PURPOSE: To obtain the subject compd. which is useful as a prodrug by reacting a cephem deriv. having a protected oxime with an inorg. acid or an aliphatic or an aromatic sulfonic acid.
CONSTITUTION: A compd. expressed by formula I (R2 is a protecting group) is reacted with a bis(benzothiazol-2-yl)disulfide expressed by formula II (R3 is H, a 1-6C alkyl, a 2-6C alkenyl or the like) and triphenylphoshine to obtain a compd. expressed by formula III. Then the obtd. compd. is reacted with a 7-aminoceph-3-em-4-carboxylic acid ester expressed by formula IV (R1 is a (1-5C)alkanoyloxy-(1-3C)alkyl, a (1-5C)alkoxycarbonyloxy-(1-3C)alkyl) to obtain a compd. expressed by formula V (the protected oxime is a syn-form). Then the compd. expressed by formula V is reacted with p-toluene sulfonic acid or the like in an org. solvent (e.g. n-propanol) at 20 to 110°C to obtain the objective compd. expressed by formula VI (X is an anion). The production of the final product is carried out in one step.
| WO/1993/011131 | CEPHALOSPORIN COMPOUNDS |
| WO/2007/086013 | FORMULATION COMPRISING OF CEFTAZIDIME, TAZOBACTAM AND LINEZOLID |
GERUTO FUITSUSHIYAA
UUBUE GERURAHA
RORUFU HEERURAIN
NORUBERUTO KURASU
RUUDORUFU RATORERU
URURITSUHI SHIYUTAAHE
TEEODOORU BUORUMAN
