세팔로스포린 유도체의 제조방법
    22.
    发明授权
    세팔로스포린 유도체의 제조방법 失效
    制备CEPHOROSPORIN衍生物的方法

    公开(公告)号:KR1019890002216B1

    公开(公告)日:1989-06-23

    申请号:KR1019870001884

    申请日:1987-03-03

    Abstract: Cephalosporin derivs. (of formula (I), R1=C1-4 aliphatic alkyl) are new. Thus, suspend 7-amino-3-carbamoyloxymethyl-3cephem-4-carboxylic acid 2.73g into ethylacetate 75mL, add N-trimethylsyllylacetamide 5.20g at 30-35 deg.C with stirring (1.5 hr), cool to 1-3 deg.C, add 2-(fur-2-yl)-2-methoxyiminoacetic acid 1.86g, diphenyl-2-pyridon-1- yl-phosphate 3.77g and (Et)3N 1.53ml sequently at same temp. and stir for 3.5hr, add ethylacetate 80ml and water 80ml, adjust pH to 2.0 with 2N HCl and stir for 1hr at 0-5 deg.C to give 3- carbamoyloxymethyl-7-2-(fur-2-yl)2-methoxyiminoacetamide-ceph-3-em-4- carboxylic acid 3.86g (87.5% yield).

    Abstract translation: 头孢菌素衍生物。 (式(I),R1 = C1-4脂族烷基)是新的。 因此,将7-氨基-3-氨基甲酰氧基甲基-3-头孢烯-4-羧酸2.73g悬浮于乙酸乙酯75mL中,在30-35℃,搅拌(1.5小时)下加入5.20g N-三甲基甲酰基乙酰胺,冷却至1-3℃。 在相同温度下,依次加入2-(呋喃-2-基)-2-甲氧基亚氨基乙酸1.86g,二苯基-2-吡啶酮-1-基 - 磷酸酯3.77g和(Et)3 N 1.53ml。 并搅拌3.5小时,加入乙酸乙酯80ml和水80ml,用2N HCl将pH调节至2.0,在0-5℃下搅拌1小时,得到3-氨基甲酰氧基甲基-7-2-(呋喃-2-基)-2- 甲氧基亚氨基乙酰胺 - 头孢-3-烯-4-羧酸3.86g(收率87.5%)。

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