Sankyo Company, Limited

Masami Fukushima

Hideo Nakao

Hiroaki Yanagisawa

Akiko Ando

Masao Arakawa

Process for preparing .beta.-lactam antibiotic substances useful as intermediate for various cephalosporin or penicillin derivatives, which comprises oxidation of 7-benzylideneaminocephem or 6-benzylideneaminopenam compounds capable of being converted to their quinoid forms by oxidation followed by reaction with lower alkanols.

Process for preparing beta-lactam antibiotic substances

Process for preparing 7-alkoxy cephalosporins useful as intermediates for various cephalosporin or penicillin derivatives which comprises reacting 7-benzylideneaminocephem or 6-benzylideneaminopenam compounds with a halide cation-producing compound in the presence of an alcohol and a base capable of forming a salt with a phenolic hydroxyl group or converting a phenolic hydroxyl group to phenolate ion.

Process for preparing alkoxylated derivatives of cephalosporin compounds

A process for introducing an alkoxy group into the 7.alpha.-position of a 7-amino-3-cephem-4-carboxylic acid derivative which comprises oxidizing a salt of 7-benzylideneamino-3-cephem-4-carboxylic acid derivative and reacting the product with an alkanol. The 7.alpha.-alkoxy-3-cephem-4-carboxylic acid derivatives obtained by the present invention are useful as intermediates for the synthesis of antibacterial agents.

Process for preparing 7 .alpha.-alkoxycephalosporin derivatives

Process for preparing cephalosporin derivatives

Nitrosourea derivatives represented by the formula ##STR1## wherein A represents a group of the formula B--Y-- in which B is an unsaturated 5- or 6-membered heterocyclic group which has the as hetero atom at least one nitrogen atom, an unsaturated 9-membered heterocyclic group which has as the hetero atom at least one nitrogen atom and a bicyclic fused ring or an unsaturated 10-membered heterocyclic group which has as the hetero atom at least one nitrogen atom and a bicyclic fused ring, the heterocyclic groups optionally having alkyl, alkoxy, hydroxyl, amino, hydroxyalkyl or halogen as ring substituent and Y represents a group of the formula --(CH.sub.2).sub.m -- in which m is an integer of 1 or 2, the group optionally having alkyl as a substituent; A group of the formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 may be the same or different and each represents a hydrogen atom or an alkyl group; or a group of the formula ##STR3## in which R's may be the same or different and each represents a halogen atom or an alkyl group, n is an integer of 0 to 3 inclusive and Z is an ethylene group which may be substituted with alkyl; and X represents a halogen atom and acid addition salts thereof. The Compounds of the present invention are prepared from the corresponding 2-halogeno-ethylurea derivatives by means of conventional nitrosation procedures and useful as an antileukemic drug for various types of leukemia.

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Tokyo, Japan

Masami Fukushima