| 摘要 |
<p>1465209 Clindamycin-2-phosphate derivatives UPJOHN CO 19 Nov 1974 [17 Dec 1973] 49949/74 Headings C2P and C2C The invention comprises compounds of Formula I and the acid addition salts thereof; where Halo is Cl, Br or I; X is -P(O)(OH) 2 , the zwitterion thereof or a partial salt thereof; R is C 1-4 alkyl and R 1 is C 1-8 alkyl; and their preparation by (1) protecting the 3- and 4-hydroxy groups in a corresponding compound in which X is H by reaction with an aldehyde or ketone to form an -ylidene group, (2) protecting the primary OH group by tritylation, silylation or formation of a 2-tetrahydropyranyl ether, (3) phosphorylation and (4) removal of protecting groups. In an example 1<SP>1</SP>- demethyl - 1<SP>1</SP> - (2 - hydroxyethyl)- clindamycin - 2 - phosphate hydrate (Formula I) is prepared by reacting 1<SP>1</SP>-demethyl-1<SP>1</SP>-(2- hydroxyethyl)clindamycin with acetone to give the corresponding 3,4-O-isopropylidene derivative, reacting this with trityl chloride to give the corresponding 1<SP>1</SP>-(2-trityloxyethyl) derivative, reacting this with pyridinium and cyanoethyl phosphate and then with aqueous acetic acid to give 1<SP>1</SP> - demethyl - 1<SP>1</SP> - (betahydrozyethyl)- clindamycin-2-cyanoethylphosphate and finally hydrolysing this ester. Antibacterial compositions for parenteral administration comprise a compound of the invention and a carrier.</p> |
