摘要:
1. A METHOD FOR MAKING AROMATIC ETHER ANHYDRIDES OF THE FORMULAS,
1,3-DI(O=),(R-X-)-1H,3H-NAPHTHO(1,8-CD)-PYRAN
WHICH COMPRISES, (1) EFFECTING REACTION BETWEEN AN ALKALI METAL PHENOXIDE OF THE FORMULA
R-X-M,
AND A NITRO- OR HALO-SUBSTITUTED AROMATIC ANHYDRIDE SELECTED FROM COMPOUNDS OF THE FORMULAS,
1,3-DI(O=),Y-PHTHALAN
1,3-DI(O=),Y-1H,3H-NAPHTHO(1,8-CD)-PYRAN WHERE Y CAN BE NITRO, CHLORO, FLUORO, BROMO, OR IODO, (2) AND RECOVERING FROM THE RESULTING MIXTURE OF (1), AN AROMATIC ETHER ANHYDRIDE, WHERE M IS AN ION OF AN ALKALI METAL SELECTED FROM SODIUM, POTASSIUM, LITHIUM AND RUBIDIUM, AND R IS AN AROMATIC RADICAL HAVING FROM 6-13 CARBON ATOMS SELECTED FROM THE CLASS CONSISTING OF PHENYL, TOLYL, XYLYL, NAPHTHYL, ANTHRYL, AND HALOGENATED DERIVATES THEREOF, AND X IS A DIVALENT RADICAL SELECTED FROM -S- AND -O-. 1,3-DI(O=),(R-X-)-PHTHALAN
摘要:
THIS INVENTION RELATES TO THREE HERETOFORE UNSEPARATED ANTIBIOTIC SUBSTANCES GENTAMICIN C1, GENTAMICIN C2 AND GENTAMICIN C1A; TO THEIR NOVEL STRUCTURES AND TO METHODS BY WHICH THEY MAY BE SEPARATED, ONE FROM THE OTHER.
摘要:
Compounds having potent antimicrobial effects over Gram-positive bacteria and Gram-negative bacteria, a high stability to .beta.-lactamases and DHP-I and a high safety for the human body and a process for producing the same. Carbapenem compounds represented by the following general formula (I) or salts thereof: ##STR1## wherein the ring A represents a 3- to 7-membered non-aromatic ring containing at least one nitrogen atom and optionally having a substituent other than R.sup.6 ; R.sup.1 represents hydrogen or methyl; R.sup.2 and R.sup.5 are the same or different and each represents hydrogen or a protecting group of the hydroxyl group; R.sup.3 represents hydrogen or a protecting group of the carboxyl group; R.sup.4 represents hydrogen, lower alkyl or a protecting group of the amino group; R.sup.6 represents: (1) hydrogen, (2) lower alkyl, optionally substituted by an optionally protected hydroxy, carbamoyl, formimidoyl, acetimidoyl or ##STR2## wherein R.sup.7 and R.sup.8 are the same or different and each represents hydrogen, lower alkyl, or a protecting group of the amino group), or (3) a protecting group of the amino group or a protecting group of the imino group; and m is 0 or 1. These compounds have antimicrobial effects and are useful as a drug.
摘要:
1. PROCESS FOR PRODUCTION OF A 3-AMINOMETHYL-1-PHENYLISOCHROMAN WHICH COMPRISES CONVERTING A 1-PHENYL-3-ISOCHROMANCARBOXYLIC ACID TO THE CORRESPONDING CARBOXYLIC ACID CHLORIDE OR BROMIDE, REACTING THE HALIDE THUS FORMED WITH AMMOIA, A PRIMARY OR SECONDARY AMINE HAVING FROM 1 TO 12 CARBON ATOMS TO FORM THE CORRESPONDING CARBOXYLIC ACID AMIDE, AND REDUCING THE CARBONYL GROUP OF THE AMIDE
摘要:
A MULTI-STEP, STEREOSPECIFIC TOTAL SYNTHESIS OF STEROIDS UTILIZING INTERMEDIATES HAVING A CYANOALKYL A-RING PRECURSOR IS DISCLOSED. THE INITIAL STARTING MATERIALS FOR THIS PROCESS ARE THE RELATIVELY INEXPENSIVE AND COMMERCIALLY AVAILABLE REAGENTS Y-BUTYROLACTONE AND SODIUM CYANIDE. THE PROCESS IS SUITABLE FOR THE PREPARATION OF RACEMIC OR OPTICALLY ACTIVE, MEDICINALLY VALUABLE STEROIDS, PARTICULARLY 19-NORSTEROIDS. IT IS A FEATURE OF THIS PROCESS THAT CONDITIONS EMPLOYED DURING THE MULTIPLE STEP SYNTHESIS ARE SELECTED SO AS TO RETAIN THE NORMALLY LABILE NITRILE GROUP EVEN DURING HYDROGENATION AND HYDROLYSIS STEPS. IN THIS MANNER, IT IS POSSIBLE TO EMPLOY THE NITRILE GROUP AS AN A-RING PRECURSOR WITHOUT RESORTING TO PROTECTIVE GROUPS AS WAS HERETOFORE FOUND NECESSARY IN PREVIOUS STEROID TOTAL SYNTHESIS PROCESSES.
摘要:
THE REACTION OF 2-OXA-3-KETO ANDROSTANES WITH FORMALDEHYDE AFFORDS THE CORRESPONDING 4-METHYLENE DERIVATIVES, WHICH ARE REARRANGED BY TREATMENT WITH PALLADIUM CATALYST TO AFFORD THE CORRESPONDING 4-METHYL-$4 DERIVATIVES. BOTH THE 4-METHYLENE AND 4-METHYL-$4 COMPOUNDS ARE PHARMACOLOGICALLY ACTIVE AS IS EVIDENCE BY THEIR ANABOLIC AND ANDROGENIC PROPERTIES.
摘要:
THE COMPOUND 2,3,3A,9B-TETRAHYDRO-6-HYDROXY7,8-DIMETHOXY-2-N-PROPYL-5H-FURO(3,2 -C)BENZOPYRAN-5-ONE, OBTAINED BY FERMENTATION OF HELMINTHOSPORIUM MONOCERAS EXHIBITS ANTI-FUNGAL PROPERTIES.