- A luer Ertapenem, luer he lateral chain and its preparation method
-
The invention discloses ertapenem and ertapenem side chains, as well as preparation methods of ertapenem and ertapenem side chains. L-hydroxyproline is protected by p-nitrobenzyl ester to obtain (2S,4R)-4-hydroxyl-1-(((4-Nitrobenzformyl)-oxyl)caboyl)pyrrolidine-2-carboxylic acid; then 4-nitro(1S,4S)-3-oxo-2-thia-5-azabicyclo[2.2.1]heptan-5-carboxylic anhydride can be obtained, and reacts with m-aminobenzoic acid p-nitrobenzyl ester to obtain ertapenem side chain III; and the ertapenem can be synthesized through two-step chemical reaction of condensation and deprotection to the ertapenem side chain III and a raw material MAP. An ertapenem side chain I (10), an ertapenem side chain II (13) and the ertapenem side chain III (2) which are prevailing in the market can be synthesized through simple steps, without the need of ultralow temperature, industrialization is easy, and the product purity is high, and the operation is simple and convenient.
- -
-
Paragraph 0143; 0144; 0145; 0146; 0147; 0148; 0149
(2017/07/14)
-
- Improved process for the preparation of carbapenem using carbapenem intermediates and recovery of carbapenem
-
The present invention relates to preparing carbapenem intermediates that are useful to produce Ertapenem, Meropenem and Doripenem; and provides an effective process for recovering ertapenem compounds.
- -
-
Page/Page column 9-10
(2011/12/03)
-
- Antibiotic compounds
-
The present invention relates to carbapenems and provides a compound of the formula (I): STR1 or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and are selected from hydrogen, halo, cyano, C1-4 alkyl, nitro, hydroxy, carboxy, C1-4 alkoxy, C1-4 alkoxycarbonyl, aminosulphonyl, C1-4 alkylaminosulphonyl, di-C1-4 alkylaminosulphonyl, carbamoyl, C1-4 alkylcarbamoyl, di-C1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4 alkylamino, di-C1-4 alkylamino, C1-4 alkanoylamino, C1-4 alkanoyl(N-C1-4 alkyl)amino, C1-4 alkanesulphonamido and C1-4 alkylS(O)n -- wherein n is zero, one or two: with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the --NR2 --. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
- -
-
-
