反应详情

A solution of diphenylmethyl 7-[(Z)-2-methoxyimino-2-(2-tritylaminothiazol-4-yl)acetamido]-3-iodomethyl-3-cephem-4-carboxylate [VIIa] (419 mg, 0.45 mmole) and 2-methoxycarbonylaminothiazolo[4,5-c]pyridine (94 mg, 0.45 mmole) in 2 ml of dry DMSO was allowed to stand at room temperature for 1 hour and diluted with ether to give 514 mg of crude quaternary salt, which was treated with 5 ml of TFA and 3 drops of anisole at room temperature for 30 minutes. The mixture was evaporated in vacuo and triturated with ether to afford 338 mg of crude Is which was purified on a column of HP-20 resin (40 ml) using 30% aqueous CH3OH as an eluant to give 95 mg (35%) of Is. Mp. 156°~184° C. (dec.). Estimated purity by HPLC: 40%.

1. customto give 514 mg of crude quaternary salt, which
2. customThe mixture was evaporated in vacuo
3. customtriturated with ether
4. customto afford 338 mg of crude
5. customwas purified on a column of HP-20 resin (40 ml)
6. customto give 95 mg (35%) of Is