The present invention provides a method to improve the optical purity of 1-benzyl-3-aminopyrrolidine having a low optical purity using an inexpensive agent via a simple procedure. The present invention provides a method for improving the optical purity of 1-benzyl-3-aminopyrrolidine including the steps of converting 1-benzyl-3-aminopyrrolidine into an equimolar salt with an optically inactive acid, and recovering the salt as crystals. The present invention also provides a salt of 1-benzyl-3-amin...

Chemical intermediates which are of use in the production of quinolone carboxylic acid derivatives having antibacterial activity.

A compound of Formula (I) ##STR00001## and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.20 are each independently H, Cl, Br, F, I, CF.sub.3, OCF.sub.3, Me or Et; R.sup.4 is het or C.sub.3-7 cycloalkyl optionally substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, alkoxyalkyl containing 2 to 4 carbon atoms or --S--(C.sub.1-4 alkyl); a is 0 or 1; and het is a non-aromatic 4-, 5- or 6-membered heterocycle which contains at least one...

The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically the present invention relates to a novel quinoline(naphthyridine)carboxylic acid derivative represented by the following formula (I), which has an 4-aminomethyl-3-oximepyrrolidine substituent on 7-position of the quinolone nucleus and shows a superior antibacterial activity in contrast to the known quinolone antibactrial agents having a weak activity against gram-positive bac...

A process for the preparation of chiral 3-aminopyrrolidine and analogous bicyclic derivatives from dihydroxy olefins by treatment with titanium isopropoxide, an optically active tartrate ester and tert-butyl hydroperoxide, followed by subsequent alkylation of the intermediate with an alkyl or alkenyl magnesium halide, then pyrrolidine ring formation by condensation with an arylmethylamine, subsequent chiral replacement of a ring hydroxyl group with an amino group with further protection thereof,...

The invention is concerned with a process for making a compound of formula ##STR1## wherein R.sup.1 is hydrogen, alkyl, cyclo-alkyl, alkenyl, aryl or an amino protecting group; and R.sup.2, R.sup.3 each independently is hydrogen, alkyl, cyclo-alkyl, alkenyl or aryl; by reacting a compound of the formula ##STR2## wherein X is a protected hydroxy group; with R.sup.1 NH.sub.2 to form a compound of formula ##STR3## wherein X and R.sup.1 are described herein above; and then reacting the compound of f...

1-Aminopyrrolidine which is obtained by reacting hydrazine hydrate with a compound represented by the following formula (I): wherein X.sup.1 and X.sup.2 are the same or different, and each represents a leaving group, in methanol; and a process for producing 1-aminopyrrolidine, comprising the step of reacting hydrazine hydrate with the above compound represented by formula (I) in methanol.

A process for the preparation of enantiomerically homogeneous aminopyrrolidinyl naphthyridine carboxylic acids and quinolone carboxylic acids, and for the preparation of intermediates that are useful in the production of these carboxylic acids.

The present invention relates to process for the isolation of (-)-(S)-3-methylamino-4-methylenepyrrolidine derivatives of the formula: ##STR1## wherein R is hydrogen or amino-protecting group, from the racemic mixture of them comprising the salt formation of the racemate with L-(+)-tartaric acid in a molar ratio of 2:1 and subsequent treatment with a base, and optionally followed by deprotection of the amino-protecting group. By this process, complicated procedure in resolutional crystallization...

A novel process for preparing a stereospecific (S)-3-amino-1-substituted pyrrolidine used as a key intermediate in preparing quinolone and naphthyridone antibacterial agents where the 7-position is occupied with a sterospecific 3-amino-pyrrolidine side chain is described starting from inexpensive L-aspartic acid. L-aspartic acid is converted to the desired (S)-3-aminopyrrolidine via a novel, high yield transformation of a substituted aziridine.