KR830003501A - Aminothiadiazolyl compound, preparation method thereof, pharmaceutical preparation containing the compound and use thereof - Google Patents

Abstract

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Description

Aminothiadiazolyl compound, preparation method thereof, pharmaceutical preparation containing the compound and use thereof

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Claims (1)

7β-amino in the compound of formula (II) by treating a compound of formula (II), wherein the 7β-amino group is optionally substituted by a group allowing acylation, with an acylating agent that introduces an acyl moiety of the carboxylic acid of formula Acylating the group, or reacting a compound of formula (IV) with a hydroxylamine of formula H ₂ NOR ₁ (V), or isomerizing a 2-cefem compound of formula (VI), or wherein Am is primary or 2 To prepare a compound of formula (I) representing a tertiary amino group, the compound of formula (II) is treated with a salt of thiocyanic acid or a diisothiocyanate ester or a compound of formula (X) representing hydrogen is thiocyanogen. Or by treating a compound of formula (I) with a nitrosizing agent to produce a compound of formula (I) wherein R ₁ represents hydrogen, or lower alkyl or cycloalkyl optionally substituted by R ₁ To prepare a compound of formula (I) representing a substituted carbamoyl, a hydroxyimino group in the compound of formula (If) with a residue R ₁ introducing agent, or to prepare a compound of formula (I) wherein R ₂ represents lower alkoxy. The mercaptanHR ₃ compound is introduced to form a lower alkoxy group at the α-position of the protected group (Ig) or to prepare a compound of formula (I) wherein R ₃ represents heterocyclylthio. to handle, or, R ₃ is or process the structural formula (Ii) compound to produce the structural formula (I) compound that exhibits an acyloxy as acylating agent R ⁴ is manufactured by the following structural formula (I) compound that free carboxyl as R ⁴ Is a structural formula (Ij) wherein R ⁴ represents an esterified carboxyl group by removing the carboxyl-protecting group and substituting with hydrogen in the compound of formula (Ij) In order to prepare a compound of formula (I) wherein Am is a primary, secondary or tertiary amino group by esterifying a 4-carboxyl group in the compound of formula (Ik), B) reacting with the primary or secondary amine Am-H or metal amides thereof and decomposing unwanted protecting groups in the resulting compounds, if desired, and converting the compounds with the resulting salt-producing groups to salts or salts formed To prepare a salt of these compounds having the 7β-aminothiadiazolyl acetamido-3-cepem-4-carboxylic acid compound of formula (I) and a salt-producing group, Way. In the above structural formula Am represents an optionally protected amino group R ₁ represents hydrogen, optionally substituted loweralkyl or cycloalkyl, or optionally N-substituted carbamoyl R ₂ represents hydrogen or lower alkoxy R ₃ represents hydrogen, acyloxy or heterocyclylthio R ⁴ represents an optionally protected carboxyl group. R ⁰ ₃ represents a moiety which may be substituted by a heterocyclylthio moiety R ₃ , Y is halogen. ※ Note: The disclosure is based on the initial application.