Abstract: A compound of the formula: ##STR1## in which R.sup.1 represents alkyl, cycloalkyl or aralkyl, R* represents fluorophenyl or trifluoromethylphenyl when R.sup.1 is alkyl; R* represents dichlorophenyl, neopentyl, trimethylsilylmethyl, dimethylphenylsilylmethyl or a group of the formula: ##STR2## wherein R.sup.2 represents halogen, trifluoromethyl, lower alkyl or lower alkoxy when R.sup.1 is cycloalkyl; or R* represents 2-thienyl, 3-thienyl, neopentyl, trimethylsilylmethyl, dimethylphenylsilylmethyl or a group of the formula: ##STR3## wherein R.sup.3, R.sup.4 and R.sup.5 independently represent halogen, trifluoromethyl, lower alkyl or lower alkoxy when R.sup.1 is aralkyl, m represents 1 or 2, and X represents halogen, imidazolyl, triazolyl, phenylthio or a radical selected from the group consisting of: ##STR4## wherein R.sup.6 represents alkyl, R.sup.7 and R.sup.8 independently represent lower alkyl and R.sup.9 and R.sup.
Abstract: There is disclosed a process for the production of certain 3-hydrocarbyl-3-cephem derivatives wherein the hydrocarbyl group is selected from 1-alkenyl and conjugated and unconjugated 1-polyalkenyl, 1-alkynl, carbocyclic and heterocyclic aryl, and carbocyclic and heterocyclic arylmethyl and, in the case of the 1-alkenyl and conjugated 1-polyalkenyl derivatives, with substantially complete stereospecificity, by coupling a 3-triflyloxy cephem with a hydrocarbyltributylstannane in the presence of bis(dibenzylideneacetonyl)-palladium, a phosphine, and a metal halide such as, for example, zinc chloride. The 3-unsaturated alkyl-3-cephem derivatives so-produced are useful as broad-spectrum antibacterial agents.
Type:
Grant
Filed:
February 26, 1987
Date of Patent:
September 26, 1989
Assignee:
Bristol-Myers Company
Inventors:
Stephen R. Baker, Vittorio Farina, Chester Sapino, Jr.
Abstract: A compound of the formula: ##STR1## in which R.sup.1 represents alkyl, cycloalkyl or aralkyl, R* represents fluorophenyl or trifluoromethylphenyl when R.sup.1 is alkyl; R* represents dichlorophenyl, neopentyl, trimethylsilylmethyl, dimethylphenylsilylmethyl or a group of the formula: ##STR2## wherein R.sup.2 represents halogen, trifluoromethyl, lower alkyl or lower alkoxy when R.sup.1 is cycloalkyl; or R* represents 2-thienyl, 3-thienyl, neopentyl, trimethylsilylmethyl, imethylphenylsilylmethyl or a group of the formula: ##STR3## wherein R.sup.3, R.sup.4 and R.sup.5 independently represent hydrogen, halogen, trifluoromethyl, lower alkyl or lower alkoxy when R.sup.1 is aralkyl, m represents 1 or 2, and X represents halogen, imidazolyl, triazolyl, phenylthio or a radical selected from the group consisting of: ##STR4## wherein R.sup.6 represents alkyl, R.sup.7 and R.sup.8 independently represent lower alkyl and R.sup.9 and R.sup.
Abstract: Tin compounds, a process for the preparation thereof, a process for the preparation of a medicine using such a tin compound for the treatment of malignant tumors in mice as well as the shaped medicine thus obtained.This invention relates to novel tin compounds, a pharmaceutical composition using the novel compounds and methods for treating cancer using the pharmaceutical composition.
Type:
Grant
Filed:
September 13, 1982
Date of Patent:
October 15, 1985
Assignee:
Nederlandse Centrale Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek