Abstract: 1-Carbapenam-2-one-3-carboxylic acid and 1-carba-3-hydroxy-3-cephem-4-carboxylic acid and esters thereof are provided by a process comprising a rhodium C.sub.2 -C.sub.10 carboxylate catalyzed cyclization of an ester of a 4-(1-alkoxy- or 1-substituted alkxoy)-2-oxo-4-azetidinyl)-.alpha.-diazo-.beta.-ketobutyric acid and an ester of a 5-(1-alkoxy- or 1-substituted alkoxy-2-oxo-4-azetidinyl)-.alpha.-diazo-.beta.-ketovaleric acid respectively. The process is carried out in an inert organic solvent at a temperature between about 15.degree. C. and about 85.degree.0 C. The 1-carba bicyclic .beta.-lactams are intermediates for preparing antibiotics.

Abstract: A molding system utilizes a cold mold with a large thermal mass and contoured thin mold inserts with a low thermal mass. A composite sheet blank of glass fibers in a thermoplastic matrix resin is placed between the inserts, heated and then transported to the cold mold. The composite sheet is pressed in the cold mold between the mold inserts to flow form and then cool the part. The mold inserts keep the surfaces of the composite sheet hot during the forming process, thereby enabling the matrix resin to flow and form smooth surfaces.

Abstract: A method of passively shimming a magnet having a central bore using ferromagnetic shims is provided. The field strength in the bore of the magnet is measured at a predetermined number of points. The field inhomogeneity is determined from the measured field strengths. The fields created by a single shim of known size when positioned, at different predetermined positions in the bore of the magnet is determined. The shim locations in the bore of the magnet and shim size are determined using a linear programming solver to minimize the field inhomogeneity and the total amount of shims used. The shim sizes are determined based on the measured field in the bore of the magnet and the field created by a single shim when positioned at a predetermined number of locations. The shim size at the appropriate locations are adjusted to the determined values and the field strength of the magnet is again measured at the predetermined points.

Abstract: An actively shielded refrigerated superconductive magnet is provided. The magnet includes a generally cylindrical vacuum vessel having an axially extending bore. A plurality of superconductive main coils are positioned in the vacuum vessel concentrically surrounding and spaced away from the bore. A pair of superconductive shield coils having a larger diameter than the superconductive main coils are situated in the vacuum vessel, concentric with the superconductive main coils. The superconductive shield coils are situated at either end of the superconductive main coils. The superconductive shield coils and the superconductive main coils are electrically connected to one another so that the superconductive shield coils and the superconductive main coils are capable of carrying current in opposite circumferential directions. A thermal shield encloses the superconductive main and shield coils, with the thermal shield spaced away from the vacuum vessel and superconductive main and shield coils.

Abstract: A multilayer mold for use in blow molding parts within short cycle times is provided. The multilayer mold has a hard skin layer, an insulating layer and a base containing cooling means. The transient temperature increase of the skin layer of the mold as a hot parison contacts the mold is used to produce smooth surfaces on parts since the skin layer remains hot during parison inflation.

Abstract: This invention provides an improvement in the large scale processing of vancomycin which comprises the quiescent precipitation of vancomycin base from an aqueous solution of a pH of at least about 7.8.

Abstract: An upper contoured die which mates with a lower contoured die is rotated relative to and against the lower die to progressively squeeze and deform a softened thermoplastic sheet. The two dies create sharp detail on both surfaces of the deformed sheet without tearing the sheet.

Abstract: A method of shimming a magnet having correction coils is provided. The field strength in the bore of the magnet is measured at a predetermined number of points. The field inhomogeneity is determined from the measured field strengths. The field created by a fixed current in each shim coil operating alone, at each of the predetermined points is determined. The shim correction coil currents are determined using a linear programming solver to minimize the field inhomogeneity and the correction coil currents. The correction coil currents are determined based on the measured field in the bore of the magnet and the field created by each of the shim coils when carrying a fixed current, with the correction coil currents each constrained to a maximum value which is adjusted for the current in the correction coils when the field strength was measured. The correction coils are adjusted to the determined values and the fields strength of the magnet is gain measured at the predetermined points.

Abstract: A process for forming a thermoplastic resin coating on glass fibers comprises heating a thermoplastic resin powder until molten and applying it to the glass fibers. The coated fibers can then be heated and drawn into a desired shape which also removes resin. Then the coated fibers are cooled to make a preform. The coated fiber preform can then be molded. Several resin layers with glass fibers of varying lengths can be deposited to make a graded preform. Apparatus for forming a thermoplastic resin on glass fibers sprays hot thermoplastic powder on the glass fibers. The coated fibers can then be heated such as by IR lamps and then drawn through a die which has a spigot to remove excess plastic. Alternately, a plurality of plastic and glass fiber layers can be deposited on a veil.

Abstract: Monocyclic .beta.-lactam compounds represented by the formula ##STR1## wherein R.sub.1 is H, NH.sub.2, acylamino, C.sub.1 -C.sub.4 alkyl, etc.; R.sub.2 is e.g. C.sub.1 -C.sub.4 alkyl, hydroxyalkyl, aminoalkyl, carboxy, esterified carboxy, esterified carboxyalkyl, or carboxyalkyl; and R.sub.3 is hydrogen, benzyl, substituted benzyl, pivaloyl, --SO.sub.3 M, or --P(C.dbd.O)(OM')2; are obtained by the cyclization of an O-substituted hydroxamate of a .beta.-substituted alkylcarboxylic acid. For example, .alpha.-ethylmalic acid monobenzyl ester is reacted with O-benzylhydroxylamine to form the O-benzylhydroxamate of the free carboxy group, and the hydroxamate is cyclized with diethyl diazodicarboxylate and triphenylphosphine to form the .beta.-lactam of the above formula wherein R.sub.1 is ethyl, R.sub.2 is benzyloxycarbonyl and R.sub.3 is benzyl. The .beta.-lactam compounds are useful intermediates for preparing .beta.-lactamase inhibitors and monocyclic .beta.-lactam antibiotics and, when R.sub.3 is --SO.sub.

Abstract: A layer of a neat resin in powder form is deposited either on a mold surface or on a bulk thermoplastic composite fiber reinforced sheet. The resin layer is adjacent to an insulated wall of a compression mold. The bulk sheet is preheated and compression deformed with the powdered resin. The heat from the sheet flows to and melts the powder layer producing a resin rich layer. The insulated wall permits the heat of the sheet to be retained sufficiently to melt the powdered resin. In the alternative, the neat resin powder may be replaced with a preformed film of thermoplastic resin compatible with the sheet resin. A structural homogeneous integral molecular bond is formed between the neat resin layer and the sheet.

Abstract: An apparatus for installing shim guide rails in an MR magnet is provided including a plurality of beam members, one for every guide rail to be installed. A plurality of coaxial ring shaped members spaced apart from one another are joined together by the beam members. The beam members extend axially and are spaced circumferentially about the outer diameter of the ring shaped members forming a cylindrical open ended cage. Each of the beam members defines a plurality of radially extending spaced apart apertures. A plurality of ladder-like structures each of which is associated with a respective beam member is provided. Each of the ladder-like structures included two side pieces joined by a plurality of rungs extending between the side pieces. The rungs pass through the holes in the beam members with one of the side pieces situated inside the cylindrical cage and the other situated outside the cage.

Abstract: This invention provides a matrix composition for sustained drug delivery which is comprised of an active agent, a hydrophilic polymer and an enteric polymer. The enteric polymer is impermeable to gastric fluids and aids in retarding drug release in regions of low pH, thus allowing lower levels of hydrophilic polymer to be employed. At the pH range of intestinal fluids, this polymer will dissolve and thereby increase the permeability of the dosage form. This approach is useful in sustaining the release of numerous active agents whose solubility declines as the pH is increased, a characteristic of weakly basic drugs. By responding to changes in physiological pH, these sustained release dosage forms have acceptable performance, in spite of variability in the gastrointestinal transit times of the formulation.

Abstract: 3-Exomethylenecepham sulfoxide esters are obtained in improved yields via cyclization of 3-methyl-2-(4-chlorosulfinyl-2-oxo-3-acylamino-1-azetidinyl)-3-butenoic acid esters under anhydrous conditions with stannic chloride in the presence of both an oxo compound, e.g., an ether such as diethyl ether, a ketone such as acetone or methylethyl ketone, and an unsaturated compound, e.g., an alkene such as 1- or 2-hexene, a non-conjugated alkadiene such as 1,4-hexadiene, a cycloalkene such as cyclohexene, an allene, or a non-conjugated cycloalkadiene such as 1,4-cyclohexadiene.

Abstract: The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics represented by the formula ##STR1## wherein R is amino or protected amino, R.sub.1 is H or alkoxy, R.sub.3 is H or alkyl, Z is ##STR2## where R.sub.2 is, e.g., H, halogen, or alkyl, or --CH.sub.2 R.sub.2 ' where R.sub.2 ' is, e.g., hydroxy, methoxy, or heterocyclicthio group, and A is a carboxy-protecting group which comprises heating a 2-substituted-methylcephalosporin 1,1-dioxide of the formula ##STR3## wherein R, R.sub.1, R.sub.3, and A are the same as in the formula above and Y is a free radical precursor group, e.g., C.sub.1 -C.sub.6 --Se--, C.sub.1 -C.sub.6 --S--, or phenyl--Se--; with a free radical initiator, e.g., a trialkyltin hydride, radiation, or a cobalt I salophen. Also provided are free radical compounds formed as intermediates in the process.

Abstract: Epoxyimines, formed from epoxyaldehydes, react via cycloaddition with amino-protected glycyl halides to provide 3-protected-amino-4-(substituted oxiranyl)azetidinones represented by the formula ##STR1## wherein, e.g., R is protected amino; R.sub.1 and R.sub.2 is H, alkyl, phenyl, etc.; and R.sub.3 inter alia a nitrogen-protecting group. Chiral epoxyimines from chiral epoxyaldehydes induce high levels of asymmetric induction during the cycloaddition to provide substantially one diastereomer of the 3,4-disubstituted azetidinone. For example, the epoxyimine formed with (2R,3S)-2-formyl-3-phenyloxirane and 2,4-dimethoxybenzylamine is reacted with phthalimidoacetyl chloride to provide [3R,4R,4(2S,3S]-1-(2,4-dimethoxybenzyl)-3-phthalimido-4-(3-phenyloxiran-2- yl)-2-azetidinone.The epoxy-substituted azetidinones are useful intermediates for .beta.-lactam antibiotic compounds.

Abstract: Bicyclic pyrazolidinones which have antimicrobial and/or herbicidal properties are discussed. The use of these compounds in pharmaceutical compositions, herbicidal compositions, and methods for treating bacterial infections and controlling undesired plants is set forth.

Abstract: 7.beta.-Acylamino-3-alkoxycarbonyl-(and 3-keto)-1-carba(1-dethia)-3-cephem-4-carboxylic acids and derivatives and related 3-substituted compounds are provided as antibiotics useful for treating infections in man and animals. Pharmaceutical formulations comprising the antibiotics and intermediates a process for their preparation are provided. Exemplary compounds provided are 7.beta.-[D-(2-phenyl-2-aminoacetyl)amino]-3-methoxycarbonyl-1-carba(1-deth ia)-3-cephem-carba(1-dethia)-3-cephem-4-carb oxylic acid and 7.beta.-[2-(2-aminothiazol-4-yl)-2-methoxyimino-acetamido]-3-acetyl-1-carb a(1-dethia)-3-cephem-4-carboxylic acid.

Abstract: Gel-free concentrated aqueous formulations of vancomycin hydrochloride are provided which comprise the antibiotic salt at a concentration between about 12% and about 50% w/v and a gel-inhibiting compound, e.g., ethanol, at a concentration between about 1% and about 20% v/v. The gel-free formulations are especially useful in a freeze-drying process for preparing vancomycin hydrochloride as a dry flowable powder in bulk or in unit-dosage form.

Abstract: Azetidinone-2 intermediates represented by the formula ##STR1## wherein R is phenyl, phenoxy or thienyl, R.sub.1 is --CH.dbd.CH--COOR.sub.1 ' wherein R.sub.1 ' is an ester, e.g., benzyl; --CH.sub.2 CH.sub.2 COR.sub.2 wherein R.sub.2 is OH or imidazol-1-yl; --CH.sub.2 CH.sub.2 C(O)CH.sub.2 COOR.sub.1 ' where R.sub.1 ' is an ester, e.g., p-nitrobenzyl; and R', R" and R'" are C.sub.1 -C.sub.4 alkyl, aryl or aralkyl; are converted to 1-carba(dethia)cephalosporin antibiotics. Preferably, R is phenoxy and the 1-silyl group is dimethyl-t-butylsilyl. Also provided is 3.beta.-phenoxyacetylamino-4.beta.-(2-carboxyethyl)azetidinone, likewise useful in the preparation of 1-carbacephalosporin antibiotics.