| 摘要 |
<p>1,221,227. Novel penicillins; amino acid derivatives. BRISTOL-MYERS CO. 4 Sept., 1968 [5 Sept., 1967], No. 42095/68. Headings C2A and C2C. Novel penicillins having the formulae and the non-toxic pharmaceutically acceptable salts thereof are prepared by acylating 6-aminopenicillanic acid or a carboxylic acid salt thereof, with an acid of formula or a suitable acylating derivative thereof, wherein -NXY is a protected amino group, in an inert solvent at a temperature below 0‹ C., and subsequently removing the protecting group to produce a compound of Formula I and, if desired, further reacting with acetone at a pH of 5-9 at a temperature of - 20‹ to 50‹ C, to produce a compound of Formula II. The amino acid starting material of Formula III is prepared from the corresponding unprotected acid by known methods and suitable protecting groups specified are those wherein X is H and Y is benzyloxy carbonyl or 2,2,2-trichloroethoxycarbonyl or X and Y taken together represent the 2 - hydroxy - 1 - naphthylmethylene group. The D - (-) - 2 - (3 - chloro - 4 - hydroxyphenyl)- glycine is prepared by bubbling HCl gas through a solution of D-( - )-2-(p-hydroxyphenyl)glycine until the hydrochloride salt crystallizes out and treating the product with sulphuryl chloride. The D - ( - ) - 2 - (p - hydroxyphenyl) glycine is prepared according to the following reaction scheme: Pharmaceutical compositions comprise a compound of Formula I or II and a diluent or carrier.</p> |
