摘要:
A process for preparing penem esters by reacting ##STR1## wherein R.sub.1 is a hydroxy protecting group and X is a C.sub.1 -C.sub.10 alkyl or aryl group, with ##STR2## wherein R.sub.2 is hydrogen or a C.sub.1 -C.sub.6 alkyl group in the presence of an anhydrous organic solvent, condensing the product with ##STR3## wherein X is a halogen atom or a --OCOOR.sub.3 group and then cyclizing.
摘要:
An efficient process for converting readily available 4-acetoxy-2-azetidinones to allyl 2-thioxopenam-3-carboxylates, intermediates useful for the synthesis of penem antibiotics.
摘要:
Sodium amoxycillin is obtained by spray drying a solution of sodium amoxycillin in aqueous isopropyl alcohol, wherein the initial ratio of isopropyl alcohol to sodium amoxycillin present in the solution to be spray dried is from 5:3 to 3:1 w/w.
摘要:
Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the general formula: ##STR2## in which R.sub.1 is a hydrogen atom or linear or branched C.sub.1 --C.sub.6 alkyl group, R.sub.2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1-6, Y is a 5- or 6-membered heterocyclic aliphatic group having 1 or 2 oxygen atoms in the ring thereof, and Z is a specific 5-substituted 2-oxo-1,3-dioxolen-4-yl group. Antibiotic compositions for oral administration are also described.
摘要:
The present invention is related to compounds which inhibit pancreatic cholesterol esterase. The compounds have the formula: ##STR1## wherein R.sup.1 is H or C.sub.1-6 alkyl;R.sup.2 is H or C.sub.1-6 alkyl;R.sup.3 is H or C.sub.1-6 alkyl;X is CHR.sup.6, S or O;R.sup.6 is H or C.sub.1-6 alkyl;R.sup.4 is a hydrophobic moiety; and pharmaceutically acceptable salts thereof.
摘要:
Disclosed is a process for preparing a .beta.-lactam compound represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy-substituted lower alkyl group or an amino group each of which may be protected; R.sup.2 represents hydrogen atom or an ester residue; X represents a methylene group which may be substituted by a lower alkyl group, sulfur atom or a group represented by the formula: --A--CH.sub.2 -- where A represents sulfur atom, oxygen atom or methylene group; and W represents an active ester residue of hydroxyl group, or a salt thereof, which comprises the steps of treating a 1-aza-3-thia-bicycloalkane compound represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 and X have the same meanings as defined above, or a salt thereof with a base in the presence of a desulfurizing agent and then reacting the resulting compound with an active esterifying agent of hydroxyl group.
摘要:
This invention relates to penicillanic acid derviatives of the formula I ##STR1## in which X stands for chlorine, bromine or iodine, to pharmaceutically acceptable, non-toxic salts of the compounds of formula I, to pharmaceutically acceptable, easily hydrolyzable esters thereof, including salts of such esters, to pharmaceutical compositions containing the compounds of the invention and dosage units thereof, to methods for the preparation of the compounds of the invention, and to methods of using the said new compounds in the human and veterinary therapy.The 6.beta.-halopenicillanic acids of formula I are potent inhibitors of .beta.-lactamases from a variety of gram-positive and gram-negative bacteria, making the 6.beta.-halopenicillanic acids as well as their salts and easily hydrolyzable esters valuable in human and veterinary medicine.
摘要:
A process for preparing halomethyl esters of penicillanic acid sulfone, intermediates to beta-lactamase inhibitors, from the corresponding substituted thiomethyl and sulfinylmethyl esters and a halogenating agent. The thiomethyl and sulfinylmethyl esters of penicillanic acid sulfone are useful intermediates.
摘要:
In-vivo hydrolysable esters of certain .alpha.-amino penicillins and cephalosporins have been rendered relatively tasteless by formulating into reconstitutable powders with a disodium or dipotassium salt of a di-carboxylic amino acid or tri- or di-sodium or -potassium phosphate, tartrate or citrate.
摘要:
The present invention is related to processes for the preparation of faropenem, which comprises treating the compound of Formula II, with an alkali metal salt of a substituted or unsubstituted C5-10 carboxylic acid and a catalytic amount of a palladium complex in the presence of an organic solvent, followed by the treatment of the reaction mixture of with water and a water miscible solvent, and isolating a hydrate of an alkali metal salt of faropenem from the reaction mass, wherein water is not removed from the reaction mixture in water treatment or isolation steps.