초록

A method for the preparation of clindamycin phosphate by first preparing the novel intermediate, clindamycin phosphoryl benzylate. The method can be used to make other, structurally related compounds.

대표청구항 ▼

A process for the preparation of clindamycin phosphate, said process comprising: treating protected clindamycin hydrochloride with phosphorous oxychloride in a suitable solvent to obtain a reaction mixture; adding benzyl alcohol to the reaction mixture and subsequently adding water to complete the r

A process for the preparation of clindamycin phosphate, said process comprising: treating protected clindamycin hydrochloride with phosphorous oxychloride in a suitable solvent to obtain a reaction mixture; adding benzyl alcohol to the reaction mixture and subsequently adding water to complete the reaction and thereby obtaining protected clindamycin benzylate, hydrochloride; heating the protected clindamycin benzylate hydrochloride in the presence of an acid to obtain deprotected clindamycin hydrochloride; isolating the deprotected clindamycin benzylate hydrochloride; treating the deprotected clindamycin benzylate hydrochloride with a suitable base to obtain clindamycin benzylate free base; isolating the clindamycin benzylate free base; and treating the clindamycin free base with hydrogen gas in the presence of Pd/C catalyst in a suitable solvent to thereby obtain clindamycin phosphate.