脫。收集含產(chǎn)物的組分，濃縮。殘物經(jīng)MCl膠CHP 20P柱層析提純，以2%乙醇水溶液洗脫。收集含產(chǎn)物的組分，濃縮，凍干，得0.2g頭孢唑蘭，收率17%。
0.4g頭孢唑蘭溶于1.0ml 0.01mol/L鹽酸，經(jīng)Amberlite XAD-2層析，以0.01mol/L鹽酸-乙腈(1：9體積比)洗脫。洗脫液濃縮，加入丙酮，過濾收集產(chǎn)生的粉末，以小量丙酮洗，干燥，得0.25g鹽酸頭孢唑蘭。
常見問題列表
Cefozopran (SCE-2787) is a fourth-generation cephalosporin that has good activity against gram-positive organisms including methicillin-susceptible staphylococci, enterococci, and viridans group streptococci; and against gram-negative organisms including hemophilus influenza. Moreover, cefozopran has comparatively good activity against enterococci and P. aeruginosa , which are refractory to other cephalosporins.
Cefozopran (SCE-2787) (5-80 mg/kg; s.c.; twice a day for 5 days; four-week-old ICR male mice) is effective against acute respiratory tract infections caused by Kiebsiella pneumonia DT-S. In the model of chronic respiratory tract infection caused by K. pneumoniae 27, Cefozopran (20-80 mg/kg; s.c.; twice a day for 7 days; five-week-old CBA/J female mice) is as effective as Ceftazidime.