Abstract: Process for the production of substituted 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acids having useful analgesic and anti-inflammatory activity.

Abstract: A process for preparing compounds of the formula ##STR1## in which R is hydrogen or methoxy,R.sub.1 is a hydroxyl group,R.sub.2 is chlorine, bromine, OCOCH.sub.3 or SHET,R.sub.3 is hydrogen or a cleavable carboxy-protecting group preferably selected from loweralkyl, benzyl, benzhydryl, loweralkoxyloweralkyl, loweralkoxybenzyl, phenacyl, trimethylsilyl, 2,2,2-trichloroethyl or pivaloyl,R.sub.4 is hydrogen or a cleavable acyl group, or R.sub.4 NH represents phthalimido, andHET is a five membered aromatic heterocycle containing 1-4 heteroatoms and optionally substituted with loweralkyl,and from which the corresponding 1-oxacephem derivtives can be prepared is described. The novel intermediate compounds of the formula 1 are produced from a penicillin derivative of formula 1 wherein R, R.sub.3 and R.sub.4 are as above described and R.sub.1 and R.sub.2 are both the same halogen, by treatment with a formylating agent in a halogenated hydrocarbon solvent to obtain the corresponding compound in which R.sub.1 and R.

Abstract: A process for preparing compounds of the formula ##STR1## in which R is hydrogen or methoxy,R.sub.1 is a hydroxyl group,R.sub.2 is chlorine, bromine, OAc or SHET,R.sub.3 is hydrogen or a cleavable carboxy-protecting group preferably selected from loweralkyl, benzyl, benzhydryl, loweralkoxyloweralkyl, loweralkoxybenzyl, phenacyl, trimethylsilyl, 2,2,2-trichloroethyl or pivaloloxy,R.sub.4 is hydrogen or a cleavable amino-protecting acyl group, or R.sub.4 NH represents phthalimido, andHET is a five or six membered aromatic heterocycle containing 1-4 heteroatoms and optionally substituted with loweralkyl,and from which the corresponding 1-oxacephem derivatives can be prepared is described. The novel intermediate compounds of the formula 1 are produced from a penicillin derivative of formula 1 wherein R, R.sub.3 and R.sub.4 are as above described and R.sub.1 and R.sub.

Abstract: 3,4-Diarylisoxazol-5-acetic acids of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are the same or different and are selected from phenyl and naphthyl, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are the same or different and are selected from hydrogen, halogen, trifluoromethyl, lower alkyl, and lower alkoxy, and R.sup.5 is selected from hydrogen, lower alkyl, and lower alkoxy. The compounds have anti-inflammatory, analgesic, and anti-pyretic activities and a low order of toxicity, and methods for their preparation and use are also disclosed.

Abstract: Thiazolineazetidinone derivatives of the formulae 1,2, and 3. ##STR1## wherein R is derived from the commonly known carboxamido groups present in penicillins, R.sup.1 is a carboxy protecting group commonly used in penicillin chemistry, and R.sup.2 is Cl, Br, I, CN, lower alkoxy, lower acyloxy, SCN, SCH.sub.3, S-phenyl, S-heteroaryl such as 5-mercaptotetrazole or 2-mercapto-5-methyl-1,3,4-thiadiazole, NO.sub.3, N.sub.3, NH-phenyl, and N(CH.sub.3).sub.2 with the proviso that R.sup.2 in the compounds of formula 1 is limited to Cl, Br, I, and lower acyloxy, and a process for preparing said compounds from 2-(substituted methyl) penicillin sulfoxides followed by treatment with a base.The compounds of formulae 1,2, and 3 are useful as intermediates in the synthesis of cephalosporins.