Abstract: A process for producing optically active 16-substituted prostaglandins and new 16-substituted prostaglandins produced thereby which are useful as cardiovascular agents and as agents for inducing labor in pregnant females and for the termination of pregnancy.

Abstract: A total synthesis of canthaxanthin or dinor-canthaxanthin, known food coloring agents, from pentols.

Abstract: The present invention concerns compounds of the formula ##STR1## wherein X is hydrogen or halogen; R.sub.1 is hydrogen, halogen or trifluoromethyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 is hydrogen, --COO lower alkyl or CON(R.sub.4).sub.2 wherein R.sub.2 is lower alkyl or hydrogen and may be differentand the pharmaceutically acceptable salts thereof.Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formula illustrated above are useful as anxiolytics, anticonvulsants, muscle relaxants and sedative agents.

Abstract: The present invention relates to the conversion of the antibiotic mocimycin to the antibiotic known as X-5108 by treating mocimycin with a methylating agent after first protecting the 4-hydroxy functional group of the pyridone moiety, followed by subjecting the protecting group containing ester of X-5108 to mild basic hydrolysis whereby antibiotic X-5108 is obtained.

Abstract: L-3,4-dehydroproline is produced in good yield from D,L-3,4-dehydroproline by resolution via the tartaric acid salt and thermal racemization of the D-3,4-dehydroproline tartaric acid salt containing mother liquors.

Abstract: Derivatives of 5[2,5,7,8-tetramethyl-chromanyl]-pentane which are intermediates for Vitamin E.

Abstract: A process of isolating beta-lipoproteins from blood serum in about 99% purity comprising precipitating beta-lipoproteins from blood serum substantially free of chylomicrons with polyanethole sulfonate and a divalent cation, forming a solution of the beta-lipoproteins and reprecipitating them with the divalent cation, again forming a solution of said beta-lipoproteins and passing them through a DEAE cellulose column. The beta-lipoproteins purified by the method are particularly suited as a calibration standard for use in assays of the beta-lipoprotein content of blood serum.

Abstract: Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a "meso" type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids.

Abstract: Optically active organic compounds are prepared starting from optically inactive reactants by means of an optically active agent which influences the course of the reaction. In particular optically active compounds having a "meso" type carbon atom undergo an intramolecular ring closure in the presence of an optically active agent to yield an optically active product having one additional ring. The present process is particularly useful in the preparation of optically active bicyclic diketones which are important intermediates in the total synthesis of steroids.

Abstract: An improved solid phase peptide synthesis method is disclosed utilizing base labile N.alpha.-amino acid protecting groups. Such method provides a more efficient synthesis procedure in that it eliminates acid treatment thereby preventing loss of peptide from the support during each deprotection cycle and eliminates a substantial number of wash cycles in each step. A preferred base labile N.alpha.-amino protecting group is the 9-fluorenylmethyloxycarbonyl group (Fmoc) and a preferred base for deprotection is piperidine.

Abstract: Dienylphosphates of the formula ##STR1## wherein each of R.sub.1 and R.sub.1' is lower alkyl, aryl or benzyl and each of R.sub.2, R.sub.3 and R.sub.4 is hydrogen or lower alkyl,Are useful as anthelmintic agents and as intermediates for enolphosphates having anthelmintic activity.

Abstract: Epinephrine and norepinephrine type catecholamines can be individually assayed by immunoassay directed against the side chain common to these compounds by employing an oxidation procedure which selectively converts one or more of the epinephrine or norepinephrine type catecholamines to another compound which is not bound by the antibody. By measuring the difference between the total epinephrine or norepinephrine type catecholamine content and that after each of the oxidation steps, it is possible to determine the quantity of individual catecholamines of either type present in the original sample.

Abstract: The present invention relates to a new synthesis for the preparation of 5-(substituted benzyl)-2,4-diamino-pyrimidines, including new pyrimidine derivatives. More particularly, a new synthesis of ormetoprin, diaveridine and related compounds, including novel derivatives, is disclosed. The synthesis involves the condensation of a substituted benzene and an acrylonitrile derivative to directly give enol ether intermediates, which upon subsequent reaction by known techniques with guanidine, provides the desired 5-(substituted benzyl)-2,4-diamino-pyrimidines, including novel compounds. The pyrimidine end products are useful as potentiators of sulfonamides and as antibacterial agents.

Abstract: A synthesis of 2,6,10-trimethyl-undecan-1-ol, an intermediate for producing vitamin E, from methacrolein, crotonaldehyde, .beta.-hydroxy-isobutyric acid including intermediates in this synthesis.

Abstract: A sensitive radioimmunoassay for methaqualone and its major metabolites is described. Included within this disclosure is the preparation of novel methaqualone haptens, the preparation of antigens from such haptens by coupling to an immunogenic carrier material, the use of such antigens to elicit antibodies selective to methaqualone and its major metabolites and an improved radiolabelled derivative of a methaqualone analog used in the practice of said radioimmunoassay.

Abstract: Barbituric acid antigens are prepared by coupling 5- or 5,5-substituted barbituric acid to immunogenic carrier materials. In preferred embodiments, proteins are used as the carrier materials and the coupling is effected by an amide linkage between the 5-substituent of the barbituric acid and a carboxyl or amino group of the protein. The resulting antigens produce immunological effects when injected into host animals, including the formation of antibodies specific for 5- and 5,5-substituted barbituric acids. These specific antibodies are useful in bioanalytical techniques for the assay of barbituric acids in biological fluids.

Abstract: The invention relates to synthetic processes to produce the known pharmacologically active 9-methoxypsoralen. Also disclosed are various novel intermediates utilized in these processes.

Abstract: Novel 9-substituted phenyl-3,7-dimethyl-nona-2,4,6,8-tetraene derivatives useful as anti-tumor agents.

Abstract: The compound 5(3,12-dihydroxy-pregnan-20-yl)-pentanoic acid and 7-(3,12-dihydroxy-pregnan-20-yl)-heptanoic acid as well as ester and unsaturated derivatives thereof useful for decreasing the level of lipids such as cholesterol and triglycerides.

Abstract: This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C.sub.1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula ##STR2## in which R.sup.a represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C--R.sup.b wherein R.sup.b represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R.sup.3 represents a phenyl, halophenyl or 2-pyridyl group and acid addition salts thereof.