Abstract: Novel polymers having a linear backbone which is free from both branching and cross-linking, comprising quaternized nitrogen atoms linked to each other through trimethylene groups. By the term "linear backbone" is meant that the polymer has only acyclic groups, i. e. trimethylene, linking the nitrogen atoms in a single continuous chain; the polymer is free from "branching" when it has no repeating monomer units extending from the polymer backbone; and it is free from "cross-linking" when there is no joining of two linear backbones. These polymers are useful as antimicrobials, flocculating agents, antistatic agents, electroconductive agents for coating paper, chelating agents and bile acid binding agents, as well as in similar applications where their high charge to weight ratio and fully accessible nitrogen atoms can be employed. The polymers are obtained by the polymerization of dihydro-oxazine, reductive alkylation of the resulting polymer, followed by quaternization.

Abstract: The invention disclosed herein relates to a novel process for preparing the monomer, 3-[N-(3-chloropropyl)methylamino]-N,N,N-trimethyl-propan-1-aminium chlorid e, which comprises reacting N,N-bis(3-chloropropyl)methylamine with trimethylamine. The 3,3-ionene monomer thus obtained is a key intermediate for making the linear, unbranched, non-cross-linked polymer, poly-[{methyl-(3-trimethylammoniopropyl)imino}trimethylene dichloride], which is valuable as an oral bile acid sequestrant.

Abstract: The invention disclosed herein relates to antiandrogenic compositions active, in vivo, as inhibitors of the aggregation of mammalian blood platelets, and to the method of preventing, arresting or reversing blood platelet aggregation by the administration to mammals of such antiandrogenic compositions.

Abstract: The invention disclosed herein relates to novel partially cross-linked, fully quaternized poly-[(methylimino)trimethylene] polymers wherein a minor proportion (1% to 20%) of the nitrogen atoms in adjacent poly-[(methylimino)trimethylene] linear chains are, by quaternization, joined through trimethylene or 2-hydroxy-trimethylene bridges, the non-cross-linked nitrogens in the said linear chains being fully quaternized with lower alkyl or trialkylammoniopropyl groupings; and to the novel process for preparing these partially cross-linked, fully quaternized polymers which comprises reacting poly-[(methylimino)trimethylene] with 0.01 to 0.2 equivalents of 1,3-dihalo-propane or 1,3-dihalo-2-hydroxypropane per equivalent of tertiary amine in said poly-[(methylimino)trimethylene], and subsequently reacting the resulting product with excess alkyl halide or 3-halopropyltrialkylammonium halide.

Abstract: 3-Fluoro-D-alanine and its deutero analogs, which are potent antibacterial agents, are prepared from fluoropyruvic acid by asymmetric synthesis using an optically active amine such as D-.alpha.-methyl-benzylamine.

Abstract: The racemates of 2-deutero-3-fluoro-alanine and its salts are prepared by reductive amination of 3-fluoro-pyruvic acid, its hydrate or salts thereof, via the intermediate 2-imino-3-fluoro propionic acid salt, using alkali metal borodeuterides as reducing agents. The racemates thus obtained are valuable in the production of the corresponding 2-deutero-3-fluoro-D-alanine, and its pharmacologically acceptable salts, and derivatives thereof, which are potent antibacterial agents.

Abstract: 3-Fluoro-D-alanine, its pharmacologically acceptable esters, and pharmacologically acceptable salts of the foregoing, as well as other pharmacologically acceptable derivatives of 3-fluoro-D-alanine which, when administered clinically, are effective in releasing 3-fluoro-D-alanine in vivo, are potent antibacterial agents, and are prepared by fluorination of D-alanine with fluoroxyperfluoroalkanes or fluoroxypentasulfur in the presence of a free radical initiator followed by esterification and/or treatment with acids or bases.

Abstract: A process for preparing peptides containing lysine wherein the terminal amino group of lysine is protected by a pyridyl-4-methyloxycarbonyl group during formation of the peptide and removing this group with zinc in acid.

Abstract: Novel N-protected-.alpha.-amino acid compounds are disclosed in which the amino functionality is protected by a 1-methylcyclobutyloxycarbonyl or 1-methylcyclohexyloxycarbonyl. Processes for the synthesis of amino acids containing these protecting groups and the use of these novel amino acid compounds in the preparation of peptides are also disclosed.

Abstract: The invention disclosed herein relates to processes and intermediates useful in the preparation of certain 16-lower alkyl-1,4-pregnadiene compounds. It is particularly concerned with novel methods of preparing 16-lower alkyl-9.alpha.-fluoro-11.beta.,17.alpha.,21-trihydroxy-1,4-pregndiene-3,20 -dione and esters thereof, and with novel intermediates useful in these novel methods. It is further concerned with 16-lower alkyl-1,4,9(11)-pregnatriene-17.alpha.,21-diol-3,20-diones and their 21-lower alkanoates which, in addition to being valuable as intermediates, are valuable diuretic agents useful in the treatment of edema.

Abstract: Stabilized cycloserine compositions, having enhanced stability, and effective in releasing cycloserine compounds in vivo, are prepared by reacting D-4-amino-3-isoxazolidinone or its 5-methyl derivative with 2,4-pentanedione or alkyl-substituted-2,4-pentanedione to form the corresponding N-substituted-cycloserine compound in which one of the hydrogens attached to the primary amino group is replaced by 1-methyl-3-oxo-1-butenyl or an alkyl substituted-1-methyl-3-oxo-1-butenyl grouping.