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SHINKISEFUAROSUHORINJUDOTAIOYOBISONOSEIZOHO

机译:新塞弗阿罗斯霍林朱德带及其成因

摘要

NEW MATERIAL:A compound shown by formula I {R is (substituted) lower alkyl, lower alkenyl (with the proviso that 1-carboxy-1-vinyl is omitted), etc.; Q is group shown by formula II-IV [R1 is H or acetyl; R2 is H, carboxyl or carboxymethyl; Y is S or O; Z is S, O or (lower alkyl-substituted) imino]}. EXAMPLE:7beta-[2-(2-Aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-[5-( 3,4- dihydroxyphenyl)-1,3,4-oxadiazol-2-yl]thiomethyl-3-cephem-4-carboxylate sodium salt (syn isomer). USE:An antibacterial agent against gram-negative bacteria. PREPARATION:A compound shown by formula V [R3 is amino-protecting group; R4 is (substituted) lower alkyl, etc.; R5 is H or carboxyl protecting group; X is eliminable group] is treated with a compound shown by the formula HS-Q1 (Q1 is Q, etc.) to give a compound shown by formula VI, which is optionally deprotected.
机译:新材料:式I所示的化合物(R是(取代的)低级烷基,低级烯基(前提是省略了1-羧基-1-乙烯基),等等; Q为式II-IV所示的基团[R 1为H或乙酰基; R 2为H,羧基或羧甲基; Y是S或O; Z是S,O或(低级烷基取代的)亚氨基]}。实施例:7β-[2-(2-氨基噻唑-4-基)-2-甲氧基亚氨基乙酰胺基] -3- [5-(3,4-二羟基苯基)-1,3,4-恶二唑-2-基]硫代甲基-3 -头孢-4-羧酸钠盐(同分异构体)。用途:一种革兰氏阴性细菌的抗菌剂。制备:式V [R 3]所示的化合物为氨基保护基; R4为(取代的)低级烷基等; R 5为H或羧基保护基。 [X是可消除的基团]用式HS-Q 1所示的化合物(Q 1是Q等)处理,得到式VI所示的化合物,其任选地被脱保护。

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