Claims
- 1. A process for the preparation of 7(S)-chloro-7-deoxylincomycin-2-phosphoryl benzylate, said process comprising:
- treating protected clindamycin hydrochloride with phosphorous oxychloride in the presence of a suitable solvent to obtain a reaction mixture;
- adding benzyl alcohol to the reaction mixture; and
- subsequently adding water to the reaction mixture to obtain the product.
- 2. A process for the preparation of a compound having the formula: ##STR7## wherein X is hydrogen, loweralkyl, halo, loweralkoxy, nitro, --CF.sub.3 or phenyl, said process comprising: treating protected clindamycin hydrochloride with phosphorous oxychloride in the presence of a suitable solvent to obtain a reaction mixture; adding benzyl alcohol, unsubstituted or substituted with loweralkyl, halo, loweralkoxy, nitro, --CF.sub.3 or phenyl to the reaction mixture, provided that said benzyl alcohol is unsubstituted when X is hydrogen and when substituted, the substituent is the same as X; and subsequently adding water to the reaction mixture to complete the reaction.
- 3. The process of claim 2 wherein X is hydrogen, loweralkyl or halo.
- 4. The process of claim 3 wherein X is hydrogen.
- 5. 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.
Parent Case Info
This application is a division of application Ser. No. 07/234,717, filed 08/22/88, now U.S. Pat. No. 4,849,515.
US Referenced Citations (5)
Number |
Name |
Date |
Kind |
3487068 |
Morozowich et al. |
Dec 1969 |
|
3496163 |
Birkenmeyer et al. |
Feb 1970 |
|
3856943 |
Birkenmeyer et al. |
Dec 1974 |
|
3892729 |
Birkenmeyer et al. |
Jul 1975 |
|
4430495 |
Patt et al. |
Feb 1984 |
|
Divisions (1)
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Number |
Date |
Country |
Parent |
234717 |
Aug 1988 |
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